Drug Target Review

JULY 6, 2023

TPD is a rapidly evolving therapeutic modality to degrade a disease-causing proteins, thereby eliminating their function specifically. 1 TPD is expected to challenge undruggable proteins, which are highly difficult to target by conventional small molecules. How does TPD work?

Targeted Protein Degradation 98

Targeted Protein Degradation Small Molecule Clinical Trials Science 98

Drug Hunter

JULY 21, 2023

With the popular success of diabetes and weight-loss peptide drugs from Novo (e.g. 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.

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. Drug Hunter Premium is drug discovery, distilled, so you can quickly catch up and make informed decisions based on industry examples. Get ahead now by requesting a trial. already a member?

Targeted Protein Degradation 130

Targeted Protein Degradation Drugs Trials 130

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

Covalent Modifiers

FEBRUARY 1, 2024

Therefore, understanding mechanisms by which acquired mutations in BTK confer drug resistance and developing new therapies to overcome resistance are critically important. 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.

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

Drug Hunter

AUGUST 21, 2023

Obtaining adequate drug exposure in the brain is key to treating CNS diseases effectively. Recently, Dennis Koester gave us a crash course in CNS drug discovery in a Drug Hunter Flash Talk. Why Kp,uu is the Most Important Parameter in CNS Drug Discovery What Influences the Kp,uu of Drugs?

Drugs 206

Drugs Disease Targeted Protein Degradation Screening Hits 206