Timothy P Spicer

Timothy P Spicer, Ph.D.

Senior Scientific Director, Department Of Molecular Medicine

Department: SR-MM-SPICER LAB
Business Phone: (561) 228-2150
Business Email: spicert@ufl.edu

About Timothy P Spicer

Additional Positions:
Assistant Professor of Molecular Therapeutics, Molecular Therapeutics
2015 – 2017 · Scripps Research
Senior Staff Scientist, Lead Identification
2005 – 2013 · Translational Research Institute, Scripps Research
Research Scientist II, Lead Discovery and Profiling
2003 – 2005 · Bristol-Myers Squibb Pharmaceutical Research Institute, Bristol-Myers Squibb
Research Scientist I, Discovery Technologies
2000 – 2003 · Bristol-Myers Squibb Pharmaceutical Research Institute, Bristol-Myers Squibb
Associate Research Scientist II, Department of Virology HIV-1 Novel Targets
1996 – 2000 · Bristol-Myers Squibb Pharmaceutical Research Institute, Bristol-Myers Squibb
Research Technician II, Department of Medicine
1990 – 1996 · State University of New York Health Science Center
Related Links:

Accomplishments

Associate Editor SLAS Discovery
2020-Current · SLAS
SLAS Board of Directors
2020-2022 · Society of Lab Automation and Screening (SLAS)
Co-Chair
2019-2020 · SLAS Americas Scientific Program Committee
Member
2019-2020 · SLAS Knowledge Council and Dissemination Committee
Conference Co-Chair
2018 · SLAS
Member, Graduate Education Fellowship Grant Review Panel
2018 · SLAS Graduate Education Fellowship Grant Review Panel-2018,2019 AACR, 2018-2020
Inducted
2017 · SLAS Fellow
Inducted
2017 · SLAS Fellows
SBIR Study Section Reviewer
2017 · National Institutes of Health
Track Chair, Automation and HTS Technologies
2016 · SLAS
Associate Track Chair, Automation and HTS Technologies
2015 · SLAS
Applied Biotechnology Collaboration Award
2005 · Bristol-Myers Squibb
Triumph Award
2003 · Bristol-Myers Squibb
Applied Biotechnology Collaboration Award
2002 · Bristol-Myers Squibb
Star Award, First quarter
2002 · Bristol-Myers Squibb
Star Award, Fourth quarter
2002 · Bristol-Myers Squibb
President’s Award
2000 · Bristol-Myers Squibb
Excellence Award
1997-2005 · Bristol-Myers Squibb

Teaching Profile

Teaching Philosophy
Scripps Research- Graduate School Co-director TRBIO 450 Drug Discovery and Development (2019-2022) Lecturer in Drug Discovery (2018)

Research Profile

The focus of our research involves enabling technologies for High Throughput Screening (HTS) of any target of unmet therapeutic need. Our facility supports scientist and faculty locally as well as those in the US and throughout the world. We do this by implementing their biological applications into high density plates for HTS. The breadth of biology we deal with is virtually unlimited due to the diversity of skill sets of the scientist and engineers within our group as well as the expanded capability of the readers associated to our system. We operate a fully automated 1536 well compatible platform and perform HTS on large compound libraries such as the Scripps Drug Discovery Library (645K) or small focused collections (FDA approved drugs). We have expertise in microfluidics, low nanoliter volume liquid handling, ultra-sensitive plate reader technologies and informatics set-up to handle large volume data sets. Key components are high-content readers, imaging detectors such as the ViewLux and FLIPR Tetra, as well as pintool and acoustic transfer devices. Through collaborative efforts we have successfully translated multiple small molecules into the clinics. We are open to any pharmacology desired (agonist, PAMs, NAMs, inverse agonist, etc.) vs. kinases, GPCR, NHRs, proteases, phenotypic assays, etc. which can be applied to any therapeutic area; i.e. CNS, infectious diseases, cardiovascular, oncology, metabolic diseases. In addition, we are currently funded (R33CA206949) to develop 3D spheroid based uHTS assays for the purpose of testing molecules in a more phenotypically relevant format to cancer biology.

