Below please find all papers generated by the Lead Identification Division and its scientific staff. If an article is available for viewing in PubMed, clicking on the PubMed ID (PMID) number for the relevant article will direct you to the appropriate viewing website.
There are currently 164 papers that have been either published or accepted.
164 – Delgado R, Vishwakarma J, Moghadasi S, Otsuka Y, Shumate J, Cuell A, Tansiongco M, Cooley C, Chen Y, Dabrowska A, Basu R, Anindita P, Luo D, Dosa P, Harki D, Bannister T, Scampavia L, Spicer T, Harris R.
SARS-CoV-2 Mpro Inhibitor Identification Using a Cellular Gain-of-Signal Assay for High-Throughput Screening
SLAS Discovery. 2024 Aug. 39173830
163 – Otsuka Y, Kim E, Krueger A, Shumate J, Wang C, Bdiri B, Ullah S, Park H, Scampavia L, Bannister T, Chung D, Spicer T.
High Throughput Screening for SARS-CoV-2 Helicase InhibitorsSLAS Discovery. 2024 Aug. 39173831
162 – Otsuka Y, Zhang L, Mou H, Shumate J, Kitzmiller C, Scampavia L, Bannister T, Farzan M, Choe H, Spicer T.
Simultaneous Screening for Selective SARS-CoV-2, Lassa, and Machupo Virus Entry InhibitorsSLAS Discovery. 2024 Aug. 39159824
161 – Anindita PD, Otsuka Y, Lattmann S, Ngo KH, Kang C, Harris RS, Scampavia L, Spicer T, Luo D.
A High-Throughput Cell-Based Screening Method for Zika Virus Protease Inhibitors DiscoverySLAS Discovery. 2024 May. 38796112
160 – Sprague D, Park S, Gramberg S, Bauer L, Rohr C, Chulkov C, Smith E, Scampavia L, Spicer T, Haeberlein S, Marchant J.
Target-based Discovery of a Broad-Spectrum FlukicideNature Structural & Molecular Biology. 2024 May. 37790347
159 – Smith E, Dickson L, Pickford P, Rowland A, Shumate J, Perez K, Scampavia L, Hernandez D, Spicer T.
Protocol for Kinetic Mode Potassium Channel Assays on Common Plate Readers and MicroscopesSLAS Discovery. 2024 March. 38677875
158 – Aziz F, Reddy K, Fernandez-Vega V, Dey R, Hicks K, Rao S, Ortiz L, Smith E, Shumate J, Scampavia L, Carpino N, Spicer T, French J.
Rebamipide and Derivatives are Potent, Selective Inhibitors of Histidine Phosphatase Activity of the Suppressor of T Cell Receptor Signaling ProteinsJournal of Medicinal Chemistry. 2024 January. 38252624
157 – Ortiz L, Fernandez-Vega V, Shumate J, Peles A, Zeiger J, Scampavia L, Spicer T.
Protocol for High Throughput 3D Drug Screening of Patient Derived Melanoma and Renal Cell CarcinomaSLAS Discovery. 2024 January. 38218316
156 – Coant N, Bickel JD, Rahaim R, Otsuka Y, Choi Y, Xu R, Simoes M, Cariello C, Mao C, Saied EM, Arenz C, Spicer TP, Bannister TD, Tonge PJ, Airola MV, Scampavia L, Hannun Y, Rizzo RC, Haley JD.
Neutral ceramidase-active site inhibitor chemotypes and binding modesBioorganic Chemistry. 2023 October. 37531819
155 – Lee E, Archasappawat S, Ji K, Pena J, Fernandez-Vega V, Gangaraju R, Beesabathuni NS, Kim MJ, Tian Q, Shah P, Scampavia L, Spicer T, Hwang CI
A new vulnerability to BET inhibition due to enhanced autophagy in BRCA2 deficient pancreatic cancerCell Death & Disease. 2023 September. 37398312
154 – Rajan RG, Fernandez-Vega V, Sperry J, Nakashima J, Do LH, Andrews W, Boca S, Islam R, Chowdhary SA, Seldin J, Souza GR, Scampavia L, Hanafy KA, Vrionis FD, Spicer TP
In Vitro and In Vivo Drug-Response Profiling Using Patient-Derived High-Grade GliomaCancers. 2023 June. 37444398
153 – Hou S, Li Z, Chen X, Wang W, Duan T, Scampavia L, Yuan Y, Spicer TP, Chen X, Xie T
Elemene sensitizes pancreatic cancer cells to bortezomib by enhancing proteasome inhibition via molecular patch mechanismNature – Signal Transduction and Targeted Therapy. 2023 February. 36849489
152 – Liao GY, Xu H, Shumate J, Scampavia L, Spicer T, Xu B
High throughput assay for compounds that boost BDNF expression in neuronsSLAS Discovery. 2023 February. 36842668
151 – Fernandez-Vega V, Yang D, Jordán LO, Ye F, Conway L, Chen LY, Shumate J, Baillargeon P, Scampavia L, Souza G, Parker C, Shen B, Spicer TP
Protocol for 3D Screening of Lung Cancer Spheroids using Natural ProductsSLAS Discovery. 2023 January. 36681384
150 – Liu Z, Chen K, Dai J, Xu P, Sun W, Liu W, Zhao Z, Bennett SP, Li P, Ma T, Lin Y, Kawakami A, Yu J, Wang F, Wang C, Li M, Chase P, Hodder P, Spicer TP, Scampavia L, Cao C, Pan L, Dong J, Chen Y, Yu B, Guo M, Fang P, Fisher DE, Wang J
A unique hyperdynamic dimer interface permits small molecule perturbation of the melanoma oncoprotein MITF for melanoma therapy.Nature – Cell Research. 2023 January. 36588115
149 – Smith E, Davis-Gardner ME, Garcia-Ordonez RD, Nguyen TT, Hull M, Chen E, Yu X, Bannister TD, Baillargeon P, Scampavia L, Griffin P, Farzan M, Spicer TP
High Throughput Screening for Drugs that Inhibit 3C-Like Protease in SARS-CoV-2SLAS Discovery. 2023 January. 36646172
148 – Reed A, Ichu TA, Milosevich N, Melillo B, Schafroth MA, Otsuka Y, Scampavia L, Spicer TP, Cravatt BF
LPCAT3 Inhibitors Remodel the Polyunsaturated Phospholipid Content of Human Cells and Protect from Ferroptosis.ACS Chem Biol. 2022 June. 35658397
147 – Moghadasi SA, Esler MA, Otsuka Y, Becker JT, Moraes SN, Anderson CB, Chamakuri S, Belica C, Wick C, Harki DA, Young DW, Scampavia L, Spicer TP, Shi K, Aihara H, Brown WL, Harris RS
Gain-of-Signal Assays for Probing Inhibition of SARS-CoV-2 Mpro/3CLpro in Living Cells.mBio 2022 April. 35471084
146 – Souza G, Spicer TP
SLAS special issue editorial 2022: 3D cell culture approaches of microphysiologically relevant modelsSLAS Discovery. 2022 Mar. 35339725
145 – Smith E, Campbell S, Wilson A, Shumate J, Baillargeon P, Scampavia L, Kamenecka T, Spicer TP, Solt L
High throughput screening for compounds to the orphan nuclear receptor NR2F6SLAS Discovery. 2022 Mar. 35331960
