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- W1589778210 abstract "US28 is a human cytomegalovirus (HCMV) encoded G protein-coupled receptor that signals in a constitutively active manner. Recently, we identified 1 {5-(4(4-chlorophenyl)-4-hydroxypiperidin-1-yl)-2,2-diphenylpentanenitrile} as the first reported nonpeptidergic inverse agonist for a viral-encoded chemokine receptor. Interestingly, this compound is able to partially inhibit the viral entry of HIV-1. In this study we describe the synthesis of 1 and several of its analogues and unique structure-activity relationships for this first class of smallmolecule ligands for the chemokine receptor US28. Moreover, the compounds have been pharmacologically characterized as inverse agonists on US28. By modification of lead structure 1, it is shown that a 4-phenylpiperidine moiety is essential for affinity and activity. Other structural features of 1 are shown to be of less importance. These compounds define the first SAR of ligands on a viral GPCR (US28) and may therefore serve as important tools to investigate the significance of US28-mediated constitutive activity during viral infection." @default.
- W1589778210 created "2016-06-24" @default.
- W1589778210 creator A5075166625 @default.
- W1589778210 date "2007-01-01" @default.
- W1589778210 modified "2023-09-23" @default.
- W1589778210 title "Design and synthesis of small nonpeptidergic ligands for the human cytomegalovirus-encoded receptor US28" @default.
- W1589778210 cites W1489288393 @default.
- W1589778210 cites W1495173924 @default.
- W1589778210 cites W1508985019 @default.
- W1589778210 cites W1554666404 @default.
- W1589778210 cites W1601621203 @default.
- W1589778210 cites W1607819524 @default.
- W1589778210 cites W1701484549 @default.
- W1589778210 cites W1733590462 @default.
- W1589778210 cites W1766423076 @default.
- W1589778210 cites W1874468630 @default.
- W1589778210 cites W1906536207 @default.
- W1589778210 cites W1957990440 @default.
- W1589778210 cites W1963723282 @default.
- W1589778210 cites W1966815718 @default.
- W1589778210 cites W1966875239 @default.
- W1589778210 cites W1967410242 @default.
- W1589778210 cites W1969293297 @default.
- W1589778210 cites W1971908496 @default.
- W1589778210 cites W1972630226 @default.
- W1589778210 cites W1973135900 @default.
- W1589778210 cites W1973739813 @default.
- W1589778210 cites W1974089699 @default.
- W1589778210 cites W1974624016 @default.
- W1589778210 cites W1975888651 @default.
- W1589778210 cites W1977404210 @default.
- W1589778210 cites W1978179730 @default.
- W1589778210 cites W1978201079 @default.
- W1589778210 cites W1978404758 @default.
- W1589778210 cites W1978475414 @default.
- W1589778210 cites W1980841045 @default.
- W1589778210 cites W1982047106 @default.
- W1589778210 cites W1983349156 @default.
- W1589778210 cites W1983379803 @default.
- W1589778210 cites W1983750978 @default.
- W1589778210 cites W1988369982 @default.
- W1589778210 cites W1989506590 @default.
- W1589778210 cites W1990372914 @default.
- W1589778210 cites W1990515631 @default.
- W1589778210 cites W1991138299 @default.
- W1589778210 cites W1992732379 @default.
- W1589778210 cites W1992898199 @default.
- W1589778210 cites W1993860161 @default.
- W1589778210 cites W1994415948 @default.
- W1589778210 cites W1995055452 @default.
- W1589778210 cites W1996453015 @default.
- W1589778210 cites W1997429492 @default.
- W1589778210 cites W1997571015 @default.
- W1589778210 cites W1997598254 @default.
- W1589778210 cites W2000736660 @default.
- W1589778210 cites W2001071956 @default.
- W1589778210 cites W2001197100 @default.
- W1589778210 cites W2002696384 @default.
- W1589778210 cites W2006973742 @default.
- W1589778210 cites W2007052124 @default.
- W1589778210 cites W2008116181 @default.
- W1589778210 cites W2008808301 @default.
- W1589778210 cites W2009474250 @default.
- W1589778210 cites W2010595835 @default.
- W1589778210 cites W2011464419 @default.
- W1589778210 cites W2013130521 @default.
- W1589778210 cites W2014592511 @default.
- W1589778210 cites W2016074757 @default.
- W1589778210 cites W2017950818 @default.
- W1589778210 cites W2019595325 @default.
- W1589778210 cites W2019770130 @default.
- W1589778210 cites W2019879894 @default.
- W1589778210 cites W2021294213 @default.
- W1589778210 cites W2022630679 @default.
- W1589778210 cites W2025617572 @default.
- W1589778210 cites W2027807600 @default.
- W1589778210 cites W2029966155 @default.
- W1589778210 cites W2031005807 @default.
- W1589778210 cites W2031115772 @default.
- W1589778210 cites W2031208709 @default.
- W1589778210 cites W2031252235 @default.
- W1589778210 cites W2032612463 @default.
- W1589778210 cites W2034373600 @default.
- W1589778210 cites W2036276955 @default.
- W1589778210 cites W2037166272 @default.
- W1589778210 cites W2037421466 @default.
- W1589778210 cites W2039156817 @default.
- W1589778210 cites W2043234993 @default.
- W1589778210 cites W2045367932 @default.
- W1589778210 cites W2045793277 @default.
- W1589778210 cites W2046564413 @default.
- W1589778210 cites W2047527650 @default.
- W1589778210 cites W2052392655 @default.
- W1589778210 cites W2053631933 @default.
- W1589778210 cites W2055428388 @default.
- W1589778210 cites W2057385062 @default.
- W1589778210 cites W2060581674 @default.
- W1589778210 cites W2060880753 @default.
- W1589778210 cites W2060892966 @default.
- W1589778210 cites W2061501801 @default.