Michael Cameron

Michael Cameron, Ph.D.

Sr Scientific Director, Associate Professor Of Molecular Medicine, Department Of Molecular Medicine

Department: SR-MM-CAMERON LAB
Business Phone: (561) 228-2223
Business Email: michaelcameron@ufl.edu

About Michael Cameron

Related Links:
Additional Positions:
Associate Professor
2013 – 2017 · Molecular Therapeutics, Scripps Research
Assistant Professor (Joint Appointment)
2007 – 2013 · Molecular Therapeutics, Scripps Research
Senior Scientist
2003 – 2005 · CellzDirect

Research Profile

The Cameron Laboratory works on a variety of independent and collaborative projects centered on the metabolic fate of new chemical compounds. We explore the role of drug metabolism in chemical induced toxicity and drug-drug interactions. Current projects include evaluation of reactive metabolites and their role in drug induced toxicity, time and mechanism based inhibition of cytochrome P450, and the development of chemical tools to differentiate CYP3A4 and CYP3A5 activity in biological samples. The lab is also involved in several translational projects focused on the development of clinical candidates or molecular probes for the study of biological pathways. The lab offers Drug Metabolism and Pharmacokinetics (DMPK) expertise, collaborating with medicinal chemistry, biology and pharmacology groups. The lab evaluates such factors as chemical and metabolic stability, solubility, oral absorption, rat and mouse pharmacokinetics, tissue distribution, protein binding, P450 inhibition, reactive intermediate formation, and metabolite identification to help refine molecules. Current projects include optimization of neuropeptide Y Y2 receptor antagonists, orexin-1 receptor antagonists, (GABA) B receptor positive allosteric modulators, neurotensin 1 receptor agonists, a5* nicotinic acetylcholine receptors, positive allosteric modulators, kappa opioid receptor antagonists, and functionally biased mu opioid receptor agonists.

Open Researcher and Contributor ID (ORCID)

