JeanMarie Lisnock

From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9

Whitney L. Petrilli, Gregory C. Adam, Roman S. Erdmann, Pravien Abeywickrema et autres

From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9

Whitney L. Petrilli, Gregory C. Adam, Roman S. Erdmann, Pravien Abeywickrema et autres

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From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9

Whitney L. Petrilli, Gregory C. Adam, Roman S. Erdmann, Pravien Abeywickrema et autres

Proprotein convertase substilisin-like/kexin type 9 (PCSK9) is a serine protease involved in a protein-protein interaction with the low-density lipoprotein (LDL) receptor that has both human genetic and clinical validation. Our pursuit of small molecule direct binders for this difficult to drug PPI …

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From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9

Whitney L. Petrilli, Gregory C. Adam, Roman S. Erdmann, Pravien Abeywickrema et autres

Proprotein convertase substilisin-like/kexin type 9 (PCSK9) is a serine protease involved in a protein-protein interaction with the low-density lipoprotein (LDL) receptor that has both human genetic and clinical validation. Our pursuit of small molecule direct binders for this difficult to drug PPI …

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Discovery of novel non-steroidal reverse indole mineralocorticoid receptor antagonists

Anthony K. Ogawa, Ellen Vande Bunte, Rudrajit Mal, Ping Lan et autres

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Discovery of Benzimidazole Oxazolidinediones as Novel and Selective Nonsteroidal Mineralocorticoid Receptor Antagonists

Christine Yang, Jaume Balsells, Hong D. Chu, Jason M. Cox et autres

Elaboration of the oxazolidinedione series led to replacement of the exocyclic amides with substituted benzimidazoles. The structure-activity relationship (SAR) exploration resulted in the discovery of potent and selective nonsteroidal mineralocorticoid receptor (MR) antagonists with significantly improved microsomal stability and pharmacokinetic (PK) profile …

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Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety

Shuwen He, Qingmei Hong, Zhong Lai, David Yang et autres

We report the discovery of a novel series of DGAT1 inhibitors in the benzimidazole class with a piperdinyl-oxy-cyclohexanecarboxylic acid moiety. This novel series possesses significantly improved selectivity against the A2A receptor, no ACAT1 off-target activity at 10 μM, and higher aqueous solubility …

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Pyrazoles as non-classical bioisosteres in prolylcarboxypeptidase (PrCP) inhibitors

Thomas H. Graham, Min Shu, Andreas Verras, Chen Qing et autres

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Mineralocorticoid receptor antagonists: Identification of heterocyclic amide replacements in the oxazolidinedione series

Jason M. Cox, Hong D. Chu, Christine Yang, Hong C. Shen et autres

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Discovery and optimization of orally active cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors

John S. Debenham, Thomas H. Graham, Andreas Verras, Yong Zhang et autres

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Potent DGAT1 Inhibitors in the Benzimidazole Class with a Pyridyl-oxy-cyclohexanecarboxylic Acid Moiety

Shuwen He, Qingmei Hong, Zhong Lai, Zhicai Wu et autres

We report the design and synthesis of a series of novel DGAT1 inhibitors in the benzimidazole class with a pyridyl-oxy-cyclohexanecarboxylic acid moiety. In particular, compound 11A is a potent DGAT1 inhibitor with excellent selectivity against ACAT1. Compound 11A significantly reduces triglyceride excursion …

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Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists

Christine Yang, Hong C. Shen, Zhicai Wu, Hong D. Chu et autres

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