Sch 213766, a novel chemokine receptor CCR-5 inhibitor from Chaetomium globosum.
A novel fungal secondary metabolite, Sch 213766 was isolated from the fungal fermentation broth of Chaetomium globosum as the chemokine receptor CCR-5 inhibitor and shown to be the methyl ester of the previously described tetramic acid Sch 210972 on the basis of UV, MS and NMR spectral data analyses. Sch213766 exhibited an IC(50) value of 8.6 muM in the CCR-5 receptor in vitro binding assay.
Yang
Shu-Wei
SW
Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, USA. shu-wei.yang@spcorp.com
Mierzwa
Ronald
R
Terracciano
Joseph
J
Patel
Mahesh
M
Gullo
Vincent
V
Wagner
Nicole
N
Baroudy
Bahige
B
Puar
Mohindar
M
Chan
Tze-Ming
TM
Chu
Min
M
D019380:Anti-HIV Agents / Q000737:chemistry / Q000302:isolation & purification / Q000378:metabolism; D065100:CCR5 Receptor Antagonists; D002597:Chaetomium / Q000254:growth & development / Q000378:metabolism*; D017077:Culture Media, Conditioned / Q000378:metabolism; D005285:Fermentation; D008738:Methyl Ethers / Q000737:chemistry / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology