T. Koudriakova

发表

An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms.

Shinji Yamazaki, Gordon Alton, Pei-Pei Kung, 2007, Cancer research.

Microsoft Word-49434885-file00

Weiwei Tan, K. Wilner, T. Koudriakova, 2010 .

Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development.

P. Bonaventure, Kiev S. Ly, T. Lovenberg, 2010, Bioorganic & medicinal chemistry letters.

Pharmacologic properties of AG-012986, a pan-cyclin-dependent kinase inhibitor with antitumor efficacy

P. O'Connor, S. Bender, B. Jessen, 2008, Molecular Cancer Therapeutics.

Isolation and identification of major urinary metabolites of rifabutin in rats and humans.

P. Vouros, T. Koudriakova, N. Gerber, 1997, Drug metabolism and disposition: the biological fate of chemicals.

Metabolic Stability Assessed by Liver Microsomes and Hepatocytes

T. Koudriakova, K. Coe, 2014 .

TITLE: Prediction of Oral Pharmacokinetics of cMet Kinase Inhibitors in Humans: Physiologically Based Pharmacokinetic Model versus Traditional One Compartment Model AUTHORS:

Weiwei Tan, K. Wilner, S. Yamazaki, 2010 .

Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor.

T. Lovenberg, N. Carruthers, Hong Ao, 2016, Journal of medicinal chemistry.

Characterization of JNJ-2482272 [4-(4-Methyl-2-(4-(Trifluoromethyl)Phenyl)Thiazole-5-yl) Pyrimidine-2-Amine] As a Strong Aryl Hydrocarbon Receptor Activator in Rat and Human

A. Bittner, N. Lim, J. W. Higgins, 2022, Drug Metabolism and Disposition.

Quantitation and mapping of aflatoxin B1-induced DNA damage in genomic DNA using aflatoxin B1-8,9-epoxide and microsomal activation systems.

G. Pfeifer, M. Denissenko, T. Koudriakova, 1999, Mutation research.

Discovery of N-arylpyrroles as agonists of GPR120 for the treatment of type II diabetes.

Z. Sui, T. Koudriakova, W. Murray, 2018, Bioorganic & medicinal chemistry letters.

Novel Octahydropyrrolo[3,4-c]pyrroles Are Selective Orexin-2 Antagonists: SAR Leading to a Clinical Candidate.

P. Bonaventure, Kiev S. Ly, T. Lovenberg, 2015, Journal of medicinal chemistry.

Characterization of JNJ-42847922, a Selective Orexin-2 Receptor Antagonist, as a Clinical Candidate for the Treatment of Insomnia

P. Bonaventure, T. Lovenberg, N. Carruthers, 2015, The Journal of Pharmacology and Experimental Therapeutics.

Identification of Time-Dependent CYP Inhibitors Using Human Liver Microsomes (HLM)

T. Koudriakova, J. Skaptason, K. Coe, 2014 .

Substituted Azabicyclo[2.2.1]heptanes as Selective Orexin-1 Antagonists: Discovery of JNJ-54717793.

P. Bonaventure, C. Dvorak, T. Lovenberg, 2020, ACS medicinal chemistry letters.

4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate.

P. Bonaventure, C. Dvorak, T. Lovenberg, 2017, Journal of medicinal chemistry.

Substituted 5,6-(Dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)-methanones as P2X7 Antagonists.

P. Bonaventure, T. Lovenberg, N. Carruthers, 2016, ACS chemical neuroscience.

In vitro and in vivo evaluation of 6-azido-2',3'-dideoxy-2'-fluoro-beta-D-arabinofuranosylpurine and N6-methyl-2',3'-dideoxy-2'-fluoro-beta-D-arabinofuranosyladenine as prodrugs of the anti-HIV nucleosides 2'-F-ara-ddA and 2'-F-ara-ddI.

L. Kotra, R. Schinazi, C. K. Chu, 1996, Journal of Medicinal Chemistry.

Enhanced brain delivery of an anti-HIV nucleoside 2'-F-ara-ddI by xanthine oxidase mediated biotransformation.

R. Schinazi, C. K. Chu, J. Gallo, 1994, Journal of medicinal chemistry.

Pharmacologic Characterization of JNJ-42226314, [1-(4-Fluorophenyl)indol-5-yl]-[3-[4-(thiazole-2-carbonyl)piperazin-1-yl]azetidin-1-yl]methanone, a Reversible, Selective, and Potent Monoacylglycerol Lipase Inhibitor

P. Bonaventure, T. Lovenberg, P. Connolly, 2019, The Journal of Pharmacology and Experimental Therapeutics.

Metabolism of rifabutin in human enterocyte and liver microsomes: Kinetic parameters, identification of enzyme systems, and drug interactions with macrolides and antifungal agents

T. Koudriakova, N. Gerber, Douglas F. Smith, 1997, Clinical pharmacology and therapeutics.

Metabolism of the human immunodeficiency virus protease inhibitors indinavir and ritonavir by human intestinal microsomes and expressed cytochrome P4503A4/3A5: mechanism-based inactivation of cytochrome P4503A by ritonavir.

