In their efforts to develop next-generation drugs whose structures differ from those of conventional IMiDs, researchers at Fujimoto Pharmaceutical Corp. developed FPFT-2216 through optimization of a lead compound.
In their ongoing search for effective small-molecule inhibitors of focal adhesion kinase (FAK), researchers at Beijing Normal University and collaborators started from a promising lead compound that they previously described.
Individuals with both sickle cell disease (SCD) and sickle cell trait are at higher risk than others of developing renal medullary cancer (RMC), the rarest and deadliest subtype of kidney cancer. Researchers at MD Anderson Cancer Center have identified the molecular mechanisms behind the increased risk, gaining new insights into antitumor immunity more generally and, potentially, new ways to treat RMC, and possibly other tumors as well.SCD “has been studied for 30 years, but 95% of the effort [has been] working on the red blood cells … how red blood cells contribute to hypoxia and then reduce oxygen supply,” Chunru Lin told BioWorld.
Scientists at Jiangsu Hengrui Medicine Co. Ltd. and Shanghai Hengrui Pharmaceutical Co. Ltd. have described GTPase KRAS (G12D mutant) and/or KRAS (G12V mutant) inhibitors reported to be useful for the treatment of cancer.
Chia Tai Tianqing Pharmaceutical Group Co. Ltd. has synthesized poly(ADP-ribose) polymerase 1 (PARP-1; ARTD1) inhibitors reported to be useful for the treatment of cancer.
Incyte Corp. has disclosed GTPase KRAS (mutant) inhibitors reported to be useful for the treatment of cancer, as well as autoimmune and inflammatory disorders.
Major histocompatibility complex class I-related protein A and B (MICA and MICB) are ligands for the natural killer group 2 member D (NKG2D) receptor and are widely expressed on tumor cells, with very limited expression on normal tissues.
Tissue factor (TF), a transmembrane protein overexpressed in tumors such as cervical, head and neck, NSCLC, and pancreatic cancers, initiates the extrinsic coagulation pathway under normal subendothelial expression. TF-targeted vedotin antibody-drug conjugates (ADCs) are in clinical evaluation for solid tumors, but toxicities, including peripheral neuropathy, ocular effects and epistaxis, limit their use.
Tumors with high levels of microsatellite instability (MSI-H), such as some subsets of colorectal, endometrial and gastric cancers, are associated with a hypermutated phenotype and a specific dependency on the WRN gene. Pharmacologic inhibition of WRN has been shown to selectively impair the viability of MSI-H cancer cells, effectively blocking tumor growth while sparing microsatellite-stable (MSS) cells.
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