0000-0003-3154-4775

Publications

2024
HDAC specificity and kinase off-targeting by purine-benzohydroxamate anti-hematological tumor agents
European Journal of Medicinal Chemistry. 263 [DOI] 10.1016/j.ejmech.2023.115935.
2023
1,3-Diphenylureido hydroxamate as a promising scaffold for generation of potent antimalarial histone deacetylase inhibitors
Scientific Reports. 13(1) [DOI] 10.1038/s41598-023-47959-z. [PMID] 38030668.
2023
Addressing the oxamniquine in vitro-in vivo paradox to facilitate a new generation of anti-schistosome treatments
International Journal for Parasitology: Drugs and Drug Resistance. 21:65-73 [DOI] 10.1016/j.ijpddr.2023.01.003. [PMID] 36758271.
2023
Structure–Activity Relationship and Biological Investigation of a REV-ERBα-Selective Agonist SR-29065 (34) for Autoimmune Disorders
Journal of Medicinal Chemistry. 66(21):14815-14823 [DOI] 10.1021/acs.jmedchem.3c01413.
2022
A Novel HER2-Selective Kinase Inhibitor Is Effective in HER2 Mutant and Amplified Non-Small Cell Lung Cancer.
Cancer research. 82(8):1633-1645 [DOI] 10.1158/0008-5472.CAN-21-2693. [PMID] 35149586.
2022
Advances in Sulfonamide Kappa Opioid Receptor Antagonists: Structural Refinement and Evaluation of CNS Clearance
ACS Chemical Neuroscience. 13(8):1315-1332 [DOI] 10.1021/acschemneuro.2c00140.
2022
An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer.
Nature cancer. 3(4):402-417 [DOI] 10.1038/s43018-022-00351-8. [PMID] 35422503.
2022
Development of a putative Zn2+-chelating but highly selective MMP-13 inhibitor.
Bioorganic & medicinal chemistry letters. 76 [DOI] 10.1016/j.bmcl.2022.129014. [PMID] 36202189.
2022
DNA-Encoded Library Screening To Inform Design of a Ribonuclease Targeting Chimera (RiboTAC)
Journal of the American Chemical Society. 144(46):21096-21102 [DOI] 10.1021/jacs.2c07217. [PMID] 36342850.
2022
Dual Inhibitors of Main Protease (MPro) and Cathepsin L as Potent Antivirals against SARS-CoV2
Journal of the American Chemical Society. 144(46):21035-21045 [DOI] 10.1021/jacs.2c04626. [PMID] 36356199.
2022
Identification and Characterization of a Novel Indoleamine 2,3-Dioxygenase 1 Protein Degrader for Glioblastoma
Journal of Medicinal Chemistry. 65(23):15642-15662 [DOI] 10.1021/acs.jmedchem.2c00771. [PMID] 36410047.
2022
Morphing Natural Product Platensimycin via Heck, Sonogashira, and One-Pot Sonogashira/Cycloaddition Reactions to Produce Antibiotics with In Vivo Activity.
Antibiotics (Basel, Switzerland). 11(4) [DOI] 10.3390/antibiotics11040425. [PMID] 35453177.
2021
A promising chemical series of positive allosteric modulators of the μ-opioid receptor that enhance the antinociceptive efficacy of opioids but not their adverse effects
Neuropharmacology. 195 [DOI] 10.1016/j.neuropharm.2021.108673. [PMID] 34153316.
2021
Chemical systems biology reveals mechanisms of glucocorticoid receptor signaling
Nature Chemical Biology. 17(3):307-316 [DOI] 10.1038/s41589-020-00719-w. [PMID] 33510451.
2021
Comparison of morphine, oxycodone and the biased MOR agonist SR-17018 for tolerance and efficacy in mouse models of pain.
Neuropharmacology. 185 [DOI] 10.1016/j.neuropharm.2020.108439. [PMID] 33345829.
2021
Discovery of Selective Inhibitors for In Vitro and In Vivo Interrogation of Skeletal Myosin II
ACS Chemical Biology. 16(11):2164-2173 [DOI] 10.1021/acschembio.1c00067.
2021
Oxidative Metabolism as a Modulator of Kratom’s Biological Actions
Journal of Medicinal Chemistry. 64(22):16553-16572 [DOI] 10.1021/acs.jmedchem.1c01111. [PMID] 34783240.
2021
Reprogramming of Protein-Targeted Small-Molecule Medicines to RNA by Ribonuclease Recruitment.
Journal of the American Chemical Society. 143(33):13044-13055 [DOI] 10.1021/jacs.1c02248. [PMID] 34387474.
2021
Small molecule 1a reduces FMRpolyG-mediated toxicity in in vitro and in vivo models for FMR1 premutation.
