Sunesis Pharmaceuticals, Inc.

Millennium Pharmaceuticals Limited

Carmot Therapeutics, Inc.

Cannot Therapeutics, Inc.

Biogen Idec Ma Inc.

Stig Hansen

Daniel A Erlanson

Kevin Guckian

Wen-Cherng Lee

Edward Yin-Shiang Lin

Lei Zhang

Lihong Sun

Thinh Nguyen

Robert Lowell Simmons

Kathy Jingyuan Cao

Raymond V Fucini

Shyam Krishnan

Steven Sethofer

Kenneth Egnard Lind

Bradley T Tangonan

Nuzhat Pathan

Robert S McDowell

Kenneth Jay Barr

Christian Wiesmann

Bruce Fahr

Dan Erlanson

Johan Enquist

Suman Atwal

Mark Cancilla

Andrew Sawayama

Jeff Iwig

Enrique Moya

Daniel Erlanson

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt) that modulate (e.g., agonize or partially agonize or antagonize) glucagon-like peptide-1 receptor ('GLP-1R') and/or the gastric inhibitory polypeptide receptor (“GIPR”). The chemical entities are useful, e.g., for treating a disease, disorder, or condition in which modulation (e.g., agonism, partial agonism or antagonism) of GLP-1R and/or GIPR activities is beneficial for the treatment or prevention of the underlying pathology and/or symptoms and/or progression of the disease, disorder, or condition. In some embodiments, modulation results in enhancement of (e.g., increases) existing levels (e.g., normal or below normal levels) of GLP-1R and/or GIPR activity (e.g., signaling). In some embodiments, the chemical entities described herein further modulate (e.g., attenuate, uncouple) β-arrestin signaling relative to what is observed with the native ligand. This disclosure also features compositions as well as other methods of using and making the said chemical entities.

Modulators of G-protein coupled receptors

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt and/or hydrate and/or prodrug of the compound) that modulate (e.g., agonize or partially agonize or antagonize) glucagon?like peptide?1 receptor ('GLP?1R') and/or the gastric inhibitory polypeptide receptor ('GIPR'). The chemical entities are useful, e.g., for treating a subject (e.g., a human) having a disease, disorder, or condition in which modulation (e.g., agonism, partial agonism or antagonism) of GLP?1R and/or GIPR activities is beneficial for the treatment or prevention of the underlying pathology and/or symptoms and/or progression of the disease, disorder, or condition. In some embodiments, the modulation results in an enhancement of (e.g., an increase in) existing levels (e.g., normal or below normal levels) of GLP?1R and/or GIPR activity (e.g., signaling). In some embodiments, the chemical entities described herein further modulate (e.g., attenuate, uncouple)-arrestin signaling relative to what is observed with the native ligand. This disclosure also features compositions as well as other methods of using and making the said chemical entities.

Herein is described a method to rapidly screen a large chemical space for a compound that binds to a target protein through an iterative fragment assembly approach that can be performed at low reagent cost and without requiring purification of the assembled product. The method employs a library of test ligands each of which comprise a 'bait' molecule, which is known from prior art or prior screening to have some intrinsic affinity for the target protein, and a test moiety.

Methods of chemotype evolution

The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.

Methods of treatment using pyridinonyl PDK1 inhibitors

Pyridinonyl PDK1 inhibitors

The present invention relates to methods for identifying compounds that modulate enzymatic activity by contacting covalently bonded PTP-extender complexes or modified covalently bonded PTP-extender complexes with ligand candidates.

Methods for identifying compounds that modulate enzymatic activities by employing covalently bonded target-extender complexes with ligand candidates

The present invention relates to a new and improved method for treating diabetes and or its associated complications by modulating the activity of protein tryosin phosphatase 1B (&ldquo;PTP-1B&rdquo;). The inventive compounds modulate the activity PTP-1B by binding to a novel binding site referred herein as the PTP-1B exosite that is distal to the active site of PTP-1B. The present invention also relates to a new and improved method of treating immune system disorders by modulating the activity of T-cell protein tyrosine phosphatase (&ldquo;TC-PTP&rdquo;). The inventive compound modulate the activity of TC-PTP by binding to a novel binding site referred herein as the TC-PTP exosite that is distal to the active site of PTP-1B.

Compounds that modulate the activity of PTP-1B and TC-PTP

Growing community of inventors

Kensington, CA, United States of America

Stig Hansen