A simple and efficient route to the FKBP-binding domain from rapamycin

Wei Li; Shridhar Bhat; Jun O. Liu

doi:10.1016/j.tetlet.2011.07.094

A simple and efficient route to the FKBP-binding domain from rapamycin

Wei Li, Shridhar Bhat, Jun O. Liu

School of Medicine

Research output: Contribution to journal › Article › peer-review

2 Scopus citations

Abstract

A simple and highly efficient route to the FKBP-binding domain (FKBD) from the natural product rapamycin has been developed, which entails a sequence of ozonolysis/Baeyer-Villiger/Wittig reactions. The newly synthesized FKBD may serve as a core to assemble hybrid macrocyclic libraries for the discovery of novel probes of protein function and to synthesize new ligands for the FKBP family of proteins.

Original language	English (US)
Pages (from-to)	5070-5072
Number of pages	3
Journal	Tetrahedron Letters
Volume	52
Issue number	39
DOIs	https://doi.org/10.1016/j.tetlet.2011.07.094
State	Published - Sep 28 2011

Keywords

FKBP
FKBP-binding domain
Rapamycin

ASJC Scopus subject areas

Biochemistry
Drug Discovery
Organic Chemistry

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10.1016/j.tetlet.2011.07.094

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title = "A simple and efficient route to the FKBP-binding domain from rapamycin",

abstract = "A simple and highly efficient route to the FKBP-binding domain (FKBD) from the natural product rapamycin has been developed, which entails a sequence of ozonolysis/Baeyer-Villiger/Wittig reactions. The newly synthesized FKBD may serve as a core to assemble hybrid macrocyclic libraries for the discovery of novel probes of protein function and to synthesize new ligands for the FKBP family of proteins.",

keywords = "FKBP, FKBP-binding domain, Rapamycin",

author = "Wei Li and Shridhar Bhat and Liu, {Jun O.}",

note = "Funding Information: This work was supported by the NIH Director{\textquoteright}s Pioneer Award ( DP1OD006795 to JOL). We are grateful to Drs. Zufeng Guo, Manisha Das and members of the Liu Lab for helpful discussions. We thank Drs. Carol Greider and Paul Talalay for generous provision of temporary lab space for this work. ",

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T1 - A simple and efficient route to the FKBP-binding domain from rapamycin

AU - Li, Wei

AU - Bhat, Shridhar

AU - Liu, Jun O.

N1 - Funding Information: This work was supported by the NIH Director’s Pioneer Award ( DP1OD006795 to JOL). We are grateful to Drs. Zufeng Guo, Manisha Das and members of the Liu Lab for helpful discussions. We thank Drs. Carol Greider and Paul Talalay for generous provision of temporary lab space for this work.

PY - 2011/9/28

Y1 - 2011/9/28

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AB - A simple and highly efficient route to the FKBP-binding domain (FKBD) from the natural product rapamycin has been developed, which entails a sequence of ozonolysis/Baeyer-Villiger/Wittig reactions. The newly synthesized FKBD may serve as a core to assemble hybrid macrocyclic libraries for the discovery of novel probes of protein function and to synthesize new ligands for the FKBP family of proteins.

KW - FKBP

KW - FKBP-binding domain

KW - Rapamycin

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ER -

A simple and efficient route to the FKBP-binding domain from rapamycin

Abstract

Keywords

ASJC Scopus subject areas

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