Open Researcher and Contributor ID (ORCID)

0000-0002-9080-4226

Publications

2024
Protocol for high throughput 3D drug screening of patient derived melanoma and renal cell carcinoma
SLAS Discovery. [DOI] 10.1016/j.slasd.2024.01.002.
2024
Protocol for kinetic mode potassium channel assays on common plate readers and microscopes
SLAS Discovery. 29(3) [DOI] 10.1016/j.slasd.2024.100148.
2024
Rebamipide and Derivatives are Potent, Selective Inhibitors of Histidine Phosphatase Activity of the Suppressor of T Cell Receptor Signaling Proteins.
Journal of medicinal chemistry. 67(3):1949-1960 [DOI] 10.1021/acs.jmedchem.3c01763. [PMID] 38252624.
2023
A new vulnerability to BET inhibition due to enhanced autophagy in BRCA2 deficient pancreatic cancer.
Cell death & disease. 14(9) [DOI] 10.1038/s41419-023-06145-9. [PMID] 37735513.
2023
A new vulnerability to BET inhibition due to enhanced autophagy in BRCA2 deficient pancreatic cancer.
bioRxiv : the preprint server for biology. [DOI] 10.1101/2023.05.30.542934. [PMID] 37398312.
2023
Elemene sensitizes pancreatic cancer cells to bortezomib by enhancing proteasome inhibition via molecular patch mechanism.
Signal transduction and targeted therapy. 8(1) [DOI] 10.1038/s41392-023-01373-z. [PMID] 36849489.
2023
High throughput assay for compounds that boost BDNF expression in neurons
SLAS Discovery. 28(3):88-94 [DOI] 10.1016/j.slasd.2023.02.005. [PMID] 36842668.
2023
High throughput screening for drugs that inhibit 3C-like protease in SARS-CoV-2
SLAS Discovery. 28(3):95-101 [DOI] 10.1016/j.slasd.2023.01.001. [PMID] 36646172.
2023
Protocol for 3D screening of lung cancer spheroids using natural products
SLAS Discovery. 28(2):20-28 [DOI] 10.1016/j.slasd.2023.01.005. [PMID] 36681384.
2022
Gain-of-Signal Assays for Probing Inhibition of SARS-CoV-2 Mpro/3CLpro in Living Cells.
mBio. 13(3) [DOI] 10.1128/mbio.00784-22. [PMID] 35471084.
2022
High Throughput Screening for Compounds to the Orphan Nuclear Receptor NR2F6.
SLAS discovery : advancing life sciences R & D. [DOI] 10.1016/j.slasd.2022.03.005. [PMID] 35331960.
2022
Identification of potent small molecule inhibitors of SARS-CoV-2 entry.
SLAS discovery : advancing life sciences R & D. 27(1):8-19 [DOI] 10.1016/j.slasd.2021.10.012. [PMID] 35058179.
2022
Lead Identification using 3D Models of Pancreatic Cancer
SLAS discovery : advancing life sciences R & D. [DOI] 10.1016/j.slasd.2022.03.002. [PMID] 35306207.
2022
LPCAT3 Inhibitors Remodel the Polyunsaturated Phospholipid Content of Human Cells and Protect from Ferroptosis
ACS Chemical Biology. 17(6):1607-1618 [DOI] 10.1021/acschembio.2c00317.
2022
Rapid deployment of inexpensive open-source orbital shakers in support of high-throughput screening.
SLAS technology. 27(3):180-186 [DOI] 10.1016/j.slast.2022.01.003. [PMID] 35066236.
2022
Screening for modulators of autism spectrum disorder using induced human neurons.
SLAS discovery : advancing life sciences R & D. 27(2):128-139 [DOI] 10.1016/j.slasd.2022.01.004. [PMID] 35123134.
2022
SLAS special issue editorial 2022: 3D cell culture approaches of microphysiologically relevant models.
SLAS discovery : advancing life sciences R & D. 27(3):149-150 [DOI] 10.1016/j.slasd.2022.03.006. [PMID] 35339725.
2021
