About 30% of patients with acute myeloid leukemia (AML) harbor mutations in the gene encoding receptor-type tyrosine-protein kinase FLT3 in the form of internal tandem duplication (ITD) or mutations in the tyrosine kinase domain.
Researchers from Epics Therapeutics SA presented preclinical data for EP-102, a novel small-molecule inhibitor of N6-adenosine-methyltransferase catalytic subunit (METTL3), being developed for the treatment of cancer.
Chimeric antigen receptor (CAR) therapies targeted against CD19 have been widely used for the treatment of B-cell malignancies. However, the down-regulation of CD19 can lead to relapse, and autologous CAR T therapies have limitations that need to be addressed.
Researchers from Hibercell Inc. recently presented preclinical data for HC-7366, a first-in-class direct activator of GCN2 (general control nonderepressible 2) currently in phase I development for the treatment of solid tumors (NCT05121948).
Researchers from Mbrace Therapeutics Inc. presented the discovery and preclinical evaluation of MBRC-101, a novel antibody-drug conjugate (ADC) targeting the membrane-associated tyrosine kinase receptor EphA5, being developed for the treatment of cancer.
Retinoic acid receptor-γ (RARγ) agonism is a key factor in CD8 T-cell-mediated immunity to infectious pathogens. The lack of studies on the effects of RARγ agonists on in vivo tumor growth of triple-negative (TNBC) or HER2+ breast cancers make it necessary to investigate whether RARγ could play a critical role in T-cell-mediated immunity in these breast cancers, using novel RARγ nuclear agonists.
HST-1021 is a novel mucosa-associated lymphoid tissue lymphoma translocation protein (MALT1) allosteric inhibitor identified using the Smart Allostery Platform, and is being developed for the potential treatment of tumors.
Nicotinamide phosphoribosyltransferase (NAmPRTase; Nampt) plays a central role in cancer metabolism as well as in metabolism in healthy tissues. Remedy Plan Therapeutics Inc. has presented data on the first hyperbolic Nampt inhibitor – RPT-1G – for the potential treatment of acute myeloid leukemia (AML).
PI3Kα H1047R accounts for one-third of all PI3Kα mutations and is associated with treatment resistance to targeted therapies in breast cancer treatment. In addition, treatment with selective PI3Kα inhibitors often results in significant adverse events such as hyperglycemia due to on-target toxicity.
Researchers from Bridgebio Pharma Inc. recently presented BBO-10203, a first-in-class, orally bioavailable, covalent small-molecule candidate designed to inhibit RAS-driven PI3Kα activity without affecting glucose metabolism.
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