Hypoxia-inducible factor 2α (HIF-2α) is a transcription factor that plays a key role in oxygen homeostasis and response to tumor hypoxic microenvironment of cancer cells. Previous research has suggested that inhibition of HIF-2α is a promising antitumor approach, particularly against tumors associated with mutant von Hippel-Lindau (pVHL).
FmlH is a bacterial adhesin of uropathogenic E. coli (UPEC) that has been shown to be up-regulated during chronic UPEC infection. Washington University scientists recently disclosed the discovery and preclinical evaluation of novel FmlH lectin antagonists as potential candidates for the treatment of chronic urinary tract infections (UTIs) and kidney infections.
Blueprint Medicines Corp. recently disclosed the chemical structure of BLU-222, an oral, potent and highly selective inhibitor of the CDK2 kinase, being developed for the potential treatment of cancers with CCNE1 amplification and/or cyclin E overexpression, such as HR-positive HER2-negative breast cancer resistant to CDK4/6 inhibitor therapy.
About 90% of patients with multiple myeloma (MM) develop severe bone disease, known as myeloma bone disease (MBD). This occurs due to the ability of MM cells to disrupt bone homeostasis, leading to excessive bone resorption. Some current treatments are effective for treating MBD, but they are associated with undesired adverse events.
Tango Therapeutics Inc. has disclosed the discovery of TNG-348, an orally active, potent, reversible allosteric inhibitor of the USP1 deubiquitinating enzyme.
Because of increasing resistance to current antimalarial drugs, new agents with novel mechanisms of action are needed. Plasmepsins are a family of 10 Plasmodium falciparum aspartic proteases (PMI to PMX), among which plasmepsins IX and X (PMIX and PMX) have been identified as potential targets due to their involvement in egress, invasion and parasite development.
Researchers presented the development of a translational pharmacokinetic (PK)/receptor occupancy (RO) model of the tetravalent bispecific antibody (bsAb) CTX-8371 (Compass Therapeutics LLC) with the aim of investigating the possible effects of tetravalency compared to bivalency on RO and target internalization.
E1A binding protein (EP300) and CREB binding protein (CBP) are two closely related histone acetyltransferases (HATs), the mutations in which are related to several cancers. In the current study, researchers from Daiichi Sankyo Co. Ltd. aimed to develop orally available small molecule EP300/CBP HAT inhibitors with antitumor activity.
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