Human molecular genetics. 30(17):1632-1648 [DOI] 10.1093/hmg/ddab143. [PMID] 34077515.
2021
Structure-Activity Relationship and Biological Investigation of SR18292 (16), a Suppressor of Glucagon-Induced Glucose Production.
Journal of medicinal chemistry. 64(2):980-990 [DOI] 10.1021/acs.jmedchem.0c01450. [PMID] 33434430.
2021
The HCK/BTK inhibitor KIN-8194 is active in MYD88-driven lymphomas and overcomes mutated BTKCys481 ibrutinib resistance
Blood. 138(20):1966-1979 [DOI] 10.1182/blood.2021011405. [PMID] 34132782.
2020
A G protein signaling-biased agonist at the μ-opioid receptor reverses morphine tolerance while preventing morphine withdrawal.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 45(2):416-425 [DOI] 10.1038/s41386-019-0491-8. [PMID] 31443104.
2020
Design of a small molecule that stimulates vascular endothelial growth factor A enabled by screening RNA fold-small molecule interactions.
Nature chemistry. 12(10):952-961 [DOI] 10.1038/s41557-020-0514-4. [PMID] 32839603.
2020
Discovery of small-molecule enzyme activators by activity-based protein profiling
Nature Chemical Biology. 16(9):997-1005 [DOI] 10.1038/s41589-020-0555-4. [PMID] 32514184.
2020
Hydrocarbon-Stitched Peptide Agonists of Glucagon-Like Peptide-1 Receptor.
ACS chemical biology. 15(6):1340-1348 [DOI] 10.1021/acschembio.0c00308. [PMID] 32348108.
2020
Increased lysosomal biomass is responsible for the resistance of triple-negative breast cancers to CDK4/6 inhibition
Science Advances. 6(25) [DOI] 10.1126/sciadv.abb2210. [PMID] 32704543.
2020
Promoting activity of (α4)3(β2)2 nicotinic cholinergic receptors reduces ethanol consumption.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 45(2):301-308 [DOI] 10.1038/s41386-019-0475-8. [PMID] 31394567.
2020
Vancomycin C-Terminus Guanidine Modifications and Further Insights into an Added Mechanism of Action Imparted by a Peripheral Structural Modification.
ACS infectious diseases. 6(8):2169-2180 [DOI] 10.1021/acsinfecdis.0c00258. [PMID] 32598127.
2019
Design and Synthesis of a Novel and Selective Kappa Opioid Receptor (KOR) Antagonist (BTRX-335140).
Journal of medicinal chemistry. 62(4):1761-1780 [DOI] 10.1021/acs.jmedchem.8b01679. [PMID] 30707578.
2019
Discovery and Optimization of a Series of Sulfonamide Inverse Agonists for the Retinoic Acid Receptor-Related Orphan Receptor-α.
Medicinal chemistry (Shariqah (United Arab Emirates)). 15(6):676-684 [DOI] 10.2174/1573406415666190222124745. [PMID] 30799793.
2019
Evaluation of Platensimycin and Platensimycin-Inspired Thioether Analogues against Methicillin-Resistant Staphylococcus aureus in Topical and Systemic Infection Mouse Models.
Molecular pharmaceutics. 16(7):3065-3071 [DOI] 10.1021/acs.molpharmaceut.9b00293. [PMID] 31244223.
2019
Precise small-molecule cleavage of an r(CUG) repeat expansion in a myotonic dystrophy mouse model.
Proceedings of the National Academy of Sciences of the United States of America. 116(16):7799-7804 [DOI] 10.1073/pnas.1901484116. [PMID] 30926669.
2019
Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor.
Cancer discovery. 9(7):926-943 [DOI] 10.1158/2159-8290.CD-18-0903. [PMID] 31092401.
2019
Site-Selective Antibody Functionalization via Orthogonally Reactive Arginine and Lysine Residues.
Cell chemical biology. 26(9):1229-1239.e9 [DOI] 10.1016/j.chembiol.2019.05.010. [PMID] 31231031.
2018
Design, synthesis, and evaluation of simple phenol amides as ERRγ agonists.
Bioorganic & medicinal chemistry letters. 28(8):1313-1319 [DOI] 10.1016/j.bmcl.2018.03.019. [PMID] 29548571.
2018
Development of matrix metalloproteinase-13 inhibitors – A structure-activity/structure-property relationship study.
Bioorganic & medicinal chemistry. 26(18):4984-4995 [DOI] 10.1016/j.bmc.2018.08.020. [PMID] 30249495.
2018
