DXC-006 (Hangzhou DAC Biotechnology Co. Ltd.) is an antibody-drug conjugate (ADC) that targets CD56, a molecule involved in cell-cell adhesion and cell-matrix adhesion that is overexpressed in neuroblastoma, small-cell lung cancer and multiple myeloma, but less frequently expressed in normal tissues. DXC-006 consists of an anti-CD56 antibody (DXA-006) linked to the topoisomerase 1 (TOP1) inhibitor CPT-116 through a linker.
The discovery of a potent, selective and orally bioavailable serine/threonine-protein kinase PLK4 (STK18) inhibitor with synthetic lethality in TRIM7-amplified cancers was reported by Oric Pharmaceuticals Inc. at the ongoing AACR meeting in San Diego.
Researchers from Puhe Biopharma Co. Ltd. presented the discovery and preclinical evaluation of PH027-1, a novel small-molecule Werner syndrome protein (WRN) inhibitor targeting microsatellite instability high (MSI-H) tumors.
Myeloperoxidase-antineutrophil cytoplasmic antibody (MPO-ANCA)-associated vasculitis is a systemic condition affecting the small vessels with production of MPO-ANCA in serum. It has been suggested that the formation of neutrophil extracellular traps (NETs) induced by MPO-ANCA is a driver of pathogenesis, with involvement of neutrophil elastase (NE), which in turn is activated by the enzyme cathepsin C.
Prior to this year’s Annual Meeting of the American Association for Cancer Research (AACR), it had been 14 years since metastasis had been the subject of a plenary session. So, the Tuesday session on “Evolution of the genome, microenvironment, and host through metastasis” had plenty of new insights to share.
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).