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 small molecule could provide a new therapeutic approach against organ fibrosis. Using genome-wide association (GWA) assays, a group of researchers from the Westmead Institute for Medical Research in Sydney identified Mer tyrosine kinase (MERTK) as a candidate to study fibrosis and showed that its inhibition with the experimental compound reduced this condition in mouse models’ liver, kidneys and lungs. “There were some studies on the role of MERTK in liver fibrosis, but its therapeutic potential for various organ fibrosis has not been explored before. This study provides unequivocal evidence that MERTK is a potent nodal regulator of fibrosis supported by detailed mechanistic studies,” the senior author Mohammed Eslam told BioWorld.
Prelude Therapeutics Inc. has divulged proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to a probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α) and transcription activator BRG1 (SMARCA4; BAF190A; SNF2-β) targeting moiety. They are described as potentially useful for the treatment of cancer.
Jiangsu Hansoh Pharmaceutical Group Co. Ltd. and Shanghai Hansoh Biomedical Co. Ltd. have identified pyrimidine-containing polycyclic compounds acting as GTPase KRAS (G12D mutant) inhibitors reported to be useful for the treatment of cancer.
Cambridge Enterprise Ltd. has synthesized casein kinase II isoform α (CK2α) inhibitors reported to be useful for the treatment of cancer, viral infection, diabetes, ischemia, neurodegeneration, circadian rhythm disorders, vascular disorders and inflammatory disorders.
Gluetacs Therapeutics (Shanghai) Co. Ltd. has disclosed molecular glue degraders comprising cereblon (CRBN) ligands acting as DNA-binding protein Ikaros (IKZF1) or zinc finger protein Aiolos (IKZF3) degradation inducers reported to be useful for the treatment of cancer, autoimmune diseases, diabetes, infections, septic shock and more.
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.
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