144 – Fernandez-Vega V, Hou S, Plenker D, Tiriac H, Baillargeon P, Shumate J, Scampavia L, Seldin J, Souza G, Tuveson D, Spicer TP
Lead Identification using 3D Models of Pancreatic CancerSLAS Discovery. 2022 Mar. 35306207
143 – Rajendra Rao S, Kostic A, Baillargeon P, Fernandez-Vega V, Rios de Anda M, Fletcher K, Shumate J, Scampavia L, Buxbaum J, Spicer TP
Screening for Modulators of Autism Spectrum Disorder Using Induced Human NeuronsSLAS Discovery. 2022 Feb. 35123134
142 – Baillargeon P, Fernandez-Vega V, Ortiz L, Shumate J, Marques N, Deng L, Spicer TP, Scampavia L
Rapid Deployment of Inexpensive Open-Source Orbital Shakers in Support of High-Throughput ScreeningSLAS Technology. 2022 Jan. 35066236
141 – Chulkov E, Smith E, Rohr C, Yahya N, Park S, Scampavia L, Spicer TP, Marchant J
Identification of novel modulators of a schistosome transient receptor potential channel targeted by praziquantelPLoS Negl Top Dis. 2021 Nov. 34731172
140 – Mediouni S, Mou H, Otsuka Y, Jablonski J, Adcock R, Batra L, Chung D, Rood C, S. de Vera I, Rahaim Jr. R, Ullah S, Yu X, Getmanenko Y, Kennedy N, Wang C, Nguyen T, Hull M, Chen E, Bannister T, Baillargeon P, Scampavia L, Farzan M, Valente S, Spicer TP
Identification of Potent Small Molecule Inhibitors of SARS-CoV-2 EntrySLAS Discovery<. 2021 October. 35058179
139 – Shirey R, Hart J, Sridharan B, Novick S, Turner L, Zhou B, Nielsen A, Eubanks L, Ueno L, Hixon M, Lairson L, Spicer TP, Scampavia L, Griffin P, Vogt P, Janda K
Synthetic fluorescent MYC probe: Inhibitor binding site elucidation and development of a high-throughput screening assayBioorganic & Medicinal Chemistry. 2021 July. 34130216
138 – Stoveken H, Fernandez-Vega V, Muntean B, Patil D, Shumate J, Bannister J, Scampavia L, Spicer TP, Martemyanov
Identification of Potential Modulators of the RGS7/G�5/R7BP ComplexSLAS Discovery. 2021 June. 34112017
137 – Diez J, Rajendrarao S, Baajour S, Sripadhan P, Spicer TP, Scampavia L, Minond D
Development and Pilot Screen of Novel High Content Assay for Down Regulators of Expression of Heterogenous Nuclear Ribonuclear Protein H2Cell Physiology & Biochemistry. 2021 May. 34014051
136 – Wang C, Diez J, Park H, Spicer TP, Scampavia L, Becker-Pauly C, Fields G, Minond D, Bannister T
Discovery and Optimization of Selective Inhibitors of Meprin a (Part II)Pharmaceuticals. 2021 February. 33673639
135 – Hou S, Diez J, Wang C, Becker-Pauly C, Fields G, Bannister T, Spicer TP, Scampavia L, Minond D
Discovery and Optimization of Selective Inhibitors of Meprin a (Part I)Pharmaceuticals. 2021 January. 33671080
134 – Spicer TP
Drug Discovery Targeting COVID-19SLAS Discovery. 2020 December. 33215959
133 – Smith E, Davis-Gardner M, Garcia-Ordonez R, Nguyen T, Hull M, Chen E, Baillargeon P, Scampavia L, Strutzenberg T, Griffin P, Farzan M, Spicer TP
High-Throughput Screening for Drugs That Inhibit Papain-Like Protease in SARS-CoV-2SLAS Discovery. 2020 October. 33043784
132 – Smith E, Dukovski D, Shumate J, Scampavia L, Miller J, Spicer TP
Identification of Compounds That Promote Readthrough of Premature Termination Codons in the CFTRSLAS Discovery. 2020 October. 33016182
131 – Llamosas N, Arora V, Vij R, Kilinc M, Bijoch L, Rojas C, Reich A, Sridharan B, Willems E, Piper D, Scampavia L, Spicer T, Miller C, Holder J, Rumbaugh G
SYNGAP1 Controls the Maturation of Dendrites, Synaptic Function, and Network Activity in Developing Human NeuronsJournal of Neuroscience. 2020 September. 32887745
130 – Grandjean J, Madhavan A, Cech L, Seguinot B, Paxman R, Smith E, Scampavia L, Powers E, Cooley C, Plate L, Spicer T, Kelly J, Wiseman R
Pharmacologic IRE1/XBP1s activation confers targeted ER proteostasis reprogrammingNature Chemical Biology. 2020 July. 32690944
129 – Otsuka Y, Airola M, Choi Y, Coant N, Snider J, Cariello C, Saied E, Arenz C, Bannister T, Rahaim R, Hannun Y, Shumate J, Scampavia L, Haley J, Spicer T
Identification of Small-Molecule Inhibitors of Neutral Ceramidase (nCDase) via Target-Based High-Throughput ScreeningSLAS Discovery. 2020 July. 32734807
128 – Smith E, Janovick JA, Bannister T, Shumate J, Ganapathy V, Scampavia L, Spicer T
Rescue of mutant gonadotropin-releasing hormone receptor function independent of cognate receptor activityNature Scientific Reports. 2020 June. 32601341
127 – Boca S, Bhuvaneshwar K, Fernandez-Vega V, Kancherla J, Rao S, Madhavan S, Riggins R, Beckman R, Bravo H, Scampavia L, Spicer T
Prioritizing targeted therapies in an evidence-based manner, integrating biological context and functional precision medicineJournal of Clinical Oncology. 2020 May.
126 – Wang L, Cheng C, Qin J, Xu M, Kao C, Shi J, You E, Gong W, Pedro-Rosa L, Chase P, Scampavia L, Madoux F, Spicer T, Hodder P, Xu H, Tsai S, Tsai M
Small-molecule inhibitor targeting orphan nuclear receptor COUP-TFII for prostate cancer treatmentScience Advances. 2020 April. 32494682
125 – Pan C, Otsuka Y, Sridharan B, Woo M, Leiton C, Babu S, Goncalves M, Kawalerski R, Bai J, Change D, Biankin A, Scampavia L, Spicer T, Escobar-Hoyos L, Shroyer K
An Unbiased High-Throughput Drug Screen Reveals a Potential Therapeutic Vulnerability in the Most Lethal Molecular Subtype of Pancreatic CancerMolecular Oncology. 2020 June. 32533886
124 – Pan C, Leiton C, Roa-Pena L, Kawalerski R, Moffitt R, Zhao J, Spicer T, Bailey P, Chang D, Biankin A, Duong T, Singh P, Shroyer K, Escobar-Hoyos L
Abstract C39: A novel rewired pathway of nucleotide metabolism drives chemoresistance in pancreatic cancerAACR Special Conference on Pancreatic CAncer: Advances in Science and Clinical Care. 2019 December.
123 – Perez O, Pena J, Fernandez-Vega V, Scampavia L, Spicer T
Drug Discovery and Development, Third EditionCRC Press. 2019 December.
122 – Baillargeon P, Spicer TP, Scampavia L
Applications for Open Source Microplate-Compatible Illumination PanelsJoVE. 2019 October. PMID:31633701
Applications for Open Source Microplate-Compatible Illumination Panels
121 – Baillargeon P, Shumate J, Hou S, Fernandez-Vega V, Marques N, Souza G, Seldin J, Spicer TP, Scampavia L
Automating a Magnetic 3D Spheroid Model Technology for High-Throughput ScreeningSLAS Technology. 2019 June. PMID:31225974
120 – Sridharan B, Hubbs C, Llamosas N, Kilinc M, Singhera F, Willems E, Piper D, Scampavia L, Rumbaugh G, Spicer TP
A Simple Procedure for Creating Scalable Phenotypic Screening Assays in Human NeuronsNature Scientific Reports. 2019 June. PMID:31227747
119 – Morgan G, Yan N, Mortenson D, Rennella E, Blundon J, Gwin R, Lin C, Stanfield R, Brown S, Rosen H, Spicer TP, Fernandez-Vega V, Merlini G, Kay L, Wilson I, Kelly J
Stabilization of amyloidogenic immunoglobulin light chains by small moleculesPNAS. 2019 April. PMID:30971495
118 – Zhou W, Yin Y, Smith E, Chou J, Shumate J, Scampavia L, Spicer TP, Carpino N, French JB
Discovery and Characterization of Two Classes of Selective Inhibitors of the Suppressor of the TCR Signaling Family of ProteinsACS Infect Dis. 2019 Feb. PMID:30485744
117 – Baillargeon P, Coss-Flores K, Singhera F, Shumate J, Williams H, DeLuca L, Spicer TP, Scampavia L
Design of Microplate-Compatible Illumination Panels for a Semiautomated Benchtop Pipetting SystemSLAS Technology. 2019 January. PMID:30698997
116 – Baillargeon P, Fernandez-Vega V, Sridharan B, Brown S, Griffin P, Rosen H, Cravatt B, Scampavia L, Spicer TP
The Scripps Molecular Screening Center and Translational Research InstituteSLAS Discovery. 2019 January. PMID:30682260
115 – Spicer TP, Fernandez-Vega V, Scampvia L, Willetts L, Vessels M
A Novel 3D Culture System for High-Throughput Hepatoxicity ScreeningBioProcess International. 2018 October. PMID:
114 – Spicer TP, Gardiner DL, Schoenen FJ, Roy S, Griffin PR, Chase P, Scampavia L, Hodder P, Trenholme KR
Identification of Antimalarial Inhibitors Using Late-Stage Gametocytes in a Phenotypic Live/Dead AssaySLAS Discovery. 2018 August. PMID:30142014
113 – Janovick JA, Spicer TP, Bannister TD, Smith E, Ganapathy V, Scampavia L
Chemical Validation and Optimization of Pharmacoperones Targeting Vasopressin Type 2 Receptor MutantBiochem J. 2018 August. PMID:30068530
112 – Nieto A, Fernandez-Vega V, Spicer TP, Sturchler E, Adhikari P, Kennedy N, Mandat S, Chase P, Scampavia L, Bannister T, Hodder P, McDonald PH
Identification of Novel, Structurally Diverse, Small Molecule Modulators of GPR119Assay Drug Dev Technol. 2018 July. PMID:30019946
111 – Quereda V, Hou S, Madoux F, Scampavia L, Spicer T, Duckett D
A Cytotoxic Three-Dimensional-Spheroid, High-Throughput Assay Using Patient-Derived Glioma Stem CellsSLAS Discovery. 2018 May. PMID:29750582
110 – Kota S, Hou S, Guerrant W, Madoux F, Troutman S, Fernandez-Vega V, Alekseeva N, Madala N, Scampavia L, Kissil J, Spicer T
A novel three-dimensional high-throughput screening approach identifies inducers of a mutant KRAS selective lethal phenotypeOncogene. 2018 May. PMID:29743592
109 – Muntean BS, Patil DN, Madoux F, Fossetta J, Scampavia L, Spicer T, Martemyanov KA
A High-Throughput Time-Resolved Fluorescence Energy Transfer Assay to Screen for Modulators of RGS7/GB5/R7BP ComplexAssay Drug Dev Technol. 2018 Apr. PMID:29658790
108 – Hou S, Tiriac H, Sridharan B, Scampavia L, Madoux F, Seldin J, Souza G, Watson D, Tuveson D, Spicer T
Advanced Development of Primary Pancreatic Organoid Tumor Models for High-Throughput Phenotypic Drug ScreeningSLAS Discovery. 2018 Apr. PMID:29673279
107 – Shumate J, Baillargeon P, Spicer T, Scampavia L
IoT for Real-Time Measurement of High-Throughput Liquid Dispensing in Laboratory EnvironmentsSLAS Technology. 2018 Apr. PMID:29649373
106 – Wolff R, Wang-Gillam A, Alvarez H, Tiriac H, Engle D, Hou S, Groff A, San Lucas A, Bernard V, Allenson K, Castillo J, Kim D, Mulu F, Huang J, Stephens B, Wistuba I, Katz M, Varadhachary G, Park Y, Hicks J, Chinnaiyan A, Scampavia L, Spicer T, Gerhardinger C, Maitra A, Tuveson D, Rinn J, Lizee G, Yee C, Levine A
Dynamic changes during the treatment of pancreatic cancer.Oncotarget. 2018 Feb. PMID:29599906
105 – Smith E, Giuliano KA, Shumate J, Baillargeon P, McEwan B, Cullen MD, Miller JP, Drew L, Scampavia L, Spicer TP
A Homogeneous Cell-Based Halide-Sensitive Yellow Fluorescence Protein Assay to Identify Modulators of the Cystic Fibrosis Transmembrane Conductance Regulator Ion Channel.Assay Drug Dev Technol. 2017 Nov. PMID:29172645
104 – Spicer T, Hubbs C, Vaissiere T, Collia D, Rojas C, Kilinc M, Vick K, Madoux F, Baillargeon P, Shumate J, Martemyanov K.A., Page D.T., Puthanveettil S, Hodder P, Davis R, Miller C.A., Scampavia L, Rumbaugh G
Improved Scalability of Neuron-Based Phenotypic Screening Assays for Therapeutic Discovery in Neuropsychiatric Disorders.Molecular Neuropsychiatry. 2017 Nov. PMID:29594133
103 – Singhera F, Cooper E, Scampavia L, Spicer T
Using bead injection to model dispensing of 3-D multicellular spheroids into microtiter plates.Talanta. 2017 Sep. PMID:29108585
102 – Kong J, Fang P, Madoux F, Spicer T, Scampavia L, Kim S, Guo M
High-Throughput Screening for Protein Synthesis Inhibitors Targeting Aminoacyl-tRNA Synthetases.SLAS Discovery. 2017 Oct. PMID:29020503
101 – Collia D, Bannister T, Tan H, Jin S, Langaee T, Shumate J, Scampavia L, Spicer T
A Rapid Phenotypic Whole-Cell Screening Approach for the Identification of Small-Molecule Inhibitors That Counter B-Lactamase Resistance in Pseudomonas aeruginosa.SLAS Discovery. 2017 Aug. PMID:28850797
100 – Janovick JA, Spicer TP, Scampavia L, Conn PM
Pharmacoperone rescue of vasopressin 2 receptor mutants reveals unexpected constitutive activity and coupling bias.PLoS One. 2017 Aug. PMID:28767678
99 – Powell K
Adding depth to cell culture.Science. 2017 Apr. PMID:
98 – Hou S, Madoux F, Scampavia L, Janovick JA, Conn PM, Spicer TP
Drug Library Screening for the Identification of Ionophores That Correct the Mistrafficking Disorder Associated with Oxalosis Kidney Disease.SLAS Discovery. 2017 Jan. PMID:28346094
97 – Madoux F, Tanner A, Vessels M, Willetts L, Hou S, Scampavia L, Spicer T.
A 1536-Well 3D Viability Assay to Assess the Cytotoxic Effect of Drugs on Spheroids.SLAS Discovery. 2017 Jan. PMID:28346088
96 – Madoux F, Dreymuller D, Pettiloud JP, Santos R, Becker-Pauly C, Ludwig A, Fields GB, Bannister T, Spicer TP, Cudic M, Scampavia LD, Minond D
Discovery of an enzyme and substrate selective inhibitor of ADAM10 using an exosite-binding glycosylated substrate.
Sci Rep. 2016 Dec. PMID:27920432
95 – Wang J, Fang P, Chase P, Tshori S, Razin E, Spicer TP, Scampavia L, Hodder P, Guo M
Development of an HTS-Compatible Assay for Discovery of Melanoma-Related Microphthalmia Transcription Factor Disruptors Using AlphaScreen Technology.
Journal of Biomolecular Screening. 2016 Nov. PMID:27827304
94 – Swingle M, Volmar CH, Saldanha SA, Chase P, Eberhart C, Salter EA, D’Arcy B, Schroeder CE, Golden JE, Wierzbicki A, Hodder P, Honkanen RE
An Ultra-High-Throughput Screen for Catalytic Inhibitors of Serine/Threonine Protein Phosphatases Types 1 and 5 (PP1C and PP5C).J Biomol Screen. 2016 Sept. PMID:27628691
93 – Plate L, Cooley CB, Chen JJ, Paxman RJ, Gallagher CM, Madoux F, Genereux JC, Dobbs W, Garza D, Spicer TP, Scampavia L, Brown SJ, Rosen H, Powers ET, Walter P, Hodder P, Weisman RL, Kelly JW.
Small molecule proteostasis regulators that reprogram the ER to reduce extracellular protein aggregation.
Elife. 2016 Jul 20. PMID:27435961
92 – Janovick JA, Spicer TP,Smith E, Bannister TD, Kenakin T, Scampavia L, Conn PM.
Receptor antagonism/agonism can be uncoupled from pharmacoperone activity.
Mol Cell Endocrinol. 2016 Jul 4. PMID:27389877
91 – Smith E, Janovick JA, Bannister TD, Shumate J, Scampavia L, Conn PM, Spicer TP.
Identification of Potential Pharmacoperones Capable of Rescuing the Functionality of Misfolded Vasopressin 2 Receptor Involved in Nephrogenic Diabetes Insipidus.
Journal of Biomolecular Screening. 2016 Jun 8. PMID:27280550
90 – Ewing H, Fernandez-Vega V, Spicer T, Chase P, Brown S, Scampavia L, Roush W, Riley S, Rosen H, Hodder P, Lambeau G, Gelb M.
Fluorometric High-Throughput Screening Assay for Secreted Phospholipases A2 Using Phospholipid Vesicles.
Journal of Biomolecular Screening. 2016 May 4. PMID:27146384
89 – Thenin-Houssier S, de Vera IM, Pedro-Rosa L, Brady A, Richard A, Konnick B, Opp S, Buffone C, Fuhrmann J, Kota S, Billack B, Pietka-Ottlik M, Tellinghuisen T, Choe H, Spicer T, Scampavia L, Diaz-Griffero F, Kojetin DJ, Valente ST.
Ebselen, a Small-Molecule Capsid Inhibitor of HIV-1 ReplicationAntimicrobial Agents and Chemotherapy. 2016 Mar. 25 PMID:26810656
88 – Jambrina E, Cerne R, Smith E, Scampavia L, Cuadrado M, Findlay J, Krambis M, Wakulchik M, Chase P, Brunavs M, Burris K, Gallagher P, Spicer T, Ursu D.
An Integrated Approach for Screening and Identification of Positive Allosteric Modulators of N-Methyl-D-Aspartate Receptors.
Journal of Biomolecular Screening. 2016 Feb 2. PMID:26838761
87 – Chase P, Enogieru I, Madoux F, Bishop E, Beer J, Scampavia L, Spicer T.
An Automated Miniaturized Method to Perform and Analyze Antimicrobial Drug Synergy Assays.
Assay and Drug Development Technologies. 2015 Dec 15. PMID:26669516
86 – Palde PB, Bhaskar A, Pedró Rosa LE, Madoux F, Chase P, Gupta V, Spicer T, Scampavia L, Singh A, Carroll KS. .
First-In-Class Inhibitors of Sulfur Metabolism with Bactericidal Activity against Non-Replicating M. tuberculosis.
ACS Chem Biol. 2015 Nov 2. PMID:26524379
85 – Sanders MA, Madoux F, Mladenovic L, Zhang H, Ye X, Angrish M, Mottillo EP, Caruso JA, Halvorsen G, Roush WR, Chase P, Hodder P, Granneman JG.
Endogenous and Synthetic ABHD5 Ligands Regulate ABHD5-Perilipin Interactions and Lipolysis in Fat and Muscle.
Cell Metab. 2015 Sep 22. PMID:26411340
84 – Abdul-Hay SO, Bannister TD, Wang H, Cameron MD, Caulfield TR, Masson A, Bertrand J, Howard EA, McGuire MP, Crisafulli U, Rosenberry TR, Topper CL, Thompson CR, Schurer SC, Madoux F, Hodder P, Leissring MA.
Selective targeting of extracellular insulin-degrading enzyme by quasi-irreversible thiol-modifying inhibitors.
ACS Chem Biol. 2015 Sep 23. PMID:26398879
83 – Conn PM, Spicer TP, Scampavia L, Janovick JA.
Assay strategies for identification of therapeutic leads that target protein trafficking.
Trends Pharmacol Sci. 2015 Jun 8. PMID:26067100
82 – Schreiber S, Kotz J, Li M, Aube J, Austin C, Reed J, Rosen H, White E, Sklar L, Lindsley C, Alexander B, Bittker J, Clemons P, Souza A, Foley M, Palmer M, Shamji A, Wawer M, McManus O, Wu M, Zou B, Yu H, Golden J, Schoenen F, Simenov A, Jadhav A, JAckson M, Pinkerton A, Chung T, Griffin P, Cravatt B, Hodder P, Roush W, Roberts E, Chung D, Jonsson C, Noah J, Severson W, Ananthan S, Edwards B, Oprea T, Conn PM, Hopkins C, Wood M, Stauffer S, Emmitte K
Advancing Biological Understanding and Therapeutics Discovery with Small Moleucle Probes.
Cell. 2015 Jun 4. PMID:26046436
81 – Smith E, Chase P, Niswender C, Utley T, Sheffler D, Noetzel M, Lamsal A, Wood M, Conn PJ, Lindsley C, Madoux F, Acosta M, Scampavia L, Spicer T, Hodder P.
Application of Parallel Multiparametric Cell-Based FLIPR Detection Assays for the Identification of Modulators of the Muscarinic Acetylcholine Receptor 4 (M4).
J Biomol Screen. 2015 Apr 16. PMID:25877150
80 – Chang J, Zuhl A, Speers A, Niessen S, Brown S, Mulvihill M, Spicer TP, Southern M, Scampavia L, Fernandez-Vega V, Ferguson J, Dix M, Hodder P, Rosen H, Nomura D, Kwon O, Hsu K-L, Cravatt B.
A selective inhibitor of platelet-activating factor acetylhydrolases 1b2 and 1b3 that impairs cancer cell survival.
ACS Chem Biol. 2015 Jan 20. PMID:25602368
79 – Madoux F, Janovick JA, Smithson D, Fargue S, Danpure CJ, Scampavia L, Chen YT, Spicer TP, Conn PM.
Development of a Phenotypic High-Content Assay to Identify Pharmacoperone Drugs for the Treatment of Primary Hyperoxaluria Type 1 by High-Throughput ScreeningAssay Drug Dev Technol. 2015 January/February;13(1):16-24. PMID:25710543
78 – Wang Y, Stowe RL, Pinello CE, Tian G, Madoux F, Li D, Zhao LY, Li JL, Wang Y, Wang Y, Ma H, Hodder P, Roush WR, Liao D
Identification of Histone Deacetylase Inhibitors with Benzoylhydrazide Scaffold that Selectively Inhibit Class I Histone DeacetylasesChem Biol. 2015 Feb 19;22(2):273-84. doi: 10.1016/j.chembiol.2014.12.015. PMID:25699604
77 – Cameron M, Kamenecka T, Madoux F, Chase P, Roush W, Hodder P
ML368 Identification of Imidazopyridines as Selective Inhibitors of the Cytochrome P450 Enzyme CYP3A4Probe Reports from the NIH Molecular Libraries Program. PMID:21433368
76 – Zhao N1, Darby CM, Small J, Bachovchin DA, Jiang X, Burns-Huang KE, Botella H, Ehrt S, Boger DL, Anderson ED, Cravatt BF, Speers AE, Fernandez-Vega V, Hodder PS, Eberhart C, Rosen H, Spicer TP, Nathan CF
Target-Based Screen Against a Periplasmic Serine Protease That Regulates Intrabacterial pH Homeostasis in Mycobacterium tuberculosisACS Chem Biol. 2014 Dec 5. [Epub ahead of print]. PMID:25457457
75 – Kadakkuzha BM, Spicer TP, Chase P, Richman JB, Hodder P, Puthanveettil SV.
High-throughput screening for small molecule modulators of motor protein Kinesin.
Assay Drug Dev Technol. 2014 Oct. PMID:25383721
74 – Timothy P. Spicer, Jianwen Jiang, Alexander B. Taylor, Jun-Yong Choi, P. JohnHart, William R. Roush, Gregg B. Fields, Peter S. Hodder, and Dmitriy Minond
Characterization of Selective Exosite-Binding Inhibitors of Matrix Metalloproteinase 13 That Prevent Articular Cartilage Degradation In Vitro J Medicinal Chemistry. 2014 Oct 20. [Epub ahead of print]. PMID:25330343
73 – Pedró-Rosa L, Buckner FS, Ranade RM, Eberhart C, Madoux F, Gillespie JR, Koh CY, Brown S, Lohse J, Verlinde CL, Fan E, Bannister T, Scampavia L, Hol WG, Spicer T, Hodder P
Identification of Potent Inhibitors of the Trypanosoma brucei Methionyl-tRNA Synthetase via High-Throughput Orthogonal Screening J Biomol Screen. 2014 Aug 27. pii: 1087057114548832. [Epub ahead of print]. PMID: 25163684
72 – Gentry PR, Kokubo M, Bridges TM, Noetzel MJ, Cho HP, Lamsal A, Smith E, Chase P, Hodder PS, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Wood MR
Development of a Highly Potent, Novel M5 Positive Allosteric Modulator (PAM) Demonstrating CNS Exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380)J Med Chem. 2014 Aug 22. [Epub ahead of print]. PMID: 25147929
71 – Madoux F, Tredup C, Spicer TP, Scampavia L, Chase PS, Hodder PS, Fields GB, Becker-Pauly C, Minond D
Development of HTS assays and pilot screen for inhibitors of metalloproteases meprin α and βBiopolymers. 2014 Jul 21. doi: 10.1002/bip.22527. [Epub ahead of print]. PMID: 25048711
70 – Conn PM, Smith E, Spicer T, Chase P, Scampavia L, Janovick JA
A phenotypic high throughput screening assay for the identification of pharmacoperones for the gonadotropin releasing hormone receptor Assay Drug Dev Technol. 2014 May;12(4):238-46. doi: 10.1089/adt.2014.576. PMID: 24831790
69 – Sturchler E, Chen W, Spicer T, Hodder P, McDonald P, Duckett D
Development of an HTS-Compatible Assay for the Discovery of ASK1 Signalosome Inhibitors Using AlphaScreen TechnologyAssay Drug Dev Technol. 2014 May;12(4):229-37. doi: 10.1089/adt.2013.558. PMID: 24831789
68 – Penas C, Ramachandran V, Simanski S, Lee C, Madoux F, Rahaim RJ, Chauhan R, Barnaby O, Schurer S, Hodder P, Steen J, Roush WR, Ayad NG
Casein Kinase 1δ Dependent Wee1 DegradationJ Biol Chem. 2014 Jul 4;289(27):18893-18903. Epub 2014 May 9. PMID: 24817118
67 – Yan F, Yu Y, Chow DC, Palzkill T, Madoux F, Hodder P, Chase P, Griffin PR, O’Malley BW, Lonard DM
Identification of verrucarin a as a potent and selective steroid receptor coactivator-3 small molecule inhibitor PLoS One. 2014 Apr 17;9(4):e95243. doi: 10.1371/journal.pone.0095243. eCollection 2014. PMID: 24743578
66 – Gentry PR, Kokubo M, Bridges TM, Cho HP, Smith E, Chase P, Hodder PS, Utley TJ, Rajapakse A, Byers F, Niswender CM, Morrison RD, Daniels JS, Wood MR, Conn PJ, Lindsley CW
Discovery, Synthesis and Characterization of a Highly Muscarinic Acetylcholine Receptor (mAChR)-Selective M5 -Orthosteric Antagonist, VU0488130 (ML381): A Novel Molecular Probe ChemMedChem. 2014 Aug;9(8):1677-82. doi: 10.1002/cmdc.201402051. Epub 2014 Apr 1. PMID: 24692176
65 – Spicer T, Fernandez-Vega V, Chase P, Scampavia L, To J, Dalton JP, Da Silva FL, Skinner-Adams TS, Gardiner DL, Trenholme KR, Brown CL, Ghosh P, Porubsky P, Wang JL, Whipple DA, Schoenen FJ, Hodder P
Identification of Potent and Selective Inhibitors of the Plasmodium falciparum M18 Aspartyl Aminopeptidase (PfM18AAP) of Human Malaria via High-Throughput Screening J Biomol Screen. 2014 Mar 11. [Epub ahead of print]. PMID: 24619116
64 – Lewallen DM, Bicker KL, Madoux F, Chase P, Anguish L, Coonrod S, Hodder P, Thompson PR
A FluoPol-ABPP PAD2 High-Throughput Screen Identifies the First Calcium Site Inhibitor Targeting the PADs ACS Chem Biol. 2014 Apr 18;9(4):913-21. doi: 10.1021/cb400841k. Epub 2014 Jan 27. PMID: 24467619
63 – Wang Y, Lonard DM, Yu Y, Chow DC, Palzkill TG, Wang J, Qi R, Matzuk AJ, Song X, Madoux F, Hodder P, Chase P, Griffin PR, Zhou S, Liao L, Xu J, O’Malley BW
Bufalin is a potent small molecule inhibitor of the steroid receptor coactivators SRC-3 and SRC-1 Cancer Res. 2014 Mar 1;74(5):1506-17. doi: 10.1158/0008-5472.CAN-13-2939. Epub 2014 Jan 3. PMID: 24390736
62 – Conn PM, Smithson DC, Hodder PS, Stewart MD, Behringer RR, Smith E, Ulloa-Aguirre A, Janovick JA
Transitioning pharmacoperones to therapeutic use: In vivo proof-of-principle and design of high throughput screens Pharmacol Res. 2014 May;83:38-51. doi: 10.1016/j.phrs.2013.12.004. Epub 2013 Dec 25. PMID: 24373832
61 – Lewallen DM, Sreelatha A, Dharmarajan V, Madoux F, Chase P, Griffin PR, Orth K, Hodder P, Thompson PR
Inhibiting AMPylation: a novel screen to identify the first small molecule inhibitors of protein AMPylation ACS Chem Biol. 2014 Feb 21;9(2):433-42. doi: 10.1021/cb4006886. Epub 2013 Nov 25. PMID: 24274060
60 – Zhou L, Lovell KM, Frankowski KJ, Slauson SR, Phillips AM, Streicher JM, Stahl EL, Schmid CL, Hodder P, Madoux F, Cameron MD, Prisinzano TE, Aube J, Bohn LM
Development of functionally selective, small molecule agonists at kappa opioid receptors J Biol Chem. 2013 Dec 20;288(51):36703-16. doi: 10.1074/jbc.M113.504381. Epub 2013 Nov 1. PMID: 24187130
59 – Gentry PR, Kokubo M, Bridges TM, Kett NR, Harp JM, Cho HP, Smith E, Chase P, Hodder PS, Niswender CM, Daniels JS, Conn PJ, Wood MR, Lindsley CW
Discovery of the First M5-Selective and CNS Penetrant Negative Allosteric Modulator (NAM) of a Muscarinic Acetylcholine Receptor: (S)-9b-(4-Chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375) J Med Chem. 2013 Nov 27;56(22):9351-5. doi: 10.1021/jm4013246. Epub 2013 Nov 13. PMID: 24164599
58 – Guerrero M, Poddutoori R, Urbano M, Peng X, Spicer TP, Chase PS, Hodder PS, Schaeffer MT, Brown S, Rosen H, Roberts E
Discovery, design and synthesis of a selective S1P3 receptor allosteric agonist Bioorg Med Chem Lett. 2013 Dec 1;23(23):6346-9. doi: 10.1016/j.bmcl.2013.09.075. Epub 2013 Oct 1. PMID: 24135724
57 – Turlington M, Chun A, Tomar S, Eggler A, Grum-Tokars V, Jacobs J, Daniels JS, Dawson E, Saldanha A, Chase P, Baez-Santos YM, Lindsley CW, Hodder P, Mesecar AD, Stauffer SR
Discovery of N-(benzo[1,2,3]triazol-1-yl)-N-(benzyl)acetamido)phenyl) carboxamides as severe acute respiratory syndrome coronavirus (SARS-CoV) 3CLpro inhibitors: Identification of ML300 and noncovalent nanomolar inhibitors with an induced-fit binding Bioorg Med Chem Lett. 2013 Nov 15;23(22):6172-7. doi: 10.1016/j.bmcl.2013.08.112. Epub 2013 Sep 7. PMID: 24080461
56 – Richard DJ, Lena R, Bannister T, Blake N, Pierceall WE, Carlson NE, Keller CE, Koenig M, He Y, Minond D, Mishra J, Cameron M, Spicer T, Hodder P, Cardone MH
Hydroxyquinoline-derived compounds and analoguing of selective Mcl-1 inhibitors using a functional biomarker Bioorg Med Chem. 2013 Nov 1;21(21):6642-6649. doi: 10.1016/j.bmc.2013.08.017. Epub 2013 Aug 15. PMID: 23993674
55 – Satsu H, Schaeffer MT, Guerrero M, Saldana A, Eberhart C, Hodder P, Cayanan C, Schürer S, Bhhatarai B, Roberts E, Rosen H, Brown SJ
A sphingosine 1-phosphate receptor 2 selective allosteric agonist Bioorg Med Chem. 2013 Sep 1;21(17):5373-82. doi: 10.1016/j.bmc.2013.06.012. Epub 2013 Jun 15. PMID: 23849205
54 – Gomes I, Fujita W, Gupta A, Saldanha SA, Negri A, Pinello CE, Eberhart C, Roberts E, Filizola M, Hodder P, Devi LA
Identification of a mu-delta opioid receptor heteromer-biased agonist with antinociceptive activity Proc Natl Acad Sci U S A. 2013 Jul 16;110(29):12072-7. doi: 10.1073/pnas.1222044110. Epub 2013 Jul 1. PMID: 23818586
53 – Conn PM, Smith E, Hodder P, Janovick JA, Smithson DC
High-throughput screen for pharmacoperones of the vasopressin type 2 receptor J Biomol Screen. 2013 Sep;18(8):930-7. doi: 10.1177/1087057113483559. Epub 2013 May 2. PMID: 23640875
52 – Yang H, Pinello CE, Luo J, Li D, Wang Y, Zhao LY, Jahn SC, Saldanha SA, Chase P, Planck J, Geary KR, Ma H, Law BK, Roush WR, Hodder P, Liao D
Small-molecule inhibitors of acetyltransferase p300 identified by high-throughput screening are potent anticancer agents Mol Cancer Ther. 2013 May;12(5):610-20. doi: 10.1158/1535-7163.MCT-12-0930. Epub 2013 Apr 26. PMID: 23625935
51 – Thomas PW, Spicer T, Cammarata M, Brodbelt JS, Hodder P, Fast W
An altered zinc-binding site confers resistance to a covalent inactivator of New Delhi metallo-beta-lactamase-1 (NDM-1) discovered by high-throughput screening >Bioorg Med Chem. 2013 Jun 1;21(11):3138-46. doi: 10.1016/j.bmc.2013.03.031. Epub 2013 Mar 29. PMID: 23591260
50 – Karapetyan YE, Sferrazza GF, Zhou M, Ottenberg G, Spicer T, Chase P, Fallahi M, Hodder P, Weissmann C, Lasmézas CI
Unique drug screening approach for prion diseases identifies tacrolimus and astemizole as antiprion agents Proc Natl Acad Sci U S A. 2013 Apr 23;110(17):7044-9. doi 10.1073/pnas.1303510110. Epub 2013 Apr 1. PMID: 23576755
49 – Gentry PR, Bridges TM, Lamasal A, Vinson PN, Smith E, Chase P, Hodder PS, Engers JL, Niswender CM, Scott Daniels J, Jeffrey Conn P, Wood MR, Lindsley CW
Discovery of ML326: The first sub-micromolar, selective M5 PAM Bioorg Med Chem Lett. 2013 May 15;23(10):2996-3000. doi: 10.1016/j.bmcl.2013.03.032. Epub 2013 Mar 16. PMID: 23562060
48 – Nagano JM, Hsu KL, Whitby LR, Niphakis MJ, Speers AE, Brown SJ, Spicer T, Fernandez-Vega V, Ferguson J, Hodder P, Srinivasan P, Gonzalez TD, Rosen H, Bahnson BJ, Cravatt BF
Selective inhibitors and tailored activity probes for lipoprotein-associated phospholipase A(2) Bioorg Med Chem Lett. 2013 Feb 1;23(3):839-43. doi: 10.1016/j.bmcl.2012.11.061. Epub 2012 Dec 2. PMID: 23260346
47 – Jacobs J, Grum-Tokars V, Zhou Y, Turlington M, Saldanha SA, Chase P, Eggler A, Dawson ES, Baez-Santos YM, Tomar S, Mielech AM, Baker SC, Lindsley CW, Hodder P, Mesecar A, Stauffer SR
Discovery, synthesis, and structure-based optimization of a series of N-(tert-Butyl)-2-(N-arylamido)-2-(pyridin-3-yl) acetamides (ML188) as potent noncovalent small molecule inhibitors of the severe acute respiratory syndrome coronavirus (SARS-CoV) 3CL protease J Med Chem. 2013 Jan 24;56(2):534-46. doi: 10.1021/jm301580n. Epub 2013 Jan 3. PMID: 23231439
46 – Qin Q, Knapinska A, Dobri N, Madoux F, Chase P, Hodder P, Petrukhin K
In pursuit of synthetic modulators for the orphan retina-specific nuclear receptor NR2E3 J Ocul Pharmacol Ther. 2013 Apr;29(3):298-309. doi: 10.1089/jop.2012.0.0135. Epub 2012 Oct 25. PMID: 23098562
45 – Urbano M, Guerrero M, Zhao J, Velaparthi S, Adrian Saldanha S, Chase P, Wang Z, Civelli O, Hodder P, Schaeffer MT, Brown S, Rosen H, Roberts E
Design, synthesis and SAR analysis of novel potent and selective small molecule antagonists of NPBWR1 (GPR7) Bioorg Med Chem Lett. 2012 Dec 1;22(23):7135-41. doi: 10.1016/j.bmcl.2012.09.074. Epub 2012 Oct 2. PMID: 23079522
44 – Adibekian A, Martin BR, Chang JW, Hsu KL, Tsuboi K, Bachovchin DA, Speers AE, Brown SJ, Spicer T, Fernandez-Vega V, Ferguson J, Hodder PS, Rosen H, Cravatt BF
Confirming target engagement for reversible inhibitors in vivo by kinetically tuned activity-based probes J Am Chem Soc. 2012 Jun 27;134(25):10345-8. Epub 2012 Jun 12. PMID: 22690931
43 – Amundsen SK, Spicer T, Karabulut AC, Londoño LM, Eberhart C, Fernandez Vega V, Bannister TD, Hodder P, Smith GR
Small-molecule inhibitors of bacterial AddAB and RecBCD helicase-nuclease DNA repair enzymes ACS Chem Biol. 2012 May 18;7(5):879-91. Epub 2012 Mar 23. PMID: 22443934
42 – Calamini B, Silva MC, Madoux F, Hutt DM, Khanna S, Chalfant MA, Saldanha SA, Hodder P, Tait BD, Garza D, Balch WE, Morimoto RI
