Covalent Modifiers

MARCH 3, 2023

Calabrese Nat Commun 14 , 1189, 2023 [link] Targeted protein degradation using heterobifunctional chimeras holds the potential to expand target space and grow the druggable proteome. Bridging covalent ligand discovery with chimeric degrader design has emerged as a potential mechanism to advance both fields.

Targeted Protein Degradation 130

Targeted Protein Degradation Small Molecule 130

Drug Hunter

JULY 21, 2023

“compound 13” – A DCAF1 binder applied to targeted protein degradation, identified through high-throughput screening and optimization by Novartis. The post Molecules of the Month – June 2023 appeared first on Drug Hunter. Not a member? Request a trial to check out substructure search and more features.

Structure Based Drug Design (SBDD) 227

Structure Based Drug Design (SBDD) Targeted Protein Degradation Clinical Trials Trials 227

Drug Hunter

APRIL 23, 2023

BCCov “A covalent BTK ternary complex compatible with targeted protein degradation” Nat. log in: Username or E-mail Password Remember Me Forgot Password The post Drug Hunter Journal Club: March 2023 appeared first on Drug Hunter. Get ahead now by requesting a trial. already a member?

Targeted Protein Degradation 130

Targeted Protein Degradation Drugs Trials 130

Covalent Modifiers

OCTOBER 19, 2023

Nat Commun 14, 6345 ( 2023 ). link] The Src homology 2 (SH2) domain recognizes phosphotyrosine (pY) post translational modifications in partner proteins to trigger downstream signaling. Drug discovery efforts targeting the SH2 domains have long been stymied by the poor drug-like properties of phosphate and its mimetics.

Targeted Protein Degradation 208

Targeted Protein Degradation Drugs 208

Covalent Modifiers

FEBRUARY 16, 2024

Lynch, Ryan Casement, Andrea Testa, Elvira Bruno, Rosaria Gitto & Alessio Ciulli Nat Commun 14 , 6345 (2023). link] The Src homology 2 (SH2) domain recognizes phosphotyrosine (pY) post translational modifications in partner proteins to trigger downstream signaling.

Targeted Protein Degradation 189

Targeted Protein Degradation Drugs 189

Covalent Modifiers

OCTOBER 10, 2023

Ebert, Nathanael Gray bioRxiv 2023 [link] Small molecules that can induce protein degradation by inducing proximity between a desired target and an E3 ligase have the potential to greatly expand the number of proteins that can be manipulated pharmacologically. Groendyke, Jun Qi, Eric S Fischer, Benjamin L.

Targeted Protein Degradation 208

Targeted Protein Degradation Small Molecule 208

Drug Hunter

MAY 21, 2023

This article highlights six recent articles of interest in the field of targeted protein degradation including but not limited to potentially new ligases, recruiting motifs, and a discussion on the feasibility of CNS-penetrant degraders.

Targeted Protein Degradation 131

Targeted Protein Degradation Trials Therapies Disease 131