Development and Pilot Screen of Novel High Content Assay for Down Regulators of Expression of Heterogenous Nuclear Ribonuclear Protein H2.
Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology. 55(3):265-276 [DOI] 10.33594/000000372. [PMID] 34014051.
2021
Discovery and Optimization of Selective Inhibitors of Meprin α (Part I).
Pharmaceuticals (Basel, Switzerland). 14(3) [DOI] 10.3390/ph14030203. [PMID] 33671080.
2021
Discovery and Optimization of Selective Inhibitors of Meprin α (Part II).
Pharmaceuticals (Basel, Switzerland). 14(3) [DOI] 10.3390/ph14030197. [PMID] 33673639.
2021
Identification of Compounds That Promote Readthrough of Premature Termination Codons in the CFTR
SLAS Discovery. 26(2):205-215 [DOI] 10.1177/2472555220962001. [PMID] 33016182.
2021
Identification of novel modulators of a schistosome transient receptor potential channel targeted by praziquantel
PLOS Neglected Tropical Diseases. 15(11) [DOI] 10.1371/journal.pntd.0009898. [PMID] 34731172.
2021
Identification of Potential Modulators of the RGS7/Gβ5/R7BP Complex
SLAS Discovery. 26(9):1177-1188 [DOI] 10.1177/24725552211020679. [PMID] 34112017.
2021
Identification of Small-Molecule Inhibitors of Neutral Ceramidase (nCDase) via Target-Based High-Throughput Screening
SLAS Discovery. 26(1):113-121 [DOI] 10.1177/2472555220945283. [PMID] 32734807.
2021
Synthetic fluorescent MYC probe: Inhibitor binding site elucidation and development of a high-throughput screening assay.
Bioorganic & medicinal chemistry. 42 [DOI] 10.1016/j.bmc.2021.116246. [PMID] 34130216.
2020
An unbiased high-throughput drug screen reveals a potential therapeutic vulnerability in the most lethal molecular subtype of pancreatic cancer.
Molecular oncology. 14(8):1800-1816 [DOI] 10.1002/1878-0261.12743. [PMID] 32533886.
2020
Drug Discovery Targeting COVID-19.
SLAS discovery : advancing life sciences R & D. 25(10):1095-1096 [DOI] 10.1177/2472555220970966. [PMID] 33215959.
2020
High-Throughput Screening for Drugs That Inhibit Papain-Like Protease in SARS-CoV-2
SLAS Discovery. 25(10):1152-1161 [DOI] 10.1177/2472555220963667. [PMID] 33043784.
2020
Pharmacologic IRE1/XBP1s activation confers targeted ER proteostasis reprogramming.
Nature chemical biology. 16(10):1052-1061 [DOI] 10.1038/s41589-020-0584-z. [PMID] 32690944.
2020
Rescue of mutant gonadotropin-releasing hormone receptor function independent of cognate receptor activity.
Scientific reports. 10(1) [DOI] 10.1038/s41598-020-67473-w. [PMID] 32601341.
2020
Small-molecule inhibitor targeting orphan nuclear receptor COUP-TFII for prostate cancer treatment
Science Advances. 6(18) [DOI] 10.1126/sciadv.aaz8031. [PMID] 32494682.
2020
SYNGAP1 Controls the Maturation of Dendrites, Synaptic Function, and Network Activity in Developing Human Neurons.
The Journal of neuroscience : the official journal of the Society for Neuroscience. 40(41):7980-7994 [DOI] 10.1523/JNEUROSCI.1367-20.2020. [PMID] 32887745.
2019
A Simple Procedure for Creating Scalable Phenotypic Screening Assays in Human Neurons.
Scientific reports. 9(1) [DOI] 10.1038/s41598-019-45265-1. [PMID] 31227747.
2019
A survey of core replacements in indole-based HIV-1 attachment inhibitors.
Bioorganic & medicinal chemistry letters. 29(11):1423-1429 [DOI] 10.1016/j.bmcl.2019.03.018. [PMID] 30940396.
