Inhibition of RANTES/CCR1-mediated chemotaxis by cosalane and related compounds.
The anti-HIV agent cosalane and several of its analogues inhibited RANTES-induced migration of human monocytes, but they did not inhibit migration induced by MIP1alpha or MIP1beta. RANTES-induced migration of single receptor CCRI-HEK transfectants was also inhibited by the cosalanes. Acetylation of the reactive amino groups of RANTES abrogated the inhibitory activity of cosalane. The data suggest that cosalane and its structural analogues may interfere with the RANTES/CCR1 interaction by binding to RANTES.
Howard
O M
OM
Laboratory of Molecular Immunoregulation, National Cancer Istitute-Frederick Cancer Research and Development Center, MD 21702, USA. howardz@mail.ncifcrf.gov
Dong
H F
HF
Oppenheim
J J
JJ
Insaf
S
S
Santhosh
K C
KC
Paul
G
G
Cushman
M
M
D000107:Acetylation; D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D001312:Aurintricarboxylic Acid / Q000031:analogs & derivatives / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D002460:Cell Line; D018946:Chemokine CCL5 / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D054377:Chemokine CXCL12; D019743:Chemokines, CXC / Q000494:pharmacology; D002633:Chemotaxis / Q000187:drug effects*; D006801:Humans; D008214:Lymphocytes / Q000187:drug effects; D015394:Molecular Structure; D011485:Protein Binding; D054389:Receptors, CCR1; D019707:Receptors, Chemokine / Q000037:antagonists & inhibitors* / Q000378:metabolism; D014162:Transfection
D019380:Anti-HIV Agents; C515300:CCR1 protein, human; C515255:CXCL12 protein, human; D018946:Chemokine CCL5; D054377:Chemokine CXCL12; D019743:Chemokines, CXC; D054389:Receptors, CCR1; D019707:Receptors, Chemokine; C083060:cosalane; D001312:Aurintricarboxylic Acid