Knowledge Library
WuXi Discovery Services Newsletter: February 2021
Protein Degradation: Shifting the Paradigm of Resistance and Undruggables for Unmet Medical Needs in Cancer, Neuroscience, and Beyond
INNOVATION THAT MATTERS By Rich Soll, Senior Advisor, Strategic Initiatives at WuXi AppTec (@richsollwx) With a recent $120 million IPO, a $55 million Series C, and a Pfizer R&D deal potentially worth $830 million, Arvinas is poised to transform the “undruggable” landscape, giving patients and healthcare providers new hope. Arvinas is doing this by developing a new …Read More >
Enabling Technology for Targeted Protein Degradation
Summary Traditional small molecule therapeutic mechanisms have recently been augmented by a new strategy to specifically manipulate the levels of disease-related proteins. By employing bifunctional molecules, we can hijack endogenous cellular degradation mechanism for targeted degradation of a disease-related protein. Bifunctional molecules consisting of a ligand that binds to an E3 ligase, connected by a …Read More >
Bifunctional Molecules: A Diverse New Modality That Unlocks New Target Classes
Targeted Protein Degradation Platform PROTAC
PROTAC BIOLOGY & PHARMACOLOGY BINARY/TERNARY COMPLEX FORMATION Biochemical & Biophysical Assays Biochemical binding assay Cellular Assays TARGET UBIQUITINATION & DEGRADATION In vitro Assays-Target ubiquitination Target degradation assay PK/PD Animal Disease Model Evaluation PROTAC CHEMISTRY PROTAC specific virtual library design Compound synthesis Conjugation and all type of custom syntheses from milligram to kilogram scale Purification and …Read More >
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