2019
Applications for Open Source Microplate-Compatible Illumination Panels.
Journal of visualized experiments : JoVE. (152) [DOI] 10.3791/60088. [PMID] 31633701.
2019
Automating a Magnetic 3D Spheroid Model Technology for High-Throughput Screening.
SLAS technology. 24(4):420-428 [DOI] 10.1177/2472630319854337. [PMID] 31225974.
2019
Design of Microplate-Compatible Illumination Panels for a Semiautomated Benchtop Pipetting System.
SLAS technology. 24(4):399-407 [DOI] 10.1177/2472630318822476. [PMID] 30698997.
2019
Discovery and Characterization of Two Classes of Selective Inhibitors of the Suppressor of the TCR Signaling Family of Proteins.
ACS infectious diseases. 5(2):250-259 [DOI] 10.1021/acsinfecdis.8b00238. [PMID] 30485744.
2019
Identification of Antimalarial Inhibitors Using Late-Stage Gametocytes in a Phenotypic Live/Dead Assay.
SLAS discovery : advancing life sciences R & D. 24(1):38-46 [DOI] 10.1177/2472555218796410. [PMID] 30142014.
2019
Stabilization of amyloidogenic immunoglobulin light chains by small molecules.
Proceedings of the National Academy of Sciences of the United States of America. 116(17):8360-8369 [DOI] 10.1073/pnas.1817567116. [PMID] 30971495.
2019
The Scripps Molecular Screening Center and Translational Research Institute
SLAS Discovery. 24(3):386-397 [DOI] 10.1177/2472555218820809. [PMID] 30682260.
2018
A Cytotoxic Three-Dimensional-Spheroid, High-Throughput Assay Using Patient-Derived Glioma Stem Cells.
SLAS discovery : advancing life sciences R & D. 23(8):842-849 [DOI] 10.1177/2472555218775055. [PMID] 29750582.
2018
A High-Throughput Time-Resolved Fluorescence Energy Transfer Assay to Screen for Modulators of RGS7/Gβ5/R7BP Complex.
Assay and drug development technologies. 16(3):150-161 [DOI] 10.1089/adt.2017.839. [PMID] 29658790.
2018
A Novel 3D Culture System for High-Throughput Hepatoxicity Screening.
BioProcess international. 16(FR 8):1-5 [PMID] 35431667.
2018
A novel three-dimensional high-throughput screening approach identifies inducers of a mutant KRAS selective lethal phenotype.
Oncogene. 37(32):4372-4384 [DOI] 10.1038/s41388-018-0257-5. [PMID] 29743592.
2018
A Rapid Phenotypic Whole-Cell Screening Approach for the Identification of Small-Molecule Inhibitors That Counter β-Lactamase Resistance in Pseudomonas aeruginosa.
SLAS discovery : advancing life sciences R & D. 23(1):55-64 [DOI] 10.1177/2472555217728489. [PMID] 28850797.
2018
Advanced Development of Primary Pancreatic Organoid Tumor Models for High-Throughput Phenotypic Drug Screening.
SLAS discovery : advancing life sciences R & D. 23(6):574-584 [DOI] 10.1177/2472555218766842. [PMID] 29673279.
2018
Chemical validation and optimization of pharmacoperones targeting vasopressin type 2 receptor mutant
Biochemical Journal. 475(18):2941-2953 [DOI] 10.1042/bcj20180065.
2018
Dynamic changes during the treatment of pancreatic cancer.
Oncotarget. 9(19):14764-14790 [DOI] 10.18632/oncotarget.24483. [PMID] 29599906.
2018
High-Throughput Screening for Protein Synthesis Inhibitors Targeting Aminoacyl-tRNA Synthetases.
SLAS discovery : advancing life sciences R & D. 23(2):174-182 [DOI] 10.1177/2472555217734128. [PMID] 29020503.
2018
Identification of Novel, Structurally Diverse, Small Molecule Modulators of GPR119.
Assay and drug development technologies. 16(5):278-288 [DOI] 10.1089/adt.2018.849. [PMID] 30019946.
2018
Improved Scalability of Neuron-Based Phenotypic Screening Assays for Therapeutic Discovery in Neuropsychiatric Disorders.
Molecular neuropsychiatry. 3(3):141-150 [DOI] 10.1159/000481731. [PMID] 29594133.
2018
IoT for Real-Time Measurement of High-Throughput Liquid Dispensing in Laboratory Environments.
SLAS technology. 23(5):440-447 [DOI] 10.1177/2472630318769454. [PMID] 29649373.
2018
Using bead injection to model dispensing of 3-D multicellular spheroids into microtiter plates.
Talanta. 177:74-76 [DOI] 10.1016/j.talanta.2017.09.022. [PMID] 29108585.
2017
A 1536-Well 3D Viability Assay to Assess the Cytotoxic Effect of Drugs on Spheroids.
SLAS discovery : advancing life sciences R & D. 22(5):516-524 [DOI] 10.1177/2472555216686308. [PMID] 28346088.
2017
A Homogeneous Cell-Based Halide-Sensitive Yellow Fluorescence Protein Assay to Identify Modulators of the Cystic Fibrosis Transmembrane Conductance Regulator Ion Channel.
Assay and drug development technologies. 15(8):395-406 [DOI] 10.1089/adt.2017.810. [PMID] 29172645.
2017
Development of an HTS-Compatible Assay for Discovery of Melanoma-Related Microphthalmia Transcription Factor Disruptors Using AlphaScreen Technology.
SLAS discovery : advancing life sciences R & D. 22(1):58-66 [DOI] 10.1177/1087057116675274. [PMID] 27827304.
2017
Drug Library Screening for the Identification of Ionophores That Correct the Mistrafficking Disorder Associated with Oxalosis Kidney Disease.
SLAS discovery : advancing life sciences R & D. 22(7):887-896 [DOI] 10.1177/2472555217689992. [PMID] 28346094.
2017
Pharmacoperone rescue of vasopressin 2 receptor mutants reveals unexpected constitutive activity and coupling bias.
PloS one. 12(8) [DOI] 10.1371/journal.pone.0181830. [PMID] 28767678.
2016
An Automated Miniaturized Method to Perform and Analyze Antimicrobial Drug Synergy Assays.
Assay and drug development technologies. 14(1):58-66 [DOI] 10.1089/adt.2015.672. [PMID] 26669516.
2016
An Integrated Approach for Screening and Identification of Positive Allosteric Modulators of N-Methyl-D-Aspartate Receptors.
Journal of biomolecular screening. 21(5):468-79 [DOI] 10.1177/1087057116628437. [PMID] 26838761.
2016
Discovery of an enzyme and substrate selective inhibitor of ADAM10 using an exosite-binding glycosylated substrate.
Scientific reports. 6(1) [DOI] 10.1038/s41598-016-0013-4. [PMID] 28442704.
2016
Ebselen, a Small-Molecule Capsid Inhibitor of HIV-1 Replication.
Antimicrobial agents and chemotherapy. 60(4):2195-208 [DOI] 10.1128/AAC.02574-15. [PMID] 26810656.
2016
First-in-Class Inhibitors of Sulfur Metabolism with Bactericidal Activity against Non-Replicating M. tuberculosis.
ACS chemical biology. 11(1):172-84 [DOI] 10.1021/acschembio.5b00517. [PMID] 26524379.
2016
Fluorometric High-Throughput Screening Assay for Secreted Phospholipases A2 Using Phospholipid Vesicles.
Journal of biomolecular screening. 21(7):713-21 [DOI] 10.1177/1087057116646742. [PMID] 27146384.
2016
Identification of Potential Pharmacoperones Capable of Rescuing the Functionality of Misfolded Vasopressin 2 Receptor Involved in Nephrogenic Diabetes Insipidus.
