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.

Structure Based Drug Design (SBDD) 227

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

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

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

The Pharma Data

DECEMBER 15, 2020

Nasdaq: ARVN), a clinical-stage biotechnology company creating a new class of drugs based on targeted protein degradation using its PROTAC ® Discovery Engine, today announced the pricing of an underwritten public offering of 5,714,286 shares of its common stock at a price of $70.00 NEW HAVEN, Conn.,

Targeted Protein Degradation 40

Targeted Protein Degradation Engineering Clinical Trials Disease 40

Drug Hunter

AUGUST 21, 2023

Overall, only a few prodrugs for CNS disorders have even reached clinical trials , so for the most part traditional property-based drug design remains the best bet for the vast majority of programs. What is K p,uu ? Figure 18. A) Progression of a Novartis HAT program from a screening hit to brain-penetrant leads.

Drugs 206

Drugs Disease Targeted Protein Degradation Screening Hits 206