K. McClure

发表

From partial to full agonism: identification of a novel 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole as a full agonist of the human GPR119 receptor.

Michael D. Hamilton, S. Wright, A. Kalgutkar, 2013, Bioorganic & medicinal chemistry letters.

Activation of the G-protein-coupled receptor 119: a conformation-based hypothesis for understanding agonist response.

A. Kalgutkar, M. Munchhof, B. Lefker, 2011, Journal of medicinal chemistry.

Oxidative metabolism of a quinoxaline derivative by xanthine oxidase in rodent plasma.

G. S. Walker, A. Stepan, A. Kalgutkar, 2011, Chemical research in toxicology.

Chapter 15. Emerging opportunities for the treatment of inflammatory bowel disease

N. Pullen, J. Gale, K. McClure, 2003 .

Biochemical basis for differences in metabolism-dependent genotoxicity by two diazinylpiperazine-based 5-HT2C receptor agonists.

J. Bauman, A. Kalgutkar, J. Aubrecht, 2009, Bioorganic & medicinal chemistry letters.

Genotoxicity of 2-(3-Chlorobenzyloxy)-6-(piperazinyl)pyrazine, a Novel 5-Hydroxytryptamine2c Receptor Agonist for the Treatment of Obesity: Role of Metabolic Activation

A. Kalgutkar, T. Maurer, J. Aubrecht, 2007, Drug Metabolism And Disposition.

Design, Synthesis, and Pharmacology of Fluorescently Labeled Analogs of Serotonin: Application to Screening of the 5-HT2C Receptor

J. Boyd, Janice A. Brown, Wen-Kuang Lin, 2009, Journal of biomolecular screening.

Structure-function relationships of the soluble form of the antiaging protein Klotho have therapeutic implications for managing kidney disease

James R. Apgar, R. Kriz, X. Zhong, 2020, The Journal of Biological Chemistry.

Preclinical pharmacokinetics and metabolism of 6‐(4‐(2,5‐difluorophenyl)oxazol‐5‐yl)‐3‐isopropyl‐[1,2,4]‐triazolo[4,3‐a]pyridine, a novel and selective p38α inhibitor: identification of an active metabolite in preclinical species and human liver microsomes

A. Kalgutkar, E. Choo, K. McClure, 2006, Biopharmaceutics & drug disposition.

Experimental Myocardial Infarction in Mice Matrix Metalloproteinase Inhibition Attenuates Early Left Ventricular Enlargement After

Richard T. Lee, P. Libby, A. Ducharme, 1999 .

Design and synthesis of truncated EGF-A peptides that restore LDL-R recycling in the presence of PCSK9 in vitro.

M. Ammirati, D. Craik, David A. Price, 2014, Chemistry & biology.

Pharmacological characterization of the first in class clinical candidate PF‐05190457: a selective ghrelin receptor competitive antagonist with inverse agonism that increases vagal afferent firing and glucose‐dependent insulin secretion ex vivo

P. Loria, S. V. Straub, S. Bhattacharya, 2016, British journal of pharmacology.

Discovery of N-(piperidin-3-yl)-N-(pyridin-2-yl)piperidine/piperazine-1-carboxamides as small molecule inhibitors of PCSK9.

P. Loria, C. Limberakis, D. W. Piotrowski, 2018, Bioorganic & medicinal chemistry letters.

Small Molecule Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors: Hit to Lead Optimization of Systemic Agents.

Jeffrey R. Chabot, J. Cate, J. Warmus, 2018, Journal of medicinal chemistry.

Structure-activity relationships of triazolopyridine oxazole p38 inhibitors: identification of candidates for clinical development.

F. Lombardo, A. Kalgutkar, E. Laird, 2006, Bioorganic & medicinal chemistry letters.

Mechanism of Stabilization of Helical Conformations of Polypeptides by Water Containing Trifluoroethanol

D. Kemp, Sherri L. Oslick, ARTHUR CAMMERS, 1996 .

Liver-Targeted Small-Molecule Inhibitors of Proprotein Convertase Subtilisin/Kexin Type 9 Synthesis.

Jeffrey R. Chabot, P. Loria, C. Halldin, 2017, Angewandte Chemie.

Pyran-containing sulfonamide hydroxamic acids: potent MMP inhibitors that spare MMP-1.

I. Otterness, R. Robinson, J. Liras, 2004, Bioorganic & medicinal chemistry letters.

A novel Heck arylation reaction: rapid access to congeners of FR 900482

S. Danishefsky, K. McClure, 1993 .

A strategy for the solid-phase synthesis of oligosaccharides.

J. Randolph, S. Danishefsky, K. McClure, 1993, Science.

Design and synthesis of diazatricyclodecane agonists of the G-protein-coupled receptor 119.

Bryan M. Li, David A. Price, A. Kalgutkar, 2013, Journal of medicinal chemistry.

Daphniphyllum alkaloids. 15. Total syntheses of (.+-.)-methyl homodaphniphyllate and (.+-.)-daphnilactone A

C. Heathcock, K. McClure, R. Ruggeri, 1992 .

Daphniphyllum alkaloids. Part 5. Total synthesis of (.+-.)-daphnilactone A: a novel fragmentation reaction

C. Heathcock, K. McClure, R. Ruggeri, 1989 .

Theoretical and experimental design of atypical kinase inhibitors: application to p38 MAP kinase.

Dennis E Danley, P. Lemotte, M. Mansour, 2005, Journal of medicinal chemistry.

An Improved Synthesis of a Template for .alpha.-Helix Formation

D. Kemp, K. McClure, P. Renold, 1995 .

An efficient synthesis of bridged heterocycles from an Ir(I) bis-amination/ring-closing metathesis sequence.

