Discovery of novel small molecule orally bioavailable C-X-C chemokine receptor 4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.
Skerlj
Renato T
RT
Genzyme Corp., 153 Second Avenue, Waltham, Massachusetts 02451, USA. renato.skerlj@genzyme.com
Bridger
Gary J
GJ
Kaller
Al
A
McEachern
Ernest J
EJ
Crawford
Jason B
JB
Zhou
Yuanxi
Y
Atsma
Bem
B
Langille
Jonathon
J
Nan
Susan
S
Veale
Duane
D
Wilson
Trevor
T
Harwig
Curtis
C
Hatse
Sigrid
S
Princen
Katrien
K
De Clercq
Erik
E
Schols
Dominique
D
D000284:Administration, Oral; D000634:Aminoquinolines; D000818:Animals; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001562:Benzimidazoles; D001682:Biological Availability; D002082:Butylamines; D002118:Calcium / Q000378:metabolism; D002460:Cell Line; D002463:Cell Membrane Permeability; D004285:Dogs; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D006573:Heterocyclic Compounds, 1-Ring / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007963:Leukocytes, Mononuclear / Q000187:drug effects / Q000378:metabolism / Q000821:virology; D011869:Radioligand Assay; D051381:Rats; D019718:Receptors, CXCR4 / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014779:Virus Replication / Q000187:drug effects
D000634:Aminoquinolines; D019380:Anti-HIV Agents; D001562:Benzimidazoles; D002082:Butylamines; D006573:Heterocyclic Compounds, 1-Ring; D019718:Receptors, CXCR4; C494414:mavorixafor; D002118:Calcium