Development of novel NEMO-binding domain mimetics for inhibiting IKK/NF-κB activation.
PLoS biology. 16(6) [DOI] 10.1371/journal.pbio.2004663. [PMID] 29889904.
2018
Discovery of Hydrolysis-Resistant Isoindoline N-Acyl Amino Acid Analogues that Stimulate Mitochondrial Respiration.
Journal of medicinal chemistry. 61(7):3224-3230 [DOI] 10.1021/acs.jmedchem.8b00029. [PMID] 29533650.
2018
Identification of an aminothiazole series of RORβ modulators.
Bioorganic & medicinal chemistry letters. 28(7):1178-1181 [DOI] 10.1016/j.bmcl.2018.03.001. [PMID] 29534930.
2018
Optimization of a Series of Mu Opioid Receptor (MOR) Agonists with High G Protein Signaling Bias.
Journal of medicinal chemistry. 61(19):8895-8907 [DOI] 10.1021/acs.jmedchem.8b01136. [PMID] 30199635.
2018
REV-ERBα Regulates TH17 Cell Development and Autoimmunity.
Cell reports. 25(13):3733-3749.e8 [DOI] 10.1016/j.celrep.2018.11.101. [PMID] 30590045.
2017
Bias Factor and Therapeutic Window Correlate to Predict Safer Opioid Analgesics.
Cell. 171(5):1165-1175.e13 [DOI] 10.1016/j.cell.2017.10.035. [PMID] 29149605.
2017
Fentanyl-related designer drugs W-18 and W-15 lack appreciable opioid activity in vitro and in vivo.
JCI insight. 2(22) [DOI] 10.1172/jci.insight.97222. [PMID] 29202454.
2017
In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.
Bioorganic & medicinal chemistry. 25(6):1990-1996 [DOI] 10.1016/j.bmc.2017.02.028. [PMID] 28237556.
2017
M344 promotes nonamyloidogenic amyloid precursor protein processing while normalizing Alzheimer’s disease genes and improving memory.
Proceedings of the National Academy of Sciences of the United States of America. 114(43):E9135-E9144 [DOI] 10.1073/pnas.1707544114. [PMID] 29073110.
2017
Precise small-molecule recognition of a toxic CUG RNA repeat expansion.
Nature chemical biology. 13(2):188-193 [DOI] 10.1038/nchembio.2251. [PMID] 27941760.
2017
Rational design of peptide derivatives for inhibition of MyD88-mediated toll-like receptor signaling in human peripheral blood mononuclear cells and epithelial cells exposed to Francisella tularensis.
Chemical biology & drug design. 90(6):1190-1205 [DOI] 10.1111/cbdd.13039. [PMID] 28599094.
2016
Albumin-Oxanorbornadiene Conjugates Formed ex Vivo for the Extended Circulation of Hydrophilic Cargo.
ACS chemical biology. 11(8):2320-7 [DOI] 10.1021/acschembio.6b00444. [PMID] 27348438.
2016
Biased agonists of the kappa opioid receptor suppress pain and itch without causing sedation or dysphoria.
Science signaling. 9(456) [PMID] 27899527.
2016
Design of a small molecule against an oncogenic noncoding RNA.
Proceedings of the National Academy of Sciences of the United States of America. 113(21):5898-903 [DOI] 10.1073/pnas.1523975113. [PMID] 27170187.
2016
N-Arylsulfonyl Indolines as Retinoic Acid Receptor-Related Orphan Receptor γ (RORγ) Agonists.
ChemMedChem. 11(23):2607-2620 [DOI] 10.1002/cmdc.201600491. [PMID] 27879053.
2016
Nonmuscle myosin IIB as a therapeutic target for the prevention of relapse to methamphetamine use.
Molecular psychiatry. 21(5):615-23 [DOI] 10.1038/mp.2015.103. [PMID] 26239291.
2016
P450 3A-Catalyzed O-Dealkylation of Lapatinib Induces Mitochondrial Stress and Activates Nrf2.
Chemical research in toxicology. 29(5):784-96 [DOI] 10.1021/acs.chemrestox.5b00524. [PMID] 26958860.
2016
Probing the Complex Binding Modes of the PPARγ Partial Agonist 2-Chloro-N-(3-chloro-4-((5-chlorobenzo[d]thiazol-2-yl)thio)phenyl)-4-(trifluoromethyl)benzenesulfonamide (T2384) to Orthosteric and Allosteric Sites with NMR Spectroscopy.
Journal of medicinal chemistry. 59(22):10335-10341 [DOI] 10.1021/acs.jmedchem.6b01340. [PMID] 27783520.
2016
Synthesis and Evaluation of Oxyguanidine Analogues of the Cysteine Protease Inhibitor WRR-483 against Cruzain.
ACS medicinal chemistry letters. 7(1):77-82 [DOI] 10.1021/acsmedchemlett.5b00336. [PMID] 26819670.