Small-molecule proteostasis regulators for protein conformational diseases Nat Chem Biol. 2011 Dec 25;8(2):185-96. doi: 10.1038/nchembio.763. PMID: 22198733
41 – Guerrero M, Urbano M, Zhao J, Crisp M, Chase P, Hodder P, Schaeffer MT, Brown S, Rosen H, Roberts E
Discovery, design and synthesis of novel potent and selective sphingosine-1-phosphate 4 receptor (S1P4-R) agonists Bioorg Med Chem Lett. 2012 Jan 1;22(1):537-42. Epub 2011 Nov 4. PMID: 22119461
40 – Roth J, Minond D, Darout E, Liu Q, Lauer J, Hodder P, Fields GB, Roush WR
Identification of novel, exosite-binding matrix metalloproteinase-13 inhibitor scaffolds Bioorg Med Chem Lett. 2011 Dec 1;21(23):7180-4. Epub 2011 Sep 22. PMID: 22018790
39 – Urbano M, Guerrero M, Velaparthi S, Crisp M, Chase P, Hodder P, Schaeffer MT, Brown S, Rosen H, Roberts E
Discovery, synthesis and SAR analysis of novel selective small molecule S1P(4)-R agonists based on a (2Z,5Z)-5-((pyrrol-3-yl)methylene)-3-alkyl-2-(alkylimino)thiazolidin-4-one chemotype Bioorg Med Chem Lett. 2011 Nov 15;21(22):6739-45. Epub 2011 Sep 20. PMID: 21982495
38 – Peatey CL, Spicer T, Hodder P, Trenholme KR, Gardiner DL
A high-throughput assay for the identification of drugs against late-stage Plasmodium falciparum gametocytes Mol Biochem Parasitol. 2011 Dec;180(2):127-31. Epub 2011 Sep 16. PMID: 21939693
37 – Tsuboi K, Bachovchin DA, Speers AE, Spicer TP, Fernandez-Vega V, Hodder P, Rosen H, Cravatt BF
Potent and selective inhibitors of Glutathione S-transferase Omega 1 that impair cancer drug resistance J Am Chem Soc. 2011 Oct 19;133(41):16605-16. Epub 2011 Sep 27. PMID: 21899313
36 – Bialkowska A, Crisp M, Bannister T, He Y, Chowdhury S, Schurer S, Chase P, Spicer T, Madoux F, Tian C, Hodder P, Zaharevitz D, Yang VW
Identification of small-molecule inhibitors of the colorectal cancer oncogene Krüppel-like factor 5 expression by ultrahigh-throughput screening Mol Cancer Ther. 2011 Nov;10(11):2043-51. Epub 2011 Sep 1. PMID: 21885866
35 – Lone AM, Bachovchin D, Westwood D, Speers AE, Spicer TP, Fernandez-Vega V, Chase P, Hodder P, Rosen H, Cravatt BF, Saghatelian A
A substrate-free activity-based protein profiling screen for the discovery of selective PREPL inhibitors J Am Chem Soc. 2011 Aug 3;133(30):11665-74. Epub 2011 Jun 21. PMID: 21692504
34 – Baillargeon P, Scampavia L, Einsteder R, Hodder P
Monitoring of HTS compound library quality via a high-resolution image acquisition and processing instrument J Lab Autom. 2011 Jun;16(3):197-203. Epub 2011 May 16. PMID: 21609702
33 – Bachovchin DA, Mohr JT, Speers AE, Wang C, Berlin JM, Spicer TP, Fernandez-Vega V, Chase P, Hodder PS, Schürer SC, Nomura DK, Rosen H, Fu GC, Cravatt BF
Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors Proc Natl Acad Sci U S A. 2011 Apr 26;108(17):6811-6. Epub 2011 Mar 11. PMID: 21398589
32 – Chou TF, Brown SJ, Minond D, Nordin BE, Li K, Jones AC, Chase P, Porubsky PR, Stoltz BM, Schoenen FJ, Patricelli MP, Hodder P, Rosen H, Deshaies RJ
Reversible inhibitor of p97 DBeQ, impairs both ubiquitin-dependent and autophagic protein clearance pathways Proc Natl Acad Sci U S A. 2011 Mar 22;108(12):4834-9. Epub 2011 Mar 7. PMID: 21383145
31 – Istrate MA, Spicer TP, Wang Y, Bernard JA, Helvering LM, Bocchinfuso WP, Richardson TI, Zink R, Kumar N, Montrose-Rafizadeh C, Dodge J, Hodder P, Griffin PR
Development of an HTS-compatible assay for discovery of ROR? modulators using AlphaScreen® technology J Biomol Screen. 2011 Feb;16(2):183-91. PMID: 21297105
30 – Doghman M, Madoux F, Hodder P, Lalli E
Identification and characterization of steroidogenic factor-1 inverse agonists Methods Enzymol. 2010;485:3-23. PMID: 21050908
29 – Madoux F, Simanski S, Chase P, Mishra JK, Roush WR, Ayad NG, Hodder PS
An ultra-high throughput cell-based screen for Wee1 degradation inhibitors J Biomol Screen. 2010 Sep;15(8):907-17. Epub 2010 Jul 26. PMID: 20660794
28 – Weide T, Saldanha SA, Minond D, Spicer TP, Fotsing JR, Spaargaren M, Frère JM, Bebrone C, Sharpless KB, Hodder P, Fokin VV
NH-1,2,3-triazole-based inhibitors of the VIM-2 metallo-beta-lactamase: synthesis and structure-activity studies. ACS Med Chem Lett. 2010 Jul 8;1(4):150-154. PMID: 20625539
27 – Brunell D, Weissbach H, Hodder P, Brot N
A high-throughput screening compatible assay for activators and inhibitors of methionine sulfoxide reductase A Assay Drug Dev Technol. 2010 Oct;8(5):615-20. Epub 2010 Jun 1. PMID: 20515413
26 – Bachovchin DA, Wolfe MR, Masuda K, Brown SJ, Spicer TP, Fernandez-Vega V, Chase P, Hodder PS, Rosen H, Cravatt BF
Oxime esters as selective, covalent inhibitors of the serine hydrolase retinoblastoma-binding protein 9 (RBBP9) Bioorg Med Chem Lett. 2010 Apr 1;20(7):2254-8. Epub 2010 Feb 6. PMID: 20207142
25 – Grimm C, Jörs S, Saldanha SA, Obukhov AG, Pan B, Oshima K, Cuajungco MP, Chase P, Hodder P, Heller S
Small molecule activators of TRPML3 Chem Biol. 2010 Feb 26;17(2):135-48. PMID: 20189104
24 – Tanaka K, Koresawa M, Iida M, Fukasawa K, Stec EM, Cassaday J, Chase P, Rickert K, Hodder P, Takagi T, Komatani H
Multiplexed random peptide library and phospho-specific antibodies facilitate human polo-like kinase 1 inhibitor screen Assay Drug Dev Technol. 2010 Feb;8(1):47-62. PMID: 20085455
23 – Kota S, Scampavia L, Spicer T, Beeler AB, Takahashi V, Snyder JK, Porco JA, Hodder P, Strosberg AD
A time-resolved fluorescence-resonance energy transfer assay for identifying inhibitors of hepatitis C virus core dimerization Assay Drug Dev Technol. 2010 Feb;8(1):96-105. PMID: 20035614
22 – Brothers SP, Saldanha SA, Spicer TP, Cameron M, Mercer BA, Chase P, McDonald P, Wahlestedt C, Hodder PS
Selective and brain penetrant neuropeptide Y Y2 receptor antagonists discovered by whole-cell high-throughput screening Mol Pharmacol. 2010 Jan;77(1):46-57. Epub 2009 Oct 16. PMID: 19837904