P. Vouros, T. Koudriakova, N. Gerber, 1998, Drug metabolism and disposition: the biological fate of chemicals.

OF THE HUMAN IMMUNODEFICIENCY VIRUS PROTEASE INHIBITORS INDINAVIR AND RITONAVIR BY HUMAN INTESTINAL MICROSOMES AND EXPRESSED CYTOCHROME P 4503 A 4 / 3 A 5 : MECHANISM-BASED INACTIVATION OF CYTOCHROME P 4503 A BY RITONAVIR

P. Vouros, T. Koudriakova, N. Gerber, 1998 .

Ocular disposition, pharmacokinetics, efficacy and safety of nanoparticle-formulated ophthalmic drugs.

T. Koudriakova, H. Gukasyan, L. Goulet, 2007, Current drug metabolism.

Peripheral white blood cell toxicity induced by broad spectrum cyclin‐dependent kinase inhibitors

B. Jessen, C. Lewis, S. Price, 2007, Journal of applied toxicology : JAT.

The p53 codon 249 mutational hotspot in hepatocellular carcinoma is not related to selective formation or persistence of aflatoxin B1 adducts

A. Riggs, G. Pfeifer, M. Denissenko, 1998, Oncogene.

A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate.

C. Dvorak, N. Carruthers, A. Bhattacharya, 2018, Journal of medicinal chemistry.

Discovery of Imidazo[1,2-a]pyrazines and Pyrazolo[1,5-c]pyrimidines as TARP γ-8 Selective AMPAR Negative Modulators.

T. Lovenberg, N. Carruthers, B. Savall, 2018, ACS medicinal chemistry letters.

Lead Optimization of 5-Aryl Benzimidazolone- and Oxindole-Based AMPA Receptor Modulators Selective for TARP γ-8.

T. Lovenberg, N. Carruthers, B. Savall, 2018, ACS medicinal chemistry letters.

In vivo disposition and metabolism by liver and enterocyte microsomes of the antitubercular drug rifabutin in rats.

P. Vouros, T. Koudriakova, N. Gerber, 1996, The Journal of pharmacology and experimental therapeutics.

Quantitative Mass Spectrometry Imaging to Study Drug Distribution in the Intestine Following Oral Dosing.

Lennart R. S. Huizing, R. Heeren, R. Vreeken, 2021, Analytical chemistry.

Prediction of Oral Pharmacokinetics of cMet Kinase Inhibitors in Humans: Physiologically Based Pharmacokinetic Model Versus Traditional One-Compartment Model

Shinji Yamazaki, Hannah M Jones, Weiwei Tan, 2011, Drug Metabolism and Disposition.

AG-024322 is a multi-targeted CDK inhibitor with potent antitumor activity in vivo

Gennady M Verkhivker, D. Knighton, C. Lewis, 2005 .

Discovery of a Gut-Restricted JAK Inhibitor for the Treatment of Inflammatory Bowel Disease.

W. Chai, Jennifer D. Venable, J. Edwards, 2020, Journal of medicinal chemistry.

Pharmacokinetic-Pharmacodynamic Modeling of Biomarker Response and Tumor Growth Inhibition to an Orally Available cMet Kinase Inhibitor in Human Tumor Xenograft Mouse Models

Shinji Yamazaki, Bill J Smith, J. Christensen, 2008, Drug Metabolism and Disposition.

Design, Synthesis and Preclinical Evaluation of 3-Methyl-6-(5-thiophenyl)-1,3-dihydro-imidazo[4,5-b]pyridin-2-ones as Selective GluN2B Negative Allosteric Modulators for the Treatment of Mood Disorders.

T. Koudriakova, K. Coe, Xiaohui Jiang, 2020, Journal of medicinal chemistry.

1H-Pyrrolo[3,2-b]pyridine GluN2B-Selective Negative Allosteric Modulators.

N. Carruthers, T. Koudriakova, K. Coe, 2019, ACS medicinal chemistry letters.

Discovery of a Series of Substituted 1H-((1,2,3-Triazol-4-yl)methoxy)pyrimidines as Brain Penetrants and Potent GluN2B-Selective Negative Allosteric Modulators.

C. Dvorak, N. Carruthers, J. Alcázar, 2023, Journal of medicinal chemistry.

Identification of highly selective SIK1/2 inhibitors that modulate innate immune activation and suppress intestinal inflammation

Jennifer D. Venable, Thomas B. Sundberg, M. Rives, 2023, Proceedings of the National Academy of Sciences of the United States of America.