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.
Mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1) is a key regulator of physiological antigen receptor signaling in B cells and T cells, as it is the only component of the MALT1-BCL10-CARD11 (CBM) signalosome with proteolytic activity.
Previous research has shown that adenosine impairs antitumor immunity, and high levels of adenosine and CD73 have been associated with poor prognosis in cancer.
Researchers from Foghorn Therapeutics Inc. recently presented preclinical data for FHD-609, a heterobifunctional degrader of BRD9 designed for the treatment of sarcoma. Synthesis and optimization of a series of first-generation compounds led to the identification of FHD-609 as a rapid, selective and highly potent BRD9 degrader, with high plasma stability and acceptable solubility.
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