Boehringer Ingelheim Pharma GmbH & Co. KG and Vanderbilt University have synthesized annulated 2-amino-3-cyano thiophenes and derivatives acting as KRAS GTPase and its mutant inhibitors reported to be useful for the treatment of cancer.
Jiangsu Simcere Pharmaceutical R&D Co. Ltd. has described 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) targeting moiety reported to be useful for the treatment of cancer.
TYK Medicines Inc. has synthesized proteolysis targeting chimera (PROTAC) compounds comprising cereblon (CRBN) binding moieties covalently linked to EGFR (HER1; erbB1) binding moieties reported to be useful for the treatment of cancer, infections, cardiovascular, immunological, inflammatory and metabolic diseases.
Creo Medical Group plc says it is poised to address the mismatch between the advances in screening technology, which are making it possible to detect early-stage lung cancer, and the current invasive and inappropriate methods of treating it, following the first-in-human use of its Microblate Flex microwave ablation device.
With age, senescent cells become detrimental to tissues. Mayo Clinic scientists have observed this phenomenon in the lung alveoli, where senescent macrophages accumulated in aging tissue and in early stages of non-small-cell lung cancer (NSCLC) driven by the Kras oncogene. “We found that the macrophages were present in the earliest stages of the disease. Strategies targeting these cells for elimination or preventing their accumulation would be worthwhile to test in other conditions (assuming we find they occur),” Darren Baker, a Mayo Clinic senescent cell biologist and senior author of the study, told BioWorld.
Ranok Therapeutics (Hangzhou) Co. Ltd. has divulged proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase binding moiety covalently coupled to a GTPase KRAS (G12D mutant) targeting moiety through a linker reported to be useful for the treatment of cancer.
It was previously shown that AXL overexpression is associated with poor prognosis, metastasis, as well as drug resistance in various hematological and solid tumors, and that inhibition of AXL phosphorylation could overcome drug resistance to FLT3 inhibitors. CTS-2016 is an AXL/FLT3 inhibitor being developed by Cytosinlab Therapeutics Co. Ltd. as a novel tyrosine kinase inhibitor for cancer.