Spiros Liras, Cristiano R W Guimarães, S. Liras, 2012, Organic letters.

Evaluation and synthesis of polar aryl- and heteroaryl spiroazetidine-piperidine acetamides as ghrelin inverse agonists.

P. Loria, D. Hepworth, S. Bhattacharya, 2015, ACS Medicinal Chemistry Letters.

Enantioselective hydroarylation of bridged [3.2.1] heterocycles: an efficient entry into the homoepibatidine skeleton.

S. Liras, R. A. Brawn, K. McClure, 2013, Organic letters.

Synthesis of spirofuranopyrimidine–piperidines

Vincent Mascitti, K. McClure, Etzer Darout, 2012 .

Cycloaddition reactions of aromatic nitroso compounds with oxygenated dienes. An approach to the synthesis of the FR-900482 family of antibiotics

S. Danishefsky, K. McClure, 1991 .

Intramolecular cycloaddition reactions of dienyl nitroso compounds: application to the synthesis of mitomycin K

S. Danishefsky, K. McClure, J. Benbow, 1993 .

A remarkable stereochemical inversion in some Heck arylation reactions. A mechanistic proposal

G. Schulte, S. Danishefsky, K. McClure, 1994 .

Synthesis and biological activity of selective pipecolic acid-based TNF-alpha converting enzyme (TACE) inhibitors.

Dennis E Danley, D. Danley, G. Schulte, 2002, Bioorganic & medicinal chemistry letters.

Major Simplifications in Oligosaccharide Syntheses Arising from a Solid-Phase Based Method: An Application to the Synthesis of the Lewis b Antigen

J. Randolph, S. Danishefsky, K. McClure, 1995 .

PF-07059013: A Noncovalent Modulator of Hemoglobin for Treatment of Sickle Cell Disease.

Roger M. Howard, S. Liras, K. Beaumont, 2020, Journal of medicinal chemistry.

A Novel Heck Arylation Reaction: Rapid Access to Congeners of FR 900482.

S. Danishefsky, K. McClure, 1993 .

Role of p38 MAPK in UVB-induced inflammatory responses in the skin of SKH-1 hairless mice.

C. Gabel, Xiuwei Tang, Yucui Zhu, 2005, The Journal of investigative dermatology.

Structural basis for selective stalling of human ribosome nascent chain complexes by a drug-like molecule

J. Cate, S. Liras, Wenfei Li, 2018, bioRxiv.

Selective stalling of human translation through small-molecule engagement of the ribosome nascent chain

J. Doudna, J. Cate, P. Loria, 2017, PLoS biology.

A compound that directly and selectively stalls PCSK9 translation

J. Doudna, J. Cate, P. Loria, 2016, bioRxiv.

Title : A compound that directly and selectively stalls PCSK 9 translation 1 2

J. Cate, P. Loria, S. Liras, 2016 .

Benzimidazolone p38 inhibitors.

C. Gabel, T. Carty, John T Barberia, 2004, Bioorganic & medicinal chemistry letters.

Continued exploration of the triazolopyridine scaffold as a platform for p38 MAP kinase inhibition.

L. Xing, S. Selness, H. Shieh, 2010, Bioorganic & medicinal chemistry letters.

Matrix metalloproteinase inhibition attenuates early left ventricular enlargement after experimental myocardial infarction in mice.

P. Libby, A. Ducharme, G. Sukhova, 1999, Circulation.

Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor.

L. Michael, T. Goosen, M. Tu, 2013, Bioorganic & medicinal chemistry letters.

Permeability of Cyclic Peptide Macrocycles and Cyclotides and Their Potential as Therapeutics.

S. Liras, K. McClure, 2019, ACS medicinal chemistry letters.

Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate.

P. Loria, D. Hepworth, S. Bhattacharya, 2014, ACS medicinal chemistry letters.

Receptor-Mediated Delivery of CRISPR-Cas9 Endonuclease for Cell-Type-Specific Gene Editing.

Kaihong Zhou, Spiros Liras, Meihua Tu, 2018, Journal of the American Chemical Society.

Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor.

Z. Hendsch, B. Posner, D. Kung, 2012, Bioorganic & medicinal chemistry letters.

Design and evaluation of a 2-(2,3,6-trifluorophenyl)acetamide derivative as an agonist of the GPR119 receptor.

A. Kalgutkar, K. Farley, M. Munchhof, 2011, Bioorganic & Medicinal Chemistry Letters.

Modulateurs de gpr 119

Vincent Mascitti, K. McClure, Etzer Darout, 2012 .

Structural basis for selective stalling of human ribosome nascent chain complexes by a drug-like molecule

J. Cate, S. Liras, Wenfei Li, 2019, Nature Structural & Molecular Biology.

Pyran-containing sulfonamide hydroxamic acids: potent MMP inhibitors that spare MMP-1.

I. Otterness, R. Robinson, J. Liras, 2004, Bioorganic & medicinal chemistry letters.

Intrinsic electrophilicity of a 4-substituted-5-cyano-6-(2-methylpyridin-3-yloxy)pyrimidine derivative: structural characterization of glutathione conjugates in vitro.

A. Kalgutkar, M. Munchhof, R. Robinson, 2011, Chemical research in toxicology.

Spiroazetidine–piperidine bromoindane as a key modular template to access a variety of compounds via C–C and C–N bond-forming reactions

S. Bhattacharya, K. McClure, Wenhua Jiao, 2012 .

Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor.

Z. Hendsch, B. Posner, D. Kung, 2012, Bioorganic & medicinal chemistry letters.