Researchers at 1200 Pharma LLC have undertaken preclinical analysis of KRAS G12C inhibitors in clinical phases with the aim of finding an explanation for the differences observed in therapeutic efficacy in tumor sites other than lung, including lung-derived metastases. Results pointed to potency and pharmacokinetics as key drivers of efficacy.
At the recently concluded AACR meeting, Biocytogen Pharmaceuticals (Beijing) Co. Ltd. discussed BSA-01, a bispecific antibody-drug conjugate (ADC) targeting both epidermal growth factor receptor (EGFR) and mucin-1 (MUC-1), two tumor-associated antigens that are highly co-expressed in several cancers.
Researchers from Oncovalent Therapeutics Inc. recently provided details on the discovery and preclinical evaluation of SB-4826, a first-in-class oral, covalent small-molecule inhibitor of the SUMO activating enzyme (SUMO E1), the initiating enzyme of the sumoylation cascade. Sumoylation is involved in diverse cell processes such as inflammation, DNA damage response, signaling and cell survival/apoptosis, and it has also emerged as a novel target for activating antitumor immunity due to its role in regulating type I interferon (IFN) signaling.
Researchers from Regor Therapeutics Inc. presented data from the company’s discovery campaign of Son of sevenless homolog 1 (SOS1) inhibitors, which show potential for the treatment of mutated KRAS-positive cancers, such as pancreatic cancers (PAC) and non-small-cell lung cancer (NSCLC). SOS1 is an upstream activator of KRAS. Therefore, SOS1 blockage has great potential as an approach for pan mutant KRAS suppression.
Checkpoint kinase 1 (CHK1) is involved in cell cycle arrest by activation of DNA damage response pathways. The aim of researchers from Shanghai Fosun Pharmaceutical (Group) Co. Ltd. was to develop a potent oral CHK1 inhibitor, XS-02, for the treatment of solid tumors.
Among over 100 members of the PTP family, protein-tyrosine phosphatase 1B (PTP-1B) and T-cell protein-tyrosine phosphatase (PTPN2, TCPTP) have the most closely related homology (72%), sharing identical catalytic subunits. Significantly, together they serve nonredundant functions suppressing CD8+ T-cell activation and negatively impacting on tumor cells antigen presentation. Agents that can simultaneously target both PTP-1B and TCPTP have the potential to provide therapeutic benefits in the context of cancer and/or diabetes by increasing T-cell activation and reversing suppression of tumor cell MHC1 expression.
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