Research at Incyte Corp. has led to the development of pyrazoloquinoline derivatives acting as GTPase KRAS (G12C mutant) inhibitors and reported to be useful for the treatment of cancer, inflammatory and immunological disorders.
Interleukin-13 (IL-13) receptor subunit α2 (IL13RA2), one of the two major receptors for IL-13 is overexpressed in glioblastoma multiforme and other solid tumors and is correlated with poor prognosis.
Hematopoietic progenitor kinase 1 (HPK1) is a serine/threonine kinase restricted to the hematopoietic compartment that plays a crucial role in cellular proliferation, apoptosis and modulation of the antitumor immune response. In mice, HPK1 deficiency is associated with enhanced immune response, and thus, HPK1 is considered a novel target for cancer immunotherapy.
Son of sevenless homolog 1 (SOS1) inhibitors have been detailed in a Shanghai Allist Pharmaceuticals Co. Ltd. patent and described as useful for the treatment of cancer, arteriovenous malformations, cardiofaciocutaneous syndrome, Costello syndrome, Legius syndrome (neurofibromatosis type 1-like syndrome), neurofibromatosis type 1, Noonan syndrome and Splenomegaly, among others.
Research at Boehringer Ingelheim Pharma GmbH & Co. KG has led to the development of proteolysis targeting chimeras (PROTACs) comprising a Von Hippel-Lindau E3 ubiquitin ligase (VHL)-binding moiety covalently linked to probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α) and/or transcription activator BRG1 (SMARCA4; BAF190A; SNF2-β) targeting moiety through a linker.
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