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.
M-9140 (Merck KGaA) is an antibody-drug conjugate (ADC) that carries a DNA topoisomerase 1 (TOP1) inhibitor payload plus an antibody directed against carcinoembryonic antigen-related cell adhesion molecule 5 (CEACAM5). CEACAM5 is a cell surface protein that is overexpressed in colorectal cancer and other solid tumors.
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.
ABM Therapeutics Inc. presented a novel small-molecule, ATP-uncompetitive, phosphorylated MEK (pMEK) inhibitor – ABM-4095 – that potently prevents phosphorylation of MEK by RAF with moderate inhibition of MEK kinase activity; it is being investigated for the potential treatment of pancreatic cancer.
At the AACR meeting, Innovent Biologics Inc. discussed the discovery and preclinical evaluation of a B7-H3/EGFR bispecific antibody-drug conjugate (bsADC).
The formation of neutrophil extracellular traps (NETs) is a common feature in the renal glomeruli of patients with antineutrophil cytoplasmic autoantibody (ANCA) vasculitis. The use of a DNA repair antibody, such as PAT-DX-1 from Patrys Ltd., could inhibit NET formation by interfering with DNA damage responses in the neutrophil, which lead to the release of DNA.
“A biotech company cannot survive on ‘drug efficacy’ alone,” former Korea Drug Development Fund (KDDF) CEO Hyunsong Muk said recently, “because novel drug development is not just a scientific problem.” Financial toxicity is, in fact, a major obstacle for biotech companies trying to advance preclinical candidates to early stage clinical trials, Muk said at Novo Nordisk A/S’ Partnering Day and Symposium on April 4 in Seoul, South Korea.
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.
Pfizer Inc. has presented preclinical data on its first-in-class, selective cyclin-dependent kinase 4 (CDK4) inhibitor compound, PF-07220060, that has shown 20-fold and 4-fold increased selectivity for CDK4 vs. CDK6 compared to palbociclib and abemaciclib/ribociclib, respectively.