Publications


Lead Identification Papers

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 113 papers that have been either published or accepted.



113 - 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 Assay
arrowSLAS Discovery.  2018 August.

 

112 - Janovick JA, Spicer TP, Bannister TD, Smith E, Ganapathy V, Scampavia L
Chemical Validation and Optimization of Pharmacoperones Targeting Vasopressin Type 2 Receptor Mutant
arrowBiochem J.  2018 August.

 

111 - 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 GPR119
arrowAssay Drug Dev Technol.  2018 July.

 

110 - 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 Cells
arrowSLAS Discovery.  2018 May.

 

109 - 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 phenotype
arrowOncogene.  2018 May.

 

108 - 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 Complex
arrowAssay Drug Dev Technol.  2018 Apr.

 

107 - 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 Screening
arrowSLAS Discovery.  2018 Apr.

 

106 - Shumate J, Baillargeon P, Spicer T, Scampavia L
IoT for Real-Time Measurement of High-Throughput Liquid Dispensing in Laboratory Environments
arrowSLAS Technology.  2018 Apr.

 

105 - 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.
arrowOncotarget.  2018 Feb.

 

104 - 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.
arrowAssay Drug Dev Technol.  2017 Nov.

 

103 - 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.
arrowMolecular Neuropsychiatry.  2017 Nov.

 

102 - Singhera F, Cooper E, Scampavia L, Spicer T
Using bead injection to model dispensing of 3-D multicellular spheroids into microtiter plates.
arrowTalanta.  2017 Sep.

 

101 - 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.
arrowSLAS Discovery.  2017 Oct.

 

100 - 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.
arrowSLAS Discovery.  2017 Aug.

 

99 - Janovick JA, Spicer TP, Scampavia L, Conn PM
Pharmacoperone rescue of vasopressin 2 receptor mutants reveals unexpected constitutive activity and coupling bias.
arrowPLoS One.  2017 Aug.

 

98 - Powell K
Adding depth to cell culture.
arrowScience.  2017 Apr.

 

97 - 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.
arrowSLAS Discovery.  2017 Jan.

 

96 - 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.
arrowSLAS Discovery.  2017 Jan.

 

95 - 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.
 arrowSci Rep.  2016 Dec.

 

94 - 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.
 arrowJournal of Biomolecular Screening.  2016 Nov.

 

93 - 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).
arrowJ Biomol Screen.  2016 Sept.

 

92 - 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.
 arrowElife.  2016 Jul 20.

 

91 - Janovick JA, Spicer TP, Smith E, Bannister TD, Kenakin T, Scampavia L, Conn PM.
Receptor antagonism/agonism can be uncoupled from pharmacoperone activity.
 arrowMol Cell Endocrinol.  2016 Jul 4.

 

90 - 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.
 arrowJournal of Biomolecular Screening.  2016 Jun 8.

 

89 - 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.
 arrowJournal of Biomolecular Screening.  2016 May 4.

 

88 - 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, Valentine ST
Ebselen, a Small-Molecule Capsid Inhibitor of HIV-1 Replication
arrowAntimicrobial Agents and Chemotherapy.  2016 Mar. 25

 

87 - 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.
 arrowJournal of Biomolecular Screening.  2016 Feb 2.

 

86 - 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.
 arrowAssay and Drug Development Technologies.  2015 Dec 15.

 

85 - 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.
 arrowACS Chem Biol.  2015 Nov 2.

 

84 - 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.
 arrowCell Metab.  2015 Sep 22.

 

83 - 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.
 arrowACS Chem Biol.  2015 Sep 23.

 

82 - Conn PM, Spicer TP, Scampavia L, Janovick JA.
Assay strategies for identification of therapeutic leads that target protein trafficking.
 arrowTrends Pharmacol Sci.  2015 Jun 8.

 

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).
 arrowJ Biomol Screen.  2015 Apr 16.