21 – Minond D, Saldanha SA, Subramaniam P, Spaargaren M, Spicer T, Fotsing JR, Weide T, Fokin VV, Sharpless KB, Galleni M, Bebrone C, Lassaux P, Hodder P
Inhibitors of VIM-2 by screening pharmacologically active and click-chemistry compound libraries Bioorg Med Chem. 2009 Jul 15;17(14):5027-37. Epub 2009 Jun 22. PMID: 19553129
20 – Doghman M, Cazareth J, Douguet D, Madoux F, Hodder P, Lalli E
Inhibition of adrenocortical carcinoma cell proliferation by steroidogenic factor-1 inverse agonists J Clin Endocrinol Metab. 2009 Jun;94(6):2178-83. Epub 2009 Mar 24. PMID: 19318454
19 – Schürer SC, Brown SJ, Gonzalez-Cabrera PJ, Schaeffer MT, Chapman J, Jo E, Chase P, Spicer T, Hodder P, Rosen H
Ligand-binding pocket shape differences between sphingosine 1-phosphate (S1P) receptors S1P1 and S1P3 determine efficiency of chemical probe identification by ultrahigh-throughput screening ACS Chem Biol. 2008 Aug 15;3(8):486-98. Epub 2008 Jul 1. PMID: 18590333
18 – Chung CC, Ohwaki K, Schneeweis JE, Stec E, Varnerin JP, Goudreau PN, Chang A, Cassaday J, Yang L, Yamakawa T, Kornienko O, Hodder P, Inglese J, Ferrer M, Strulovici B, Kusunoki J, Tota MR, Takagi T
A fluorescence-based thiol quantification assay for ultra-high-throughput screening for inhibitors of coenzyme A production Assay Drug Dev Technol. 2008 Jun;6(3):361-74. PMID: 18452391
17 – Roth J, Madoux F, Hodder P, Roush WR
Synthesis of small molecule inhibitors of the orphan nuclear receptor steroidogenic factor-1 (NR5A1) based on isoquinolinone scaffolds Bioorg Med Chem Lett. 2008 Apr 15;18(8):2628-32. Epub 2008 Mar 14. PMID: 18374567
16 – Lauer-Fields JL, Minond D, Chase PS, Baillargeon PE, Saldanha SA, Stawikowska R, Hodder P, Fields GB
High throughput screening of potentially selective MMP-13 exosite inhibitors utilizing a triple-helical FRET substrate Bioorg Med Chem. 2009 Feb 1;17(3):990-1005. Epub 2008 Mar 6. PMID: 18358729
15 – Madoux F, Li X, Chase P, Zastrow G, Cameron MD, Conkright JJ, Griffin PR, Thacher S, Hodder P
Potent, selective and cell penetrant inhibitors of SF-1 by functional ultra-high-throughput screening Mol Pharmacol. 2008 Jun;73(6):1776-84. Epub 2008 Mar 11. PMID: 18334597
14 – Schröter T, Minond D, Weiser A, Dao C, Habel J, Spicer T, Chase P, Baillargeon P, Scampavia L, Schürer S, Chung C, Mader C, Southern M, Tsinoremas N, LoGrasso P, Hodder P
Comparison of miniaturized time-resolved fluorescence resonance energy transfer and enzyme-coupled luciferase high-throughput screening assays to discover inhibitors of rho-kinase II (ROCK-II) J Biomol Screen. 2008 Jan;13(1):17-28. PMID: 18227223
13 – Lauer-Fields JL, Spicer TP, Chase PS, Cudic M, Burstein GD, Nagase H, Hodder P, Fields GB
Screening of potential a disintegrin and metalloproteinase with thrombospondin motifs-4 inhibitors using a collagen model fluorescence resonance energy transfer substrate Anal Biochem. 2008 Feb 1;373(1):43-51. Epub 2007 Sep 15. PMID: 17949675
12 – Marine S, Stec E, Chase P, Hoffman I, Szymanski S, Simon A, Shi X, Bartz S, Bagchi A, Minch E, Majercak J, Koblan K, Hazuda D, Shearman M, Gates A, Xu M, Rosahl T, Beher D, Ray W, Stone D, Espeseth A, Ferrer M, Strulovici B
Activity profile-based siRNA screen to explore the functional genomics of Alzheimer’s disease BioTechniques. 2007 Dec;43(6):Sxxii-Sxxvii. ARTICLE.
11 – Hodder PS
Building a uHTS laboratory Drug Discovery World. 2005 Winter;6:31-42. ARTICLE.
10 – Hodder PS
Integration of miniaturisation technologies into the high throughput screening laboratory
European Pharmaceutical Review. 2005 May 20;2:47-55
9 – Zuck P, O’Donnell GT, Cassaday J, Chase P, Hodder P, Strulovici B, Ferrer M
Miniaturization of absorbance assays using the fluorescent properties of white microplates Anal Biochem. 2005 Jul 15;342(2):254-9. PMID: 15949786
8 – Hale JJ, Lynch CL, Neway W, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Parent SA, Chrebet G, Bergstrom J, Card D, Ferrer M, Hodder P, Strulovici B, Rosen H, Mandala S
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists J Med Chem. 2004 Dec 30;47(27):6662-5. PMID: 15615513
7 – Hodder P, Mull R, Cassaday J, Berry K, Strulovici B
Miniaturization of intracellular calcium functional assays to 1536-well plate format using a fluorometric imaging plate reader J Biomol Screen. 2004 Aug;9(5):417-26. PMID: 15296641
6 – Kunapuli P, Ransom R, Murphy KL, Pettibone D, Kerby J, Grimwood S, Zuck P, Hodder P, Lacson R, Hoffman I, Inglese J, Strulovici B
Development of an intact cell reporter gene beta-lactamase assay for G protein-coupled receptors for high-throughput screening Anal Biochem. 2003 Mar 1;314(1):16-29. PMID: 12633598
5 – Hodder P, Cassaday J, Peltier R, Berry K, Inglese J, Feuston B, Culberson C, Bleicher L, Cosford ND, Bayly C, Suto C, Varney M, Strulovici B
Identification of metabotropic glutamate receptor antagonists using an automated high throughput screening system Anal Biochem. 2003 Feb 15;313(2):246-54. PMID: 12605861
4 – Hodder PS, Beeson C, Ruzicka J
Equilibrium and kinetic measurement of muscarinic receptor antagonism on living cells using bead injection spectroscopy Anal Chem. 2000 Jul 15;72(14):3109-15. PMID: 10939374
3 – Scampavia LD, Hodder PS, Lähdesmäki I, Ruzicka J
Automation of functional assays by flow injection fluorescence microscopy Trends Biotechnol. 1999 Nov;17(11):443-7. PMID: 10511702
2 – Hodder PS, Ruzicka J
A flow injection renewable surface technique for cell-based drug discovery functional assays Anal Chem. 1999 Mar 15;71(6):1160-6. PMID: 10093496
1 – Hodder PS, Blankenstein G, Ruzicka J
Microfabricated flow chamber for fluorescence-based chemistries and stopped-flow injection cytometry Analyst. 1997 Sep;122(9):883-7. PMID: 9374023