Generation of Novel Rapamycin Structures by Microbial Manipulations

HLROYUKI NLSHIDA; TATSUO SAKAKIBARA; FUKUMATSU AOKI; TOSHIYUKI SAITO; KATSUOMI ICHIKAWA; TAISUKE INAGAKI; YASUHIRO KOJIMA; YUJI YAMAUCHI; LIANG H. HUANG; MARK A. GUADLIANA; TAKUSHI KANEKO; NAKAO KOJIMA

doi:10.7164/antibiotics.48.657

HLROYUKI NLSHIDA, TATSUO SAKAKIBARA, FUKUMATSU AOKI, TOSHIYUKI SAITO, KATSUOMI ICHIKAWA, TAISUKE INAGAKI, YASUHIRO KOJIMA, YUJI YAMAUCHI, LIANG H. HUANG, MARK A. GUADLIANA, TAKUSHI KANEKO, NAKAO KOJIMA

Author information

HLROYUKI NLSHIDA
Central Research Division, Pfizer Pharmaceuticals Inc.
TATSUO SAKAKIBARA
Central Research Division, Pfizer Pharmaceuticals Inc.
FUKUMATSU AOKI
Central Research Division, Pfizer Pharmaceuticals Inc.
TOSHIYUKI SAITO
Central Research Division, Pfizer Pharmaceuticals Inc.
KATSUOMI ICHIKAWA
Central Research Division, Pfizer Pharmaceuticals Inc.
TAISUKE INAGAKI
Central Research Division, Pfizer Pharmaceuticals Inc.
YASUHIRO KOJIMA
Central Research Division, Pfizer Pharmaceuticals Inc.
YUJI YAMAUCHI
Central Research Division, Pfizer Pharmaceuticals Inc.
LIANG H. HUANG
Central Research Division, Pfizer Inc.
MARK A. GUADLIANA
Central Research Division, Pfizer Inc.
TAKUSHI KANEKO
Central Research Division, Pfizer Inc.
NAKAO KOJIMA
Central Research Division, Pfizer Pharmaceuticals Inc.

JOURNAL FREE ACCESS

1995 Volume 48 Issue 7 Pages 657-666

DOI https://doi.org/10.7164/antibiotics.48.657

Details

Abstract

A new rapamycin producing culture was isolated and designated as Actinoplanes sp. N902-109. The addition of a cytochrome P-450 inhibitor and precursor feeding using this culture, and biotransformation approaches generated new rapamycin analogs with modifications at C-4, C-9, C-16, C-27, C-28 and/or C-39. The immunosuppressive activity of the resulting analogs was established in the mixed lymphocyte reaction assay.

Corresponding author

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