 

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.
 arrowACS Chem Biol.  2015 Jan 20.

 

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 Screening
arrowAssay Drug Dev Technol.  2015 January/February;13(1):16-24.

 

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 Deacetylases
arrowChem Biol.  2015 Feb 19;22(2):273-84. doi: 10.1016/j.chembiol.2014.12.015.

 

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 CYP3A4
arrowProbe Reports from the NIH Molecular Libraries Program.  

 

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 tuberculosis
arrowACS Chem Biol.  2014 Dec 5. [Epub ahead of print]. 

 

75 - Kadakkuzha BM, Spicer TP, Chase P, Richman JB, Hodder P, Puthanveettil SV.
High-throughput screening for small molecule modulators of motor protein Kinesin.
 arrowAssay Drug Dev Technol.  2014 Oct.

 

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
arrow J Medicinal Chemistry.  2014 Oct 20. [Epub ahead of print]. 

 

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
arrow J Biomol Screen.  2014 Aug 27. pii: 1087057114548832. [Epub ahead of print]. 

 

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)
arrow J Med Chem.  2014 Aug 22. [Epub ahead of print]. 

 

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 β
arrow Biopolymers.  2014 Jul 21. doi: 10.1002/bip.22527. [Epub ahead of print]. 

 

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
arrow Assay Drug Dev Technol.  2014 May;12(4):238-46. doi: 10.1089/adt.2014.576. 

 

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 Technology
arrow Assay Drug Dev Technol.  2014 May;12(4):229-37. doi: 10.1089/adt.2013.558. 

 

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 Degradation
arrow J Biol Chem.  2014 Jul 4;289(27):18893-18903. Epub 2014 May 9. 

 

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
arrow PLoS One.  2014 Apr 17;9(4):e95243. doi: 10.1371/journal.pone.0095243. eCollection 2014. 

 

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
arrow ChemMedChem.  2014 Aug;9(8):1677-82. doi: 10.1002/cmdc.201402051. Epub 2014 Apr 1. 

 

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
arrow J Biomol Screen.  2014 Mar 11. [Epub ahead of print]. 

 

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
arrow ACS Chem Biol.  2014 Apr 18;9(4):913-21. doi: 10.1021/cb400841k. Epub 2014 Jan 27. 

 

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
arrow Cancer Res.  2014 Mar 1;74(5):1506-17. doi: 10.1158/0008-5472.CAN-13-2939. Epub 2014 Jan 3. 

 

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
arrow Pharmacol Res.  2014 May;83:38-51. doi: 10.1016/j.phrs.2013.12.004. Epub 2013 Dec 25. 

 

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
arrow ACS Chem Biol.  2014 Feb 21;9(2):433-42. doi: 10.1021/cb4006886. Epub 2013 Nov 25. 

 

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
arrow J Biol Chem.  2013 Dec 20;288(51):36703-16. doi: 10.1074/jbc.M113.504381. Epub 2013 Nov 1. 

 

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)
arrow J Med Chem.  2013 Nov 27;56(22):9351-5. doi: 10.1021/jm4013246. Epub 2013 Nov 13. 

 

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
arrow Bioorg Med Chem Lett.  2013 Dec 1;23(23):6346-9. doi: 10.1016/j.bmcl.2013.09.075. Epub 2013 Oct 1. 

 

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
arrow Bioorg Med Chem Lett.  2013 Nov 15;23(22):6172-7. doi: 10.1016/j.bmcl.2013.08.112. Epub 2013 Sep 7. 

 

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
arrow Bioorg Med Chem.  2013 Nov 1;21(21):6642-6649. doi: 10.1016/j.bmc.2013.08.017. Epub 2013 Aug 15. 

 

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
arrow Bioorg Med Chem.  2013 Sep 1;21(17):5373-82. doi: 10.1016/j.bmc.2013.06.012. Epub 2013 Jun 15. 

