Design, Synthesis and Evaluation of AdSS Bisubstrate Inhibitors
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DOI: 10.1002/cmdc.202000498
Abstract: Many cancers lack the expression of methylthioadenosine phosphorylase (MTAP). These cancers require adenylosuccinate synthetase (AdSS) for nucleic acid synthesis. By inhibiting adenylosuccinate synthetase, we potentially have a new therapeutic agent. Bisubstrate inhibitors were synthesized and… read more here.
Keywords: evaluation adss; design synthesis; bisubstrate inhibitors; adss ... See more keywords
Bisubstrate Inhibitors of Severe Acute Respiratory Syndrome Coronavirus-2 Nsp14 Methyltransferase
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DOI: 10.1021/acsmedchemlett.2c00265
Abstract: Taking advantage of the uniquely constricted active site of SARS-CoV-2 Nsp14 methyltransferase, we have designed bisubstrate inhibitors interacting with the SAM and RNA substrate binding pockets. Our efforts have led to nanomolar inhibitors including compounds… read more here.
Keywords: severe acute; bisubstrate inhibitors; nsp14 methyltransferase; acute respiratory ... See more keywords
Structural and biochemical evaluation of bisubstrate inhibitors of protein arginine N-methyltransferases PRMT1 and CARM1 (PRMT4)
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DOI: 10.1042/bcj20190826
Abstract: Attenuating the function of protein arginine methyltransferases (PRMTs) is an objective for the investigation and treatment of several diseases including cardiovascular disease and cancer. Bisubstrate inhibitors that simultaneously target binding sites for arginine substrate and… read more here.
Keywords: protein arginine; evaluation bisubstrate; bisubstrate; arginine methyltransferases ... See more keywords
Structural and biochemical evaluation of bisubstrate inhibitors of protein arginine N-methyltransferases PRMT1 and CARM1 (PRMT4).
Sign Up to like & getrecommendations! Published in 2020 at "Biochemical Journal"
DOI: 10.2210/pdb6s7c/pdb
Abstract: Attenuating the function of protein arginine methyltransferases (PRMTs) is an objective for the investigation and treatment of several diseases including cardiovascular disease and cancer. Bisubstrate inhibitors that simultaneously target binding sites for arginine substrate and… read more here.
Keywords: protein arginine; evaluation bisubstrate; bisubstrate; arginine methyltransferases ... See more keywords