Discovery of Selective P2Y6R Antagonists with High Affinity and In Vivo Efficacy for Inflammatory Disease Therapy.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.3c00210
Abstract: As a member of purinoceptors, the P2Y6 receptor (P2Y6R) plays a crucial role in modulating immune signals and has been considered as a potential therapeutic target for inflammatory diseases. On the basis of the speculated… read more here.
Keywords: compound; p2y6r; antagonists high; p2y6r antagonists ... See more keywords
Discovery of Selective Inhibitors of Endoplasmic Reticulum Aminopeptidase 1.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b00293
Abstract: ERAP1 is an endoplasmic reticulum-resident zinc aminopeptidase that plays an important role in the immune system by trimming peptides for loading onto major histocompatibility complex (MHC-I) proteins. Here we report discovery of the first inhibitors… read more here.
Keywords: discovery selective; endoplasmic reticulum; aminopeptidase; compound ... See more keywords
Discovery of a Selective Inhibitor for the YEATS Domains of ENL/AF9
Sign Up to like & getrecommendations! Published in 2019 at "SLAS Discovery"
DOI: 10.1177/2472555218809904
Abstract: Eleven-nineteen leukemia (ENL) contains an epigenetic reader domain (YEATS domain) that recognizes lysine acylation on histone 3 and facilitates transcription initiation and elongation through its interactions with the super elongation complex (SEC) and the histone… read more here.
Keywords: selective inhibitor; yeats domain; inhibitor; discovery selective ... See more keywords