Journal of biomolecular screening. 21(8):824-31 [DOI] 10.1177/1087057116653925. [PMID] 27280550.
2016
Receptor antagonism/agonism can be uncoupled from pharmacoperone activity.
Molecular and cellular endocrinology. 434:176-85 [DOI] 10.1016/j.mce.2016.07.003. [PMID] 27389877.
2016
Small molecule proteostasis regulators that reprogram the ER to reduce extracellular protein aggregation.
eLife. 5 [DOI] 10.7554/eLife.15550. [PMID] 27435961.
2015
Application of Parallel Multiparametric Cell-Based FLIPR Detection Assays for the Identification of Modulators of the Muscarinic Acetylcholine Receptor 4 (M4).
Journal of biomolecular screening. 20(7):858-68 [DOI] 10.1177/1087057115581770. [PMID] 25877150.
2015
Assay strategies for identification of therapeutic leads that target protein trafficking.
Trends in pharmacological sciences. 36(8):498-505 [DOI] 10.1016/j.tips.2015.05.004. [PMID] 26067100.
2015
Development of a phenotypic high-content assay to identify pharmacoperone drugs for the treatment of primary hyperoxaluria type 1 by high-throughput screening.
Assay and drug development technologies. 13(1):16-24 [DOI] 10.1089/adt.2014.627. [PMID] 25710543.
2015
Identification of potent inhibitors of the Trypanosoma brucei methionyl-tRNA synthetase via high-throughput orthogonal screening.
Journal of biomolecular screening. 20(1):122-30 [DOI] 10.1177/1087057114548832. [PMID] 25163684.
2015
Identification of small molecules that disrupt signaling between ABL and its positive regulator RIN1.
PloS one. 10(3) [DOI] 10.1371/journal.pone.0121833. [PMID] 25811598.
2015
Selective inhibitor of platelet-activating factor acetylhydrolases 1b2 and 1b3 that impairs cancer cell survival.
ACS chemical biology. 10(4):925-32 [DOI] 10.1021/cb500893q. [PMID] 25602368.
2015
Target-based screen against a periplasmic serine protease that regulates intrabacterial pH homeostasis in Mycobacterium tuberculosis.
ACS chemical biology. 10(2):364-71 [DOI] 10.1021/cb500746z. [PMID] 25457457.
2014
A phenotypic high throughput screening assay for the identification of pharmacoperones for the gonadotropin releasing hormone receptor.
Assay and drug development technologies. 12(4):238-46 [DOI] 10.1089/adt.2014.576. [PMID] 24831790.
2014
Characterization of selective exosite-binding inhibitors of matrix metalloproteinase 13 that prevent articular cartilage degradation in vitro.
Journal of medicinal chemistry. 57(22):9598-611 [DOI] 10.1021/jm501284e. [PMID] 25330343.
2014
Development of an HTS-compatible assay for the discovery of ASK1 signalosome inhibitors using alphascreen technology.
Assay and drug development technologies. 12(4):229-37 [DOI] 10.1089/adt.2013.558. [PMID] 24831789.
2014
Development of high throughput screening assays and pilot screen for inhibitors of metalloproteases meprin α and β.
Biopolymers. 102(5):396-406 [DOI] 10.1002/bip.22527. [PMID] 25048711.
2014
High-throughput screening for small molecule modulators of motor protein Kinesin.
Assay and drug development technologies. 12(8):470-80 [DOI] 10.1089/adt.2014.579. [PMID] 25383721.
2014
Identification of Potent and Selective Inhibitors of the Plasmodium falciparum M18 Aspartyl Aminopeptidase (PfM18AAP) of Human Malaria via High-Throughput Screening.
