D. S. Weinstein

发表

Autoimmune pathways in mice and humans are blocked by pharmacological stabilization of the TYK2 pseudokinase domain

K. McIntyre, C. Chaudhry, L. Salter-Cid, 2019, Science Translational Medicine.

DCAF11 Supports Targeted Protein Degradation by Electrophilic Proteolysis-Targeting Chimeras.

B. Cravatt, T. Wucherpfennig, M. Dix, 2021, Journal of the American Chemical Society.

CRYSTAL STRUCTURE OF TYROSINE KINASE 2 JH2 (PSEUDO KINASE DOMAIN) COMPLEXED WITH Compound_5 AKA 4-[(2-CARBAMOYLPHEN YL)AMINO]-6-[(5-FLUOROPYRIDIN-2-YL)AMINO]-N-METHYLPYRIDINE -3-CARBOXAMIDE

S. Spergel, K. McIntyre, J. Tokarski, 2019 .

Development of a Practical Synthesis of Functionalized Azaxanthene-Derived Nonsteroidal Glucocorticoid Receptor Modulators

Thomas M. Razler, D. Conlon, Steven A. Tymonko, 2016 .

Improving the pharmacokinetic and CYP inhibition profiles of azaxanthene-based glucocorticoid receptor modulators-identification of (S)-5-(2-(9-fluoro-2-(4-(2-hydroxypropan-2-yl)phenyl)-5H-chromeno[2,3-b]pyridin-5-yl)-2-methylpropanamido)-N-(tetrahydro-2H-pyran-4-yl)-1,3,4-thiadiazole-2-carboxamide

Michael G. Yang, Michael A. Galella, K. McIntyre, 2015, Journal of medicinal chemistry.

Azaxanthene based selective glucocorticoid receptor modulators: design, synthesis, and pharmacological evaluation of (S)-4-(5-(1-((1,3,4-thiadiazol-2-yl)amino)-2-methyl-1-oxopropan-2-yl)-5H-chromeno[2,3-b]pyridin-2-yl)-2-fluoro-N,N-dimethylbenzamide (BMS-776532) and its methylene homologue (BMS-7918

A. Doweyko, D. Shuster, J. Barrish, 2011, Journal of medicinal chemistry.

Discovery of novel dihydro-9,10-ethano-anthracene carboxamides as glucocorticoid receptor modulators.

A. Doweyko, J. Barrish, T. Huynh, 2009, Bioorganic & medicinal chemistry letters.

Aminoimidazoles as bioisosteres of acylguanidines: novel, potent, selective and orally bioavailable inhibitors of the sodium hydrogen exchanger isoform-1.

M. Kirby, Saleem Ahmad, G. Chandrasena, 2004, Bioorganic & medicinal chemistry letters.

Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists.

Michael G. Yang, A. Doweyko, D. Shuster, 2014, Bioorganic & medicinal chemistry letters.

Tryptamine and homotryptamine-based sulfonamides as potent and selective inhibitors of 15-lipoxygenase.

J. Macor, N. Murugesan, Z. Gu, 2005, Bioorganic & medicinal chemistry letters.

Identification of imidazo[1,2-b]pyridazine TYK2 pseudokinase ligands as potent and selective allosteric inhibitors of TYK2 signalling.

J. Tokarski, D. Xie, N. Araníbar, 2017, MedChemComm.

Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.

S. Spergel, K. McIntyre, D. Shuster, 2019, Journal of medicinal chemistry.

Identification of Imidazo[1,2-b]pyridazine Derivatives as Potent, Selective, and Orally Active Tyk2 JH2 Inhibitors.

James Lin, K. McIntyre, J. Tokarski, 2019, ACS medicinal chemistry letters.

Synthesis of the namenamicin A–C disaccharide: towards the total synthesis of namenamicin

K. Nicolaou, D. S. Weinstein, 1999 .

Discovery of selective imidazole-based inhibitors of mammalian 15-lipoxygenase: highly potent against human enzyme within a cellular environment.

C. S. Madsen, Shaobin Zhuang, J. Robl, 2007, Bioorganic & medicinal chemistry letters.

Novel two-step, one-pot synthesis of primary acylureas

Michael A. Galella, A. Tebben, D. S. Weinstein, 2010 .

Dimethyl-diphenyl-propanamide derivatives as nonsteroidal dissociated glucocorticoid receptor agonists.

A. Doweyko, D. Shuster, J. Barrish, 2010, Journal of medicinal chemistry.

Tyrosine Kinase 2-mediated Signal Transduction in T Lymphocytes Is Blocked by Pharmacological Stabilization of Its Pseudokinase Domain*

Stephen R. Johnson, M. Witmer, J. Tokarski, 2015, The Journal of Biological Chemistry.

Pulmonary sarcoidosis: calcified micronodular pattern simulating pulmonary alveolar microlithiasis.

D. S. Weinstein, D. S. Weinstein, 1999, Journal of thoracic imaging.

The chemical end-ligation of homopyrimidine oligodeoxyribonucleotides within a DNA triple helix.

K. Nicolaou, T. Li, D. S. Weinstein, 1997, Chemistry & biology.

Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2.

James Lin, K. McIntyre, D. Shuster, 2020, Journal of medicinal chemistry.

Advances in the Discovery and Development of Selective Tyrosine Kinase 2 (TK2) Inhibitors

D. S. Weinstein, M. MoslinRyan, 2018, 2018 Medicinal Chemistry Reviews.

Pyrazole-based sulfonamide and sulfamides as potent inhibitors of mammalian 15-lipoxygenase.

Saleem Ahmad, C. S. Madsen, Xing Chen, 2011, Bioorganic & medicinal chemistry letters.

Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.

Michael A. Galella, D. Shen, J. Barrish, 2018, Bioorganic & medicinal chemistry letters.