Janssen Pharmaceutica NV has synthesized new macrocyclic compounds acting as induced myeloid leukemia cell differentiation protein Mcl-1 inhibitors reported to be useful for the treatment of cancer.
Astellas Pharma Inc. has described new quinazoline GTPase KRAS (G12D mutant) degradation inducers reported to be useful for the treatment of pancreatic cancer. An exemplified compound degraded KRAS(G12D) mutant expressed in human pancreatic AsPC-1 cancer cells (DC50 = 37 nM) in ELISA assays. An exemplified compound degraded KRAS(G12D) mutant expressed in human pancreatic AsPC-1 cancer cells (DC50 = 37 nM) in ELISA assays. It inhibited 3D anchorage-independent proliferation of KRAS(G12D) mutant-positive AsPC-1 cancer cells (IC50 = 23 nM) in Celltiter-Glo assays.
Surviving apoptosis after administration of a drug triggered a previously unknown evolutionary process that gave tumor cells greater resistance to subsequent therapies. A cancer cell that does not die gets stronger. Cancer reappears with those cells that escape death thanks to a mechanism that, at the same time, offers a potential therapeutic target. According to a study led by St. Jude Children's Research Hospital in collaboration with the University of Glasgow and University of Oxford, the alternative to the cell death program is a stress response pathway that generates a persister cell phenotype not described before.
Sphingosine 1-phosphate (S1P) is a pleiotropic mediator involved in a variety of cellular functions. It is a product of cell membrane sphingolipid catabolism as it is generated from sphingosine intracellularly by sphingosine kinases 1 and 2 (SphK1 and SphK2), and it is exported from cells by spinster homolog 2 (Spns2) or major facilitator superfamily 2b (Mfsd2b).
Hangzhou Innogate Pharma Co. Ltd. has divulged new NLRP3 inflammasome inhibitors reported to be useful for the treatment of inflammation, cancer, infections and metabolic, respiratory, liver, kidney and autoimmune diseases, among other disorders.
Cerebral creatine (Cr) deficiency syndromes are caused by AGAT, GAMT or SLC6A8 deficiencies that may cause severe neurodevelopmental delay and intellectual disability.
Researchers from Centre National de la Recherche Scientifique and affiliated organizations presented the discovery and preclinical identification of novel inhibitors of metallo-beta-lactamases (MBLs). Synthesis and optimization of novel broad-spectrum inhibitors against most relevant MBLs, such as VIM-type enzymes and NDM-1, led to the identification of JMV-7061 as the lead from the series.
Avalo Therapeutics Inc.'s human B and T lymphocyte attenuator (BTLA) agonist fusion protein, AVTX-008, has entered IND-enabling studies, with the company evaluating a number of immune dysregulation disorders to pursue.
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