 

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
arrow Proc Natl Acad Sci U S A.  2013 Jul 16;110(29):12072-7. doi: 10.1073/pnas.1222044110. Epub 2013 Jul 1. 

 

53 - Conn PM, Smith E, Hodder P, Janovick JA, Smithson DC
High-throughput screen for pharmacoperones of the vasopressin type 2 receptor
arrow J Biomol Screen.  2013 Sep;18(8):930-7. doi: 10.1177/1087057113483559. Epub 2013 May 2. 

 

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
arrow Mol Cancer Ther.  2013 May;12(5):610-20. doi: 10.1158/1535-7163.MCT-12-0930. Epub 2013 Apr 26. 

 

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
arrow Bioorg Med Chem.  2013 Jun 1;21(11):3138-46. doi: 10.1016/j.bmc.2013.03.031. Epub 2013 Mar 29. 

 

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
arrow Proc Natl Acad Sci U S A.  2013 Apr 23;110(17):7044-9. doi 10.1073/pnas.1303510110.  Epub 2013 Apr 1. 

 

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
arrow Bioorg Med Chem Lett.  2013 May 15;23(10):2996-3000. doi: 10.1016/j.bmcl.2013.03.032.  Epub 2013 Mar 16. 

 

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)
arrow Bioorg Med Chem Lett.  2013 Feb 1;23(3):839-43. doi: 10.1016/j.bmcl.2012.11.061.  Epub 2012 Dec 2. 

 

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
arrow J Med Chem.  2013 Jan 24;56(2):534-46. doi: 10.1021/jm301580n.  Epub 2013 Jan 3. 

 

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
arrow J Ocul Pharmacol Ther.  2013 Apr;29(3):298-309. doi: 10.1089/jop.2012.0.0135.  Epub 2012 Oct 25. 

 

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)
arrow Bioorg Med Chem Lett.  2012 Dec 1;22(23):7135-41. doi: 10.1016/j.bmcl.2012.09.074. Epub 2012 Oct 2. 

 

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
arrow J Am Chem Soc.  2012 Jun 27;134(25):10345-8.  Epub  2012 Jun 12. 

 

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
arrow ACS Chem Biol.  2012 May 18;7(5):879-91.  Epub 2012 Mar 23. 

 

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
arrow Nat Chem Biol.  2011 Dec 25;8(2):185-96. doi: 10.1038/nchembio.763. 

 

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
arrow Bioorg Med Chem Lett.  2012 Jan 1;22(1):537-42.  Epub 2011 Nov 4. 

 

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
arrow Bioorg Med Chem Lett.  2011 Dec 1;21(23):7180-4.  Epub 2011 Sep 22. 

 

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
arrow Bioorg Med Chem Lett.  2011 Nov 15;21(22):6739-45.  Epub 2011 Sep 20. 

 

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
arrow Mol Biochem Parasitol.  2011 Dec;180(2):127-31.  Epub 2011 Sep 16. 

 

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
arrow J Am Chem Soc.  2011 Oct 19;133(41):16605-16.  Epub 2011 Sep 27. 

 

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
arrow Mol Cancer Ther.  2011 Nov;10(11):2043-51.  Epub 2011 Sep 1. 

 

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
arrow J Am Chem Soc.  2011 Aug 3;133(30):11665-74.  Epub 2011 Jun 21. 

 

34 - Baillargeon P, Scampavia L, Einsteder R, Hodder P
Monitoring of HTS compound library quality via a high-resolution image acquisition and processing instrument
arrow J Lab Autom.  2011 Jun;16(3):197-203. Epub 2011 May 16.  

 

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
arrow Proc Natl Acad Sci U S A.  2011 Apr 26;108(17):6811-6. Epub 2011 Mar 11.  

 

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
arrow Proc Natl Acad Sci U S A.  2011 Mar 22;108(12):4834-9. Epub 2011 Mar 7.  

 

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
arrow J Biomol Screen.  2011 Feb;16(2):183-91. 

