Linda S. Barton

Exploration of the P1 residue in 3CL protease inhibitors leading to the discovery of a 2-tetrahydrofuran P1 replacement

Linda S. Barton, James F. Callahan, Juan Cantizani, N.O. Concha et autres

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Exploration of the P1 Residue in CL Protease Inhibitors Leading to the Discovery of a Novel 2-Tetrahydrofuran P1 Replacement

Linda S. Barton, James F. Callahan, Juan Cantizani, N.O. Concha et autres

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Discovery of Proline-Based p300/CBP Inhibitors Using DNA-Encoded Library Technology in Combination with High-Throughput Screening

Dominic Suarez, Douglas W. Thomson, William Li, Elizabeth A. King et autres

E1A binding protein (p300) and CREB binding protein (CBP) are two highly homologous and multidomain histone acetyltransferases. These two proteins are involved in many cellular processes by acting as coactivators of a large number of transcription factors. Dysregulation of p300/CBP has been …

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Discovery of GSK3527497: A Candidate for the Inhibition of Transient Receptor Potential Vanilloid-4 (TRPV4)

Carl Brooks, Linda S. Barton, David J. Behm, Edward J. Brnardic et autres

GSK3527497, a preclinical candidate for the inhibition of TRPV4, was identified starting from the previously reported pyrrolidine sulfonamide TRPV4 inhibitors 1 and 2 . Optimization of projected human dose was accomplished by specifically focusing on in vivo pharmacokinetic parameters CL u, Vdss …

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Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4)

Carl Brooks, Linda S. Barton, David J. Behm, Hilary S. Eidam et autres

GSK2798745, a clinical candidate, was identified as an inhibitor of the transient receptor potential vanilloid 4 (TRPV4) ion channel for the treatment of pulmonary edema associated with congestive heart failure. We discuss the lead optimization of this novel spirocarbamate series and specifically …

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Discovery of Pyrrolidine Sulfonamides as Selective and Orally Bioavailable Antagonists of Transient Receptor Potential Vanilloid-4 (TRPV4)

Edward J. Brnardic, Guosen Ye, Carl Brooks, Carla A. Donatelli et autres

A novel series of pyrrolidine sulfonamide transient receptor potential vanilloid-4 (TRPV4) antagonists was developed by modification of a previously reported TRPV4 inhibitor (1). Several core-structure modifications were identified that improved TRPV4 activity by increasing structural rigidity and reducing the entropic energy penalty …

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The development of an automated countercurrent chromatography process for isolation of anthocyanins

David J. Thornton, Linda S. Barton, Leo C. Hsu

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The discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophore

David G. Washburn, Dennis A. Holt, Jason W. Dodson, J. Jeffrey McAtee et autres

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Improving the developability profile of pyrrolidine progesterone receptor partial agonists

Lara S. Kallander, David G. Washburn, Tram H. Hoang, James S. Frazee et autres

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Orally bioavailable nonpeptide vitronectin receptor antagonists containing 2-aminopyridine arginine mimetics

Richard M. Keenan, William H. Miller, Linda S. Barton, William E. Bondinell et autres

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Potent, Selective, Orally Active 3-Oxo-1,4-benzodiazepine GPIIb/IIIa Integrin Antagonists

James M. Samanen, Fadia E. Ali, Linda S. Barton, William E. Bondinell et autres

ADVERTISEMENT RETURN TO ISSUELetterNEXTPotent, Selective, Orally Active 3-Oxo-1,4-benzodiazepine GPIIb/IIIa Integrin AntagonistsJames M. Samanen, Fadia E. Ali, Linda S. Barton, William E. Bondinell, Joelle L. Burgess, James F. Callahan, Raul R. Calvo, Wenting Chen, Lichong Chen, Karl Erhard, Giora Feuerstein, Richard Heys, Shing-Mei …

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Direct design of a potent non-peptide fibrinogen receptor antagonist based on the structure and conformation of a highly constrained cyclic RGD peptide

Thomas W. Ku, Fadia E. Ali, Linda S. Barton, John W. Bean et autres

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTDirect design of a potent non-peptide fibrinogen receptor antagonist based on the structure and conformation of a highly constrained cyclic RGD peptideThomas W. Ku, Fadia E. Ali, Linda S. Barton, John W. Bean, William E. Bondinell, Joelle L. Burgess, …