Obesity is a chronic disorder tied to other disorders such as hyperglycemia, type 2 diabetes or cardiovascular disease, among others. Recent findings have suggested that EphB tyrosine kinase receptor and its ligand, ephrin B, may be involved in insulin signaling.
Work at Escient Pharmaceuticals Inc. has led to the discovery of novel Mas-related G protein-coupled receptor member X4 (MRGPRX4) antagonists as potential therapeutic candidates for the treatment of cholestatic and uremic pruritus.
Shasqi Inc. recently reported the discovery of novel candidates using their proprietary Click Activated Protodrugs Against Cancer (CAPAC) platform, which aims to selectively activate high doses of cancer drugs directly at the tumor site. To achieve this, CAPAC consists of two separate components: a tumor-targeted activator and an inactivated payload.
DNA-encoded library (DEL) technology is a promising new tool for identifying ligands for challenging protein targets, allowing for the preparation and screening of large chemical libraries with significantly reduced time, costs and material requirements when compared to HIT-finding strategy.
Chiesi Farmaceutici SpA presented data for novel lung-targeted muscarinic M3 receptor antagonists/β2-adrenoceptor agonists (MABAs) as candidates for the treatment of chronic obstructive pulmonary disease (COPD).
Discovery of novel Nav1.8 inhibitors capable of achieving high levels of target modulation at low oral doses for the potential treatment of pain was reported by Merck & Co. Inc.
Hypoxia-inducible factor 2α (HIF-2α) is a transcription factor that plays a key role in oxygen homeostasis and response to tumor hypoxic microenvironment of cancer cells. Previous research has suggested that inhibition of HIF-2α is a promising antitumor approach, particularly against tumors associated with mutant von Hippel-Lindau (pVHL).
FmlH is a bacterial adhesin of uropathogenic E. coli (UPEC) that has been shown to be up-regulated during chronic UPEC infection. Washington University scientists recently disclosed the discovery and preclinical evaluation of novel FmlH lectin antagonists as potential candidates for the treatment of chronic urinary tract infections (UTIs) and kidney infections.
Blueprint Medicines Corp. recently disclosed the chemical structure of BLU-222, an oral, potent and highly selective inhibitor of the CDK2 kinase, being developed for the potential treatment of cancers with CCNE1 amplification and/or cyclin E overexpression, such as HR-positive HER2-negative breast cancer resistant to CDK4/6 inhibitor therapy.
Tango Therapeutics Inc. has disclosed the discovery of TNG-348, an orally active, potent, reversible allosteric inhibitor of the USP1 deubiquitinating enzyme.