 

30 - Doghman M, Madoux F, Hodder P, Lalli E
Identification and characterization of steroidogenic factor-1 inverse agonists
arrow Methods Enzymol.  2010;485:3-23. 

 

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
arrow J Biomol Screen.  2010 Sep;15(8):907-17. Epub 2010 Jul 26. 

 

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.
arrow ACS Med Chem Lett.  2010 Jul 8;1(4):150-154. 

 

27 - Brunell D, Weissbach H, Hodder P, Brot N
A high-throughput screening compatible assay for activators and inhibitors of methionine sulfoxide reductase A
arrow Assay Drug Dev Technol.  2010 Oct;8(5):615-20.  Epub 2010 Jun 1. 

 

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)
arrow Bioorg Med Chem Lett.  2010 Apr 1;20(7):2254-8.  Epub 2010 Feb 6. 

 

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
arrow Chem Biol.  2010 Feb 26;17(2):135-48. 

 

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
arrow Assay Drug Dev Technol.  2010 Feb;8(1):47-62. 

 

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
arrow Assay Drug Dev Technol.  2010 Feb;8(1):96-105. 

 

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
arrow Mol Pharmacol.  2010 Jan;77(1):46-57.  Epub 2009 Oct 16. 

 

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
arrow Bioorg Med Chem.  2009 Jul 15;17(14):5027-37.  Epub 2009 Jun 22. 

 

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
arrow J Clin Endocrinol Metab.  2009 Jun;94(6):2178-83.  Epub 2009 Mar 24. 

 

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
arrow ACS Chem Biol.  2008 Aug 15;3(8):486-98.  Epub 2008 Jul 1. 

 

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
arrow Assay Drug Dev Technol.  2008 Jun;6(3):361-74. 

 

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
arrow Bioorg Med Chem Lett.  2008 Apr 15;18(8):2628-32.  Epub 2008 Mar 14. 

 

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
arrow Bioorg Med Chem.  2009 Feb 1;17(3):990-1005.  Epub 2008 Mar 6. 

 

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
arrow Mol Pharmacol.  2008 Jun;73(6):1776-84.  Epub 2008 Mar 11. 

 

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)
arrow J Biomol Screen.  2008 Jan;13(1):17-28. 

 

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
arrow Anal Biochem.  2008 Feb 1;373(1):43-51.  Epub 2007 Sep 15. 

 

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
arrow BioTechniques.  2007 Dec;43(6):Sxxii-Sxxvii. ARTICLE.

 

11 - Hodder PS
Building a uHTS laboratory
arrow 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
arrow Anal Biochem.  2005 Jul 15;342(2):254-9. 

 

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
arrow J Med Chem.  2004 Dec 30;47(27):6662-5. 

 

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
arrow J Biomol Screen.  2004 Aug;9(5):417-26. 

 

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
arrow Anal Biochem.  2003 Mar 1;314(1):16-29. 

 

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
arrow Anal Biochem.  2003 Feb 15;313(2):246-54. 

 

4 - Hodder PS, Beeson C, Ruzicka J
Equilibrium and kinetic measurement of muscarinic receptor antagonism on living cells using bead injection spectroscopy
arrow Anal Chem.  2000 Jul 15;72(14):3109-15. 

 

3 - Scampavia LD, Hodder PS, Lähdesmäki I, Ruzicka J
Automation of functional assays by flow injection fluorescence microscopy
arrow Trends Biotechnol.  1999 Nov;17(11):443-7. 

 

2 - Hodder PS, Ruzicka J
A flow injection renewable surface technique for cell-based drug discovery functional assays
arrow Anal Chem.  1999 Mar 15;71(6):1160-6. 

 

1 - Hodder PS, Blankenstein G, Ruzicka J
Microfabricated flow chamber for fluorescence-based chemistries and stopped-flow injection cytometry
arrow Analyst.  1997 Sep;122(9):883-7. 

 



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