Researchers from Fochon Biosciences Ltd. have reported the discovery and preclinical evaluation of a novel second-generation B-cell lymphoma 2 (BCL2) inhibitor, FCN-683, being developed for the treatment of B-cell malignancies. FCN-683 showed the ability to potently and selectively inhibit both wild-type BCL2 (IC50=0.11 nM) and multiple clinically relevant venetoclax-resistant mutants, including G101V, D103E/V/Y, F104L, A113G, R129L and V156D.

Acute lung injury (ALI) is a respiratory disease characterized by increased lung epithelial permeability, inflammatory cell infiltration and edema with a more than 40% mortality rate. Researchers from Wenzhou Medical University and colleagues reported the design and synthesis of [I], a novel cinnamic acid (CIN) derivative that targets the interaction of MD-2 protein and LPS showing anti-inflammatory activity.

In accordance with the publishing schedule, BioWorld Science will not be published on Monday, May 1, 2023.

KRAS Q61H mutation has been found in pancreatic ductal adenocarcinoma (PDAC), colorectal cancer (CRC), and non-small-cell lung cancer (NSCLC) among other solid tumors. In healthy cells, RAS proteins switch between ON and OFF states during signal transduction, but in cancer, mutations in RAS genes or regulators install RAS proteins in ON state permanently.

Cyclin-dependent kinase 8 (CDK8) is implicated in both transcription and cellular response to environmental stress signals. Due to its association with the complex that sustains cell proliferation and viability, and its role in cancer cell stress response to radiotherapy and chemotherapy, CDK8 is considered a target to watch in cancer therapy.