Journal of biomolecular screening. 19(7):1107-15 [DOI] 10.1177/1087057114525852. [PMID] 24619116.
2013
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.
Bioorganic & medicinal chemistry. 21(11):3138-46 [DOI] 10.1016/j.bmc.2013.03.031. [PMID] 23591260.
2013
Discovery, design and synthesis of a selective S1P(3) receptor allosteric agonist.
Bioorganic & medicinal chemistry letters. 23(23):6346-9 [DOI] 10.1016/j.bmcl.2013.09.075. [PMID] 24135724.
2013
Hydroxyquinoline-derived compounds and analoguing of selective Mcl-1 inhibitors using a functional biomarker.
Bioorganic & medicinal chemistry. 21(21):6642-9 [DOI] 10.1016/j.bmc.2013.08.017. [PMID] 23993674.
2013
Inhibitors of HIV-1 attachment. Part 8: the effect of C7-heteroaryl substitution on the potency, and in vitro and in vivo profiles of indole-based inhibitors.
Bioorganic & medicinal chemistry letters. 23(1):203-8 [DOI] 10.1016/j.bmcl.2012.10.117. [PMID] 23200249.
2013
Selective inhibitors and tailored activity probes for lipoprotein-associated phospholipase A(2).
Bioorganic & medicinal chemistry letters. 23(3):839-43 [DOI] 10.1016/j.bmcl.2012.11.061. [PMID] 23260346.
2013
Unique drug screening approach for prion diseases identifies tacrolimus and astemizole as antiprion agents.
Proceedings of the National Academy of Sciences of the United States of America. 110(17):7044-9 [DOI] 10.1073/pnas.1303510110. [PMID] 23576755.
2012
Confirming target engagement for reversible inhibitors in vivo by kinetically tuned activity-based probes.
Journal of the American Chemical Society. 134(25):10345-8 [DOI] 10.1021/ja303400u. [PMID] 22690931.
2012
Small-molecule inhibitors of bacterial AddAB and RecBCD helicase-nuclease DNA repair enzymes.
ACS chemical biology. 7(5):879-91 [DOI] 10.1021/cb300018x. [PMID] 22443934.
2011
A high-throughput assay for the identification of drugs against late-stage Plasmodium falciparum gametocytes.
Molecular and biochemical parasitology. 180(2):127-31 [DOI] 10.1016/j.molbiopara.2011.09.002. [PMID] 21939693.
2011
A substrate-free activity-based protein profiling screen for the discovery of selective PREPL inhibitors.
Journal of the American Chemical Society. 133(30):11665-74 [DOI] 10.1021/ja2036095. [PMID] 21692504.
2011
Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors.
Proceedings of the National Academy of Sciences of the United States of America. 108(17):6811-6 [DOI] 10.1073/pnas.1015248108. [PMID] 21398589.
2011
Development of an HTS-compatible assay for discovery of RORα modulators using AlphaScreen® technology.
Journal of biomolecular screening. 16(2):183-91 [DOI] 10.1177/1087057110389040. [PMID] 21297105.
2011
Identification of small-molecule inhibitors of the colorectal cancer oncogene Krüppel-like factor 5 expression by ultrahigh-throughput screening.
Molecular cancer therapeutics. 10(11):2043-51 [DOI] 10.1158/1535-7163.MCT-11-0550. [PMID] 21885866.
2011
Potent and selective inhibitors of glutathione S-transferase omega 1 that impair cancer drug resistance.
Journal of the American Chemical Society. 133(41):16605-16 [DOI] 10.1021/ja2066972. [PMID] 21899313.
2010
A time-resolved fluorescence-resonance energy transfer assay for identifying inhibitors of hepatitis C virus core dimerization.
