The accelerated approval by the U.S. FDA of Immunogen Inc.’s landmark antibody-drug conjugate Elahere (mirvetuximab soravtansine-gynx) injected further oomph into the NaPi2b space, where a handful of developers are due to yield important data shortly. In play are such names as Mersana Therapeutics Inc. and Zymeworks Inc., encouraged by historical – if not entirely successful – efforts by giant Roche Holding AG.
Lead Discovery Center GmbH has described 3-substituted 1H-pyrrolo[2,3-b]-pyridines acting as G protein-coupled receptor kinase 5 (GRK5) inhibitors reported to be useful for the treatment of cancer, inflammatory, immunological, metabolic and cardiovascular disorders.
Blueprint Medicines Corp. has identified substituted pyrimidinyl-pyrazoles acting as cyclin-dependent kinase (CDK) inhibitors, particularly CDK2, reported to be useful for the treatment of cancer.
Wigen Biomedicine Technology (Shanghai) Co. Ltd. has disclosed isocitrate dehydrogenase (NADP+) (IDPc, IDH1) mutant inhibitors reported to be useful for the treatment of cancer.
Recent findings have suggested that MMR-deficient CRC cells are highly sensitive to the loss of bifunctional 3ʹ-5ʹ exonuclease/ATP-dependent helicase WRN.
A Nanjing University of Chinese Medicine research team has discovered novel compounds being evaluated as potential anti-hepatocellular carcinoma (anti-HCC) agents.
Mortality rates related to non-small-cell lung cancer (NSCLC) remain still high, with about 75% of patients getting little clinical benefit from therapy. Adverse conditions in the tumor microenvironment, such as hypoxia or oxidative stress, disrupt the protein-folding capacity of the endoplasmic reticulum (ER) in infiltrating cells, provoking cellular stress that activates the unfolded protein response (UPR) pathway to restore proteostasis in this cellular organelle. During ER stress, serine/threonine-protein kinase/endoribonuclease IRE1 exerts its endoribonuclease activity on XBP1 mRNA generating a splice variant that encodes XBP1s that induces UPR target gene expression.
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