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.
Plasma pharmacodynamic biomarkers may be a reliable tool for biosimilarity assessment without having to rely on clinical trials, which are costly and time consuming.
Researchers from Merck & Co have presented the discovery of inhibitors of the YAP/TAZ-TEAD complex as potential anticancer agents. YAP and its paralogue TAZ act as terminal effectors of the Hippo signaling pathway by regulating the transcriptional activity of the different TEAD isoforms.
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