Molecular basis of USP7 inhibition by selective small-molecule inhibitors
Sign Up to like & getrecommendations! Published in 2017 at "Nature"
DOI: 10.1038/nature24451
Abstract: Ubiquitination controls the stability of most cellular proteins, and its deregulation contributes to human diseases including cancer. Deubiquitinases remove ubiquitin from proteins, and their inhibition can induce the degradation of selected proteins, potentially including otherwise… read more here.
Keywords: usp7 inhibition; basis usp7; selective small; molecular basis ... See more keywords
Selective small-molecule EPAC activators
Sign Up to like & getrecommendations! Published in 2019 at "Biochemical Society Transactions"
DOI: 10.1042/bst20190254
Abstract: The cellular signalling enzymes, EPAC1 and EPAC2, have emerged as key intracellular sensors of the secondary messenger cyclic 3′,5′-adenosine monophosphate (cyclic adenosine monophosphate) alongside protein kinase A. Interest has been galvanised in recent years thanks… read more here.
Keywords: small molecule; molecule epac; epac activators; selective small ... See more keywords
Abstract LB-068: Development of a screening cascade to identify selective small molecule inhibitors of DNMT1
Sign Up to like & getrecommendations! Published in 2018 at "Cancer Research"
DOI: 10.1158/1538-7445.am2018-lb-068
Abstract: DNA Methyltransferases (or DNMTs) play an important role in genomic integrity. The DNMT family of enzymes catalyse the transfer of methyl groups to specific CpG structures on DNA, with DNMT1 acting as a maintenance methyltransferase… read more here.
Keywords: selective small; development screening; small molecule; cascade ... See more keywords
TP-064, a potent and selective small molecule inhibitor of PRMT4 for multiple myeloma
Sign Up to like & getrecommendations! Published in 2018 at "Oncotarget"
DOI: 10.18632/oncotarget.24883
Abstract: Protein arginine methyltransferase (PRMT) 4 (also known as coactivator-associated arginine methyltransferase 1; CARM1) is involved in a variety of biological processes and is considered as a candidate oncogene owing to its overexpression in several types… read more here.
Keywords: potent selective; 064 potent; selective small; multiple myeloma ... See more keywords