Drug Target Review

JULY 6, 2023

Unlike traditional drug discovery, which focuses on inhibiting or activating proteins, TPD offers a more precise and efficient way to alter cellular pathways. 1 The concept of TPD was first demonstrated with a heterobifunctional small molecule to degrader a protein of interest in the early 2000s. How does TPD work? Nature News.

Targeted Protein Degradation 98

Targeted Protein Degradation Small Molecule Clinical Trials Science 98

Drug Hunter

JULY 21, 2023

danuglipron – An oral GLP-1-RA full agonist in Phase IIb clinical trials for obesity and Phase II trials for type 2 diabetes mellitus, identified through sensitized cell high-throughput screening and optimization, originated from Pfizer. Request a trial to check out substructure search and more features. Not a member?

Structure Based Drug Design (SBDD) 227

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

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. Get ahead now by requesting a trial. already a member?

Targeted Protein Degradation 131

Targeted Protein Degradation Trials Therapies Disease 131

Drug Hunter

APRIL 23, 2023

BCCov “A covalent BTK ternary complex compatible with targeted protein degradation” Nat. Get ahead now by requesting a trial. Drug Hunter Premium is drug discovery, distilled, so you can quickly catch up and make informed decisions based on industry examples. already a member?

Targeted Protein Degradation 130

Targeted Protein Degradation Drugs Trials 130

Covalent Modifiers

FEBRUARY 1, 2024

We therefore set out to understand the nonenzymatic functions of BTK and explored targeted protein degradation to overcome the oncogenic scaffold function of mutant BTK. RESULTS BTK enzymatic activity assays revealed that drug resistance mutations in BTK fall into two distinct groups: kinase proficient and kinase impaired.

Targeted Protein Degradation 173

Targeted Protein Degradation Clinical Trials Trials Science 173

Drug Hunter

JUNE 25, 2023

This edition includes Maze’s glycogen synthase 1 (GYS1) inhibitors that were recently licensed to Sanofi, allosteric androgen receptor (AR) modulators that may be of interest to targeted protein degradation researchers, and brain-penetrant HER2 and ROCK2 inhibitors. Get ahead now by requesting a trial. already a member?

Targeted Protein Degradation 130

Targeted Protein Degradation Computational Chemistry Trials Licensing 130

The Pharma Data

JULY 22, 2021

(NYSE: PFE) today announced a global collaboration to develop and commercialize ARV-471, an investigational oral PROTAC® (PROteolysis TArgeting Chimera) estrogen receptor protein degrader. The estrogen receptor is a well-known disease driver in most breast cancers. Chief Executive Officer at Arvinas.

Targeted Protein Degradation 52

Targeted Protein Degradation Therapies Clinical Trials Treatment 52