Structure-guided lead optimization at Merck & Co. Inc. has led to the discovery of MK-1084 as a highly potent and selective KRAS G12C-GDP inhibitor. As reported at the recent AACR-NCI-EORTC conference, the candidate demonstrated an excellent off-target and ion channel profile, with low potential for bile salt export pump (BSEP) inhibition.
Vividion Therapeutics Inc. has disclosed VVD-065, a novel, first-in-class, allosteric molecular glue of the KEAP1-CUL3 E3-ligase complex, for the potential treatment of NRF2-activated cancers. NRF2 (nuclear factor erythroid 2-related factor 2) is a significant mediator of antioxidant response.
Silo Pharma Inc. has announced promising data from a preclinical study investigating the binding affinity and optimization of SPU-21 liposomal joint homing peptide in human synovial tissue surrounding joints and tendons.
African Americans are 10 times more likely to develop chronic kidney disease (CKD) than Americans of European descent in part due to inheritance of one of two high-risk (HR) APOL1 variants (G1/G2, not G0) that are only present in people of West African or Caribbean ancestry. By contrast, these two APOL1 HR variants confer a beneficial resistance to otherwise lethal trypanosomiasis, which is caused by a pathogen endemic to West Africa, but still this ultimately results in a 4-fold increased risk for end-stage kidney disease (ESKD).
The mRNA technology used in vaccines against viral infections could also be developed for cancer therapies. A group of scientists has designed a circular RNA (circRNA) encapsulated in lipid nanoparticles (LNPs) that acts in the mitochondria of tumor cells through the protein gasdermin-D (GSDMD) and reduces adenocarcinoma. The work was published on Oct. 16, 2023, in Nature Cancer.
Additional early-stage research and drug discovery news in brief, from: Beyond Cancer, Biohaven, Corbus, Destiny, Myricx, Nextcure, Promontory, Storm, Venatorx.
Ideaya Biosciences Inc. has described piperazine substituted indazole compounds acting as poly(ADP-ribose) glycohydrolase (PARG) inhibitors reported to be useful for the treatment of cancer.
Autotelic Bio Inc. has divulged thiazole derivatives acting as TGF-β receptor type-1 (TGFBR1; ALK5; SKR4; TβR-I) inhibitors reported to be useful for the treatment of cancer.
A team at 1st Bio Therapeutics Inc. has identified indazoles acting as mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1; HPK1; MEKKK1) inhibitors reported to be useful for the treatment of cancer, autoimmune disease and inflammatory disorders.
Chengdu Easton Biopharmaceuticals Co. Ltd. has synthesized aminopyridine derivatives acting as CDK9/cyclin T1 inhibitors reported to be useful for the treatment of cancer.
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