Researchers at Schrodinger Inc. and Takeda Pharmaceutical Co. Ltd. have described 3C-like proteinase (3CLpro; Mpro; nsp5) inhibitors reported to be useful for the treatment of coronavirus acute respiratory syndrome.
Scientists at H. Lundbeck A/S and Vernalis (R&D) Ltd. have divulged leucine-rich repeat kinase 2 (LRRK2; Dardarin) and LRRK2 G2019S mutant inhibitors reported to be useful for the treatment of Parkinson’s disease, Lewy body dementia and multiple system atrophy.
Scientists at East China Normal University, East China University of Science & Technology, Jinfeng Laboratory and Zhengzhou University have identified ribosomal protein S6 kinase α-6 (RPS6KA6; RSK-4) inhibitors reported to be useful for the treatment of cancer.
Jnana Therapeutics Inc. has synthesized sodium-dependent neutral amino acid transporter B(0)AT1 (SLC6A19) inhibitors reported to be useful for the treatment of amino acid metabolism disorders, amino acid transport disorders and metabolic and nutritional genetic disorders, among others.
Cullgen (Shanghai) Inc. has disclosed proteolysis targeting chimera (PROTAC) compounds comprising a DDB1- and CUL4-associated factor 1 (DCAF1) binding moiety covalently linked to target protein moiety (such as bromodomain-containing protein 4 [BRD4; HUNK1], cyclin-dependent kinase 4 [CDK4] and estrogen receptor α [ER-α; ESR1]) through a linker reported to be useful for the treatment of cancer.
Triple-negative breast cancer (TNBC) is an aggressive type of breast cancer with poor prognosis and limited therapeutic options, and it accounts for 15%-20% of female invasive breast cancers.
Researchers from Beijing Pharscin Innobio Co. Ltd. presented the discovery and preclinical characterization of a novel highly selective poly (ADP-ribose) polymerase 7 (PARP7) inhibitor, HSN-002066, being developed for the treatment of cancer.
The U.S. FDA has cleared Tr1x Inc.’s IND application for TRX-103 for the prevention of graft-vs.-host disease (GVHD) in patients undergoing HLA-mismatched hematopoietic stem cell transplantation (HSCT).
The overexpression of transferrin receptor 1 (TfR1) has been reported in several cancer types but is also expressed in normal cell types such as erythroblasts. On the other hand, epidermal growth factor receptor (EGFR) is highly expressed in epithelial carcinomas.
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