Assay and drug development technologies. 8(1):96-105 [DOI] 10.1089/adt.2009.0217. [PMID] 20035614.
2010
NH-1,2,3-Triazole-based Inhibitors of the VIM-2 Metallo-β-Lactamase: Synthesis and Structure-Activity Studies.
ACS medicinal chemistry letters. 1(4):150-154 [PMID] 20625539.
2010
Oxime esters as selective, covalent inhibitors of the serine hydrolase retinoblastoma-binding protein 9 (RBBP9).
Bioorganic & medicinal chemistry letters. 20(7):2254-8 [DOI] 10.1016/j.bmcl.2010.02.011. [PMID] 20207142.
2010
Selective and brain penetrant neuropeptide y y2 receptor antagonists discovered by whole-cell high-throughput screening.
Molecular pharmacology. 77(1):46-57 [DOI] 10.1124/mol.109.058677. [PMID] 19837904.
2009
Inhibitors of HIV-1 attachment. Part 2: An initial survey of indole substitution patterns.
Bioorganic & medicinal chemistry letters. 19(7):1977-81 [DOI] 10.1016/j.bmcl.2009.02.040. [PMID] 19251416.
2009
Inhibitors of HIV-1 attachment. Part 3: A preliminary survey of the effect of structural variation of the benzamide moiety on antiviral activity.
Bioorganic & medicinal chemistry letters. 19(17):5136-9 [DOI] 10.1016/j.bmcl.2009.07.027. [PMID] 19632112.
2009
Inhibitors of HIV-1 attachment. Part 4: A study of the effect of piperazine substitution patterns on antiviral potency in the context of indole-based derivatives.
Bioorganic & medicinal chemistry letters. 19(17):5140-5 [DOI] 10.1016/j.bmcl.2009.07.076. [PMID] 19664921.
2009
Inhibitors of VIM-2 by screening pharmacologically active and click-chemistry compound libraries.
Bioorganic & medicinal chemistry. 17(14):5027-37 [DOI] 10.1016/j.bmc.2009.05.070. [PMID] 19553129.
2008
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).
Journal of biomolecular screening. 13(1):17-28 [DOI] 10.1177/1087057107310806. [PMID] 18227223.
2008
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 chemical biology. 3(8):486-98 [DOI] 10.1021/cb800051m. [PMID] 18590333.
2008
Screening of potential a disintegrin and metalloproteinase with thrombospondin motifs-4 inhibitors using a collagen model fluorescence resonance energy transfer substrate.
Analytical biochemistry. 373(1):43-51 [PMID] 17949675.
2003
A small molecule HIV-1 inhibitor that targets the HIV-1 envelope and inhibits CD4 receptor binding.
Proceedings of the National Academy of Sciences of the United States of America. 100(19):11013-8 [PMID] 12930892.
2003
An ultra-HTS process for the identification of small molecule modulators of orphan G-protein-coupled receptors.
Drug discovery today. 8(17):785-92 [PMID] 12946641.
2003
Discovery of 4-benzoyl-1-[(4-methoxy-1H- pyrrolo[2,3-b]pyridin-3-yl)oxoacetyl]-2- (R)-methylpiperazine (BMS-378806): a novel HIV-1 attachment inhibitor that interferes with CD4-gp120 interactions.
Journal of medicinal chemistry. 46(20):4236-9 [PMID] 13678401.
2000
In vitro resistance profile of the human immunodeficiency virus type 1 protease inhibitor BMS-232632.
Antimicrobial agents and chemotherapy. 44(9):2319-26 [PMID] 10952574.

Education

Ph.D. in Medicine
2019 · University of Queensland
Master's of Microbiology
1996 · State University of New York Health Science Center
Bachelor's of Science in Biology
1990 · State University of New York at Albany

Contact Details

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