2016
TNP [N2-(m-Trifluorobenzyl), N6-(p-nitrobenzyl)purine] ameliorates diet induced obesity and insulin resistance via inhibition of the IP6K1 pathway.
Molecular metabolism. 5(10):903-917 [DOI] 10.1016/j.molmet.2016.08.008. [PMID] 27689003.
2015
Antiobesity Effect of a Small Molecule Repressor of RORγ.
Molecular pharmacology. 88(1):48-56 [DOI] 10.1124/mol.114.097485. [PMID] 25904554.
2015
Design, Synthesis, and Biological Evaluation of Indole Biphenylcarboxylic Acids as PPARγ Antagonists.
ACS medicinal chemistry letters. 6(9):998-1003 [DOI] 10.1021/acsmedchemlett.5b00218. [PMID] 26396687.
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
Selective Targeting of Extracellular Insulin-Degrading Enzyme by Quasi-Irreversible Thiol-Modifying Inhibitors.
ACS chemical biology. 10(12):2716-24 [DOI] 10.1021/acschembio.5b00334. [PMID] 26398879.
2014
4-Aminopyridyl-based CYP51 inhibitors as anti-Trypanosoma cruzi drug leads with improved pharmacokinetic profile and in vivo potency.
Journal of medicinal chemistry. 57(16):6989-7005 [DOI] 10.1021/jm500448u. [PMID] 25101801.
2014
Binding mode and potency of N-indolyloxopyridinyl-4-aminopropanyl-based inhibitors targeting Trypanosoma cruzi CYP51.
Journal of medicinal chemistry. 57(23):10162-75 [DOI] 10.1021/jm501568b. [PMID] 25393646.
2014
Blocking lactate export by inhibiting the Myc target MCT1 Disables glycolysis and glutathione synthesis.
Cancer research. 74(3):908-20 [DOI] 10.1158/0008-5472.CAN-13-2034. [PMID] 24285728.
2014
Characterization of T-5 N-oxide formation as the first highly selective measure of CYP3A5 activity.
Drug metabolism and disposition: the biological fate of chemicals. 42(3):334-42 [DOI] 10.1124/dmd.113.054726. [PMID] 24335391.
2014
R-Configuration of 4-Aminopyridyl-Based Inhibitors of CYP51 Confers Superior Efficacy Against Trypanosoma cruzi.
ACS medicinal chemistry letters. 5(4):434-9 [DOI] 10.1021/ml500010m. [PMID] 24900854.
2014
Synthesis and activity of substituted heteroaromatics as positive allosteric modulators for α4β2α5 nicotinic acetylcholine receptors.
Bioorganic & medicinal chemistry letters. 24(2):674-8 [DOI] 10.1016/j.bmcl.2013.11.049. [PMID] 24365158.
2014
Synthesis and SAR of novel isoxazoles as potent c-jun N-terminal kinase (JNK) inhibitors.
Bioorganic & medicinal chemistry letters. 24(1):161-4 [DOI] 10.1016/j.bmcl.2013.11.052. [PMID] 24332487.
2013
Amino acid derived quinazolines as Rock/PKA inhibitors.
Bioorganic & medicinal chemistry letters. 23(6):1592-9 [DOI] 10.1016/j.bmcl.2013.01.109. [PMID] 23416002.
2013
Design and synthesis of 1-aryl-5-anilinoindazoles as c-Jun N-terminal kinase inhibitors.
Bioorganic & medicinal chemistry letters. 23(9):2683-7 [DOI] 10.1016/j.bmcl.2013.02.082. [PMID] 23518277.
2013
Development of functionally selective, small molecule agonists at kappa opioid receptors.
The Journal of biological chemistry. 288(51):36703-16 [DOI] 10.1074/jbc.M113.504381. [PMID] 24187130.
2013
Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties.
Bioorganic & medicinal chemistry letters. 23(15):4374-80 [DOI] 10.1016/j.bmcl.2013.05.075. [PMID] 23787102.
2013
Rational development of 4-aminopyridyl-based inhibitors targeting Trypanosoma cruzi CYP51 as anti-chagas agents.
Journal of medicinal chemistry. 56(19):7651-68 [DOI] 10.1021/jm401067s. [PMID] 24079662.
2013
Small molecule amides as potent ROR-γ selective modulators.
Bioorganic & medicinal chemistry letters. 23(2):532-6 [DOI] 10.1016/j.bmcl.2012.11.025. [PMID] 23232056.
2013
Synthesis and biological evaluation of urea derivatives as highly potent and selective rho kinase inhibitors.
Journal of medicinal chemistry. 56(9):3568-81 [DOI] 10.1021/jm400062r. [PMID] 23570561.
2013
Synthesis and SAR of Lehualide B: a marine-derived natural product with potent anti-multiple myeloma activity.
