At last week’s American Chemical Society meeting, Novartis AG presented the discovery of IID-432, a highly efficacious and safe inhibitor of Trypanosoma cruzi topoisomerase 2 (Top2), offering a short-duration curative treatment for Chagas disease.
Small-cell lung cancer (SCLC) and some other cancers involve dysregulation of the transcription factor E2F, and apoptosis can be induced in those cells by blocking the interaction of the RxL sequence motif in E2F with cyclin A, which leads to hyperactivation of E2F. Researchers from Dana-Farber Cancer Institute and collaborators have developed macrocyclic peptides that inhibit this interaction and thereby hyperactivate E2F, leading to anticancer activity in various preclinical systems.
Despite having lower smoking habits than other groups in the U.S., Black Americans are more likely to develop lung cancer, and their survival rates are significantly worse. What explains this disparity? Scientists at Vanderbilt University Medical Center have analyzed the genetics of their African ancestry in search of risk genes related to the disease and tobacco use. The results reveal new risk factors and confirm the presence of genetic variants that may contribute to the greater impact of lung cancer in this population.
An investigation of the epidemiology and clinical characteristics of neuropathic pain in the UK Biobank has led to the discovery of a new pain gene and potential analgesic drug target in the peripheral nervous system. The gene, SLC45A4 (solute carrier 45A4), codes for a transporter that is involved in trafficking polyamines known to be involved in pain, across the cell membrane.
Podium Bio Ltd. has described compounds acting as apolipoprotein L1 (APOL1) inhibitors reported to be useful for the treatment of chronic kidney disease, focal segmental glomerulosclerosis, HIV-associated nephropathy, microalbuminuria, renal disorders and lupus nephritis.
Inventisbio Co. Ltd. and Inventisbio LLC have divulged Werner syndrome helicase (WRN; RECQ3; RECQL2) inhibitors reported to be useful for the treatment of cancer.
Jazz Pharmaceuticals Ireland Ltd. has identified compounds acting as GTPase KRAS and its mutant inhibitors reported to be useful for the treatment of cancer.
Insmed Inc. has synthesized cathepsin C (dipeptidyl peptidase I) inhibitors reported to be useful for the treatment of amyotrophic lateral sclerosis, asthma, cancer, chronic rhinosinusitis, heart failure, inflammatory bowel disease, psoriasis and thrombosis, among others.
Certa Therapeutics Pty Ltd. has disclosed ovarian cancer G-protein coupled receptor 1 (GPR68; OGR1) antagonists reported to be useful for the treatment of cancer, inflammation and fibrosis.