Discovery of an Angiotensin II Binding Inhibitor from a Cytospora sp. Using Semi-automated Screening Procedures

SIOBHAN STEVENS-MILES; MICHAEL A. GOETZ; GERALD F. BILLS; ROBERT A. GIACOBBE; JAN S. TKACZ; RAYMOND S. L. CHANG; MARINA MOJENA; ISABEL MARTIN; MARIA TERESA DIEZ; FERNANDO PELAE; OTTO D. HENSENS; TRACY JONES; RICHARD W. BURG; Y. L. KONG; LEEYUAN HUANG

doi:10.7164/antibiotics.49.119

Discovery of an Angiotensin II Binding Inhibitor from a Cytospora sp. Using Semi-automated Screening Procedures

SIOBHAN STEVENS-MILES, MICHAEL A. GOETZ, GERALD F. BILLS, ROBERT A. GIACOBBE, JAN S. TKACZ, RAYMOND S. L. CHANG, MARINA MOJENA, ISABEL MARTIN, MARIA TERESA DIEZ, FERNANDO PELAE, OTTO D. HENSENS, TRACY JONES, RICHARD W. BURG, Y. L. KONG, LEEYUAN HUANG

Author information

SIOBHAN STEVENS-MILES
Merck Research Laboratories
MICHAEL A. GOETZ
Merck Research Laboratories
GERALD F. BILLS
Merck Research Laboratories
ROBERT A. GIACOBBE
Merck Research Laboratories
JAN S. TKACZ
Merck Research Laboratories
RAYMOND S. L. CHANG
West Point, Pennsylvania 19486 U.S.A.
MARINA MOJENA
Merck Sharp and Dohme de España
ISABEL MARTIN
Merck Sharp and Dohme de España
MARIA TERESA DIEZ
Merck Sharp and Dohme de España
FERNANDO PELAE
Merck Sharp and Dohme de España
OTTO D. HENSENS
Merck Research Laboratories
TRACY JONES
Merck Research Laboratories
RICHARD W. BURG
Merck Research Laboratories
Y. L. KONG
Merck Research Laboratories
LEEYUAN HUANG
Merck Research Laboratories

JOURNAL FREE ACCESS

1996 Volume 49 Issue 2 Pages 119-123

DOI https://doi.org/10.7164/antibiotics.49.119

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Abstract

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 μM and was specific for angiotensin II AT₂.

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