ACS chemical biology. 8(6):1241-52 [DOI] 10.1021/cb300582s. [PMID] 23547759.
2013
Synthesis of benzoquinone ansamycin-inspired macrocyclic lactams from shikimic acid.
Angewandte Chemie (International ed. in English). 52(18):4800-4 [DOI] 10.1002/anie.201301323. [PMID] 23554224.
2012
D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy.
ACS medicinal chemistry letters. 3(12):1081-1085 [PMID] 23420624.
2012
Discovery of a highly selective CYP3A4 inhibitor suitable for reaction phenotyping studies and differentiation of CYP3A4 and CYP3A5.
Drug metabolism and disposition: the biological fate of chemicals. 40(9):1803-9 [DOI] 10.1124/dmd.112.046144. [PMID] 22696420.
2012
Disubstituted piperidines as potent orexin (hypocretin) receptor antagonists.
Bioorganic & medicinal chemistry letters. 22(12):3890-4 [DOI] 10.1016/j.bmcl.2012.04.122. [PMID] 22617492.
2012
Imidazopyridines as selective CYP3A4 inhibitors.
Bioorganic & medicinal chemistry letters. 22(4):1611-4 [DOI] 10.1016/j.bmcl.2011.12.125. [PMID] 22264486.
2012
Potential role of a quetiapine metabolite in quetiapine-induced neutropenia and agranulocytosis.
Chemical research in toxicology. 25(5):1004-11 [DOI] 10.1021/tx2005635. [PMID] 22506851.
2012
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
Nature. 485(7396):62-8 [DOI] 10.1038/nature11030. [PMID] 22460951.
2012
S1P(1) receptor modulation with cyclical recovery from lymphopenia ameliorates mouse model of multiple sclerosis.
Molecular pharmacology. 81(2):166-74 [DOI] 10.1124/mol.111.076109. [PMID] 22031473.
2012
Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα.
Bioorganic & medicinal chemistry letters. 22(13):4413-7 [DOI] 10.1016/j.bmcl.2012.04.126. [PMID] 22633688.
2012
Synthesis and SAR of tetrahydroisoquinolines as Rev-erbα agonists.
Bioorganic & medicinal chemistry letters. 22(11):3739-42 [DOI] 10.1016/j.bmcl.2012.04.023. [PMID] 22560469.
2011
Antidiabetic actions of a non-agonist PPARγ ligand blocking Cdk5-mediated phosphorylation.
Nature. 477(7365):477-81 [DOI] 10.1038/nature10383. [PMID] 21892191.
2011
Discovery and optimization of indole and 7-azaindoles as Rho kinase (ROCK) inhibitors (part-II).
Bioorganic & medicinal chemistry letters. 21(23):7113-8 [DOI] 10.1016/j.bmcl.2011.09.084. [PMID] 22018789.
2011
Discovery and optimization of indoles and 7-azaindoles as Rho kinase (ROCK) inhibitors (part-I).
Bioorganic & medicinal chemistry letters. 21(23):7107-12 [DOI] 10.1016/j.bmcl.2011.09.083. [PMID] 22004718.
2011
Identification of a novel non-retinoid pan inverse agonist of the retinoic acid receptors.
ACS chemical biology. 6(6):618-27 [DOI] 10.1021/cb100396s. [PMID] 21381756.
2011
Identification of SR3335 (ML-176): a synthetic RORα selective inverse agonist.
ACS chemical biology. 6(3):218-22 [DOI] 10.1021/cb1002762. [PMID] 21090593.
2011
JNK Inhibition Protects Dopamine Neurons and Provides Behavioral Improvement in a Rat 6-hydroxydopamine Model of Parkinson’s Disease.
ACS chemical neuroscience. 2(4):207-212 [PMID] 21666838.
2011
Small Molecule c-jun-N-terminal Kinase (JNK) Inhibitors Protect Dopaminergic Neurons in a Model of Parkinson’s Disease.
ACS chemical neuroscience. 2(4):198-206 [PMID] 21666839.
2011
Synthesis and biological evaluation of 4-quinazolinones as Rho kinase inhibitors.
Bioorganic & medicinal chemistry letters. 21(6):1844-8 [DOI] 10.1016/j.bmcl.2011.01.039. [PMID] 21349713.
2011
Synthesis and SAR of 2-phenoxypyridines as novel c-Jun N-terminal kinase inhibitors.
Bioorganic & medicinal chemistry letters. 21(23):7072-5 [DOI] 10.1016/j.bmcl.2011.09.090. [PMID] 22004719.
2011
Synthesis and SAR of 4-(pyrazol-3-yl)-pyridines as novel c-jun N-terminal kinase inhibitors.
Bioorganic & medicinal chemistry letters. 21(9):2732-5 [DOI] 10.1016/j.bmcl.2010.11.104. [PMID] 21185177.
