The bromodomain and extraterminal (BET) subfamily contain two similar tandem bromodomains (BD1 and BD2). Selective inhibition of BD2 has been deeply explored; however, the obtention of selective and potent BD1 inhibitors is essential and still lacking.
A researcher at Australia’s Children’s Cancer Institute has been awarded a 3-year US$400,000 grant by the Chadtough Defeat DIPG Foundation to develop and test a new drug candidate for diffuse intrinsic pontine glioma (DIPG).
Previous studies have suggested the importance of cholesterol metabolism in multiple myeloma (MM) cells. Since ferroptosis is closely related to lipid metabolism, researchers from Houston Methodist Research Institute aimed to investigate the crosstalk between metabolic reprogramming and ferroptosis in MM cells.
Scinnohub Pharmaceutical Co. Ltd. has divulged cyclin-dependent kinase (CDK) inhibitors, particularly CDK9 inhibitors, reported to be useful for the treatment of cancer.
Scientists at Shanghai Aryl Pharmtech Co. Ltd. and Zhejiang Hisun Pharmaceutical Co. Ltd. have synthesized kinesin-like protein KIF18A inhibitors reported to be useful for the treatment of cancer.
Chicken ovalbumin upstream promoter transcription factor 2 (COUP-TFII, aka NR2F2) is dysregulated in different cancer types. However, its exact role remains controversial because it acts as an oncosuppressor in some tumors and as an oncogene in others. In glioma progression, the role of COUP-TFII is still unclear.
The targeted delivery of radionucleotides into tumors, known as radioimmunotherapy (RIT), has proven effective mainly in hematological cancer treatment, but its usefulness in solid tumors needs further exploration. Researchers from Oncoone Research & Development GmbH described the use of Pretarg-it, a novel pre-targeted RIT strategy that consists of ON-105 and the radioactively labeled DOTA-di-HSG peptide.
Combining multiple kinase inhibitors may present off-target risks or unbalanced inhibition among different targets, that may be solved using rationally designed small molecules. Researchers from Mekanistic Therapeutics Inc. and collaborators described the in vitro and in vivo profile of MTX-531.
Transcriptome-wide gene expression analyses revealed that oncogenic forms of NRAS, KRAS and HRAS (HRAS V12, KRAS V12 and NRAS Q61K) activated the expression of several genes, including IκBα.
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