Discovery of an angiotensin II binding inhibitor from a Cytospora sp. using semi-automated screening procedures.
Cytosporin A, B and C, three antagonists of [125I]-angiotensin II binding to rat adrenal glands were discovered in fermentations of an endophytic Cytospora sp. during routine screening using semi-automated procedures. The most potent of these displayed an IC50 of 1.5-3 microM and was specific for angiotensin II AT2.
Stevens-Miles
S
S
Merck Research Laboratories, Rahway, New Jersey 07065, USA.
Goetz
M A
MA
Bills
G F
GF
Giacobbe
R A
RA
Tkacz
J S
JS
Chang
R S
RS
Mojena
M
M
Martin
I
I
Diez
M T
MT
Pelaez
F
F
Hensens
O D
OD
Jones
T
T
Burg
R W
RW
Kong
Y L
YL
Huang
L
L
D000311:Adrenal Glands / Q000378:metabolism; D000804:Angiotensin II / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000818:Animals; D001578:Benzopyrans / Q000737:chemistry / Q000494:pharmacology*; D005285:Fermentation; D013058:Mass Spectrometry; D003904:Mitosporic Fungi / Q000737:chemistry*; D051381:Rats
D001578:Benzopyrans; C099196:cytosporin A; C099197:cytosporin B; C099198:cytosporin C; D000804:Angiotensin II