2011
Synthesis and SAR of novel quinazolines as potent and brain-penetrant c-jun N-terminal kinase (JNK) inhibitors.
Bioorganic & medicinal chemistry letters. 21(6):1719-23 [DOI] 10.1016/j.bmcl.2011.01.079. [PMID] 21316221.
2011
Synthesis of conolidine, a potent non-opioid analgesic for tonic and persistent pain.
Nature chemistry. 3(6):449-53 [DOI] 10.1038/nchem.1050. [PMID] 21602859.
2010
Cytochrome P450-mediated bioactivation of the epidermal growth factor receptor inhibitor erlotinib to a reactive electrophile.
Drug metabolism and disposition: the biological fate of chemicals. 38(7):1238-45 [DOI] 10.1124/dmd.109.030361. [PMID] 20382753.
2010
Discovery of Potent and Selective Urea-Based ROCK Inhibitors and Their Effects on Intraocular Pressure in Rats.
ACS medicinal chemistry letters. 1(4):175-9 [DOI] 10.1021/ml1000382. [PMID] 24900192.
2010
Metabolism considerations for kinase inhibitors in cancer treatment.
Expert opinion on drug metabolism & toxicology. 6(10):1175-93 [DOI] 10.1517/17425255.2010.506873. [PMID] 20684746.
2010
Synthesis, biological evaluation, X-ray structure, and pharmacokinetics of aminopyrimidine c-jun-N-terminal kinase (JNK) inhibitors.
Journal of medicinal chemistry. 53(1):419-31 [DOI] 10.1021/jm901351f. [PMID] 19947601.
2010
Tetrahydroisoquinoline derivatives as highly selective and potent Rho kinase inhibitors.
Journal of medicinal chemistry. 53(15):5727-37 [DOI] 10.1021/jm100579r. [PMID] 20684608.
2010
The development of benzimidazoles as selective rho kinase inhibitors.
Bioorganic & medicinal chemistry letters. 20(6):1939-43 [DOI] 10.1016/j.bmcl.2010.01.124. [PMID] 20167489.
2009
Benzothiazoles as Rho-associated kinase (ROCK-II) inhibitors.
Bioorganic & medicinal chemistry letters. 19(23):6686-90 [DOI] 10.1016/j.bmcl.2009.09.115. [PMID] 19837589.
2009
Bioactivation of the epidermal growth factor receptor inhibitor gefitinib: implications for pulmonary and hepatic toxicities.
Chemical research in toxicology. 22(10):1736-42 [DOI] 10.1021/tx900256y. [PMID] 19803472.
2009
Characterization of dasatinib and its structural analogs as CYP3A4 mechanism-based inactivators and the proposed bioactivation pathways.
Drug metabolism and disposition: the biological fate of chemicals. 37(6):1242-50 [DOI] 10.1124/dmd.108.025932. [PMID] 19282395.
2008
Benzimidazole- and benzoxazole-based inhibitors of Rho kinase.
Bioorganic & medicinal chemistry letters. 18(24):6390-3 [DOI] 10.1016/j.bmcl.2008.10.095. [PMID] 18996009.
2008
Chroman-3-amides as potent Rho kinase inhibitors.
Bioorganic & medicinal chemistry letters. 18(24):6406-9 [DOI] 10.1016/j.bmcl.2008.10.080. [PMID] 18990570.
2008
Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors.
Journal of medicinal chemistry. 51(21):6642-5 [DOI] 10.1021/jm800986w. [PMID] 18834107.
2008
Genetic regulation of behavioral and neuronal responses to fluoxetine.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 33(6):1312-22 [PMID] 17609676.
2008
Insular hypocretin transmission regulates nicotine reward.
Proceedings of the National Academy of Sciences of the United States of America. 105(49):19480-5 [DOI] 10.1073/pnas.0808023105. [PMID] 19033203.
2008
Potent, selective and cell penetrant inhibitors of SF-1 by functional ultra-high-throughput screening.
Molecular pharmacology. 73(6):1776-84 [DOI] 10.1124/mol.108.045963. [PMID] 18334597.
2007
In vitro prediction and in vivo verification of enantioselective human tofisopam metabolite profiles.
Drug metabolism and disposition: the biological fate of chemicals. 35(10):1894-902 [PMID] 17646282.
2007
Structure-activity relationships, and drug metabolism and pharmacokinetic properties for indazole piperazine and indazole piperidine inhibitors of ROCK-II.
Bioorganic & medicinal chemistry letters. 17(8):2355-60 [PMID] 17368019.

Grants

Apr 2024 ACTIVE
Preclinical development of a precision therapy for a monogenic mental health disorder
Role: Co-Investigator
Funding: NATL INST OF HLTH
Jan 2024 ACTIVE
An Innovative Approach to Identify Correctors of Metabolic Complications in HIV
Role: Co-Investigator
Funding: SCRIPPS RESEARCH INST via NATL INST OF HLTH NIDDK
Sep 2023 ACTIVE
Development of Clinical Candidates for the Treatment of Myotonic Dystrophy
Role: Co-Investigator
Funding: US ARMY MED RES ACQUISITION
Jul 2023 ACTIVE
Synthesis of peripherally active CB1 agonists as analgesics
Role: Principal Investigator
Funding: WASHINGTON UNIV SAINT LOUIS via NATL INST OF HLTH NINDS
Sep 2022 ACTIVE
Mitochondrial therapeutics for healthy brain aging
Role: Co-Investigator
Funding: NATL INST OF HLTH NIA
May 2022 ACTIVE
Midwest AViDD Center – CORE C
Role: Co-Investigator
Funding: UNIV OF MINNESOTA via NATL INST OF HLTH NIAID
Apr 2022 ACTIVE
Identification of novel anthelmintics through a target-based screen of a parasite ion channel
Role: Co-Investigator
Funding: MEDICAL COLLEGE OF WISCONSIN via NATL INST OF HLTH NIAID
Apr 2022 ACTIVE
Identification of small molecules for neurological complications of HIV and substance abuse comorbidity
Role: Co-Project Director/Principal Investigator
Funding: SCRIPPS RESEARCH INST via NATL INST OF HLTH NIDA
Apr 2022 ACTIVE
Development of novel therapeutics for opioid dependence
Role: Project Manager
Funding: ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI via NATL INST OF HLTH NIDA
Apr 2022 – May 2024
Covalent Inhibition as a Method to Counteract Botulinum Intoxication
Role: Principal Investigator
Funding: SCRIPPS RESEARCH INST via NATL INST OF HLTH NIAID
Apr 2022 – May 2024
Synthesis and Evaluation of Functionally Biased Opioid Analgesics
Role: Co-Investigator
Funding: NATL INST OF HLTH NIDA
Apr 2022 – Apr 2024
Identification of REV-ERB inverse agonists for cancer immunotherapy
Role: Project Manager
Funding: NATL INST OF HLTH NCI
Apr 2022 – Jun 2023
Synthesis of peripherally active CB1 agonists as analgesics
Role: Principal Investigator
Funding: UNIV OF HLTH SCIENCES & PHARM ST LOUIS via NATL INST OF HLTH NINDS
Apr 2022 – Aug 2022
Mitochondrial therapeutics for healthy brain aging
Role: Co-Investigator
Funding: NATL INST OF HLTH NIA

Education

Ph.D. in Biochemistry
2000 · Utah State University
Bachelor's of Science in Chemistry
1994 · Gonzaga University

Contact Details

Phones:
Business:
(561) 228-2223
Emails:
Addresses:
Business Mailing:
Location A201
130 SCRIPPS WAY BLDG 2A1
JUPITER FL 33458