Synthesis and neurotrophic activity of nonimmunosuppressant cyclosporin A derivatives

Ling Wei; Joseph P. Steiner; Gregory S. Hamilton; Yong Qian Wu

doi:10.1016/j.bmcl.2004.06.028

Synthesis and neurotrophic activity of nonimmunosuppressant cyclosporin A derivatives

Ling Wei, Joseph P. Steiner, Gregory S. Hamilton, Yong Qian Wu

School of Medicine

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

14 Scopus citations

Abstract

In order to exploit cyclophilin as a potential target for neurological drug design, we demonstrate in this presentation that several nonimmunosuppressant analogues of cyclosporin A, modified at the various positions in the 'effector' domain, are equipotent nerve growth agents compared to cyclosporin A. Our results suggest that neurotrophic activity of cyclosporin A and its derivatives resides in the binding domain, and binding to cyclophilin and/or inhibiting rotamase activity may be a necessity for neurotrophic effects of cyclophilin ligands.

Original language	English (US)
Pages (from-to)	4549-4551
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	17
DOIs	https://doi.org/10.1016/j.bmcl.2004.06.028
State	Published - Sep 6 2004

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2004.06.028

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title = "Synthesis and neurotrophic activity of nonimmunosuppressant cyclosporin A derivatives",

abstract = "In order to exploit cyclophilin as a potential target for neurological drug design, we demonstrate in this presentation that several nonimmunosuppressant analogues of cyclosporin A, modified at the various positions in the 'effector' domain, are equipotent nerve growth agents compared to cyclosporin A. Our results suggest that neurotrophic activity of cyclosporin A and its derivatives resides in the binding domain, and binding to cyclophilin and/or inhibiting rotamase activity may be a necessity for neurotrophic effects of cyclophilin ligands.",

author = "Ling Wei and Steiner, {Joseph P.} and Hamilton, {Gregory S.} and Wu, {Yong Qian}",

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AU - Wei, Ling

AU - Steiner, Joseph P.

AU - Hamilton, Gregory S.

AU - Wu, Yong Qian

PY - 2004/9/6

Y1 - 2004/9/6

N2 - In order to exploit cyclophilin as a potential target for neurological drug design, we demonstrate in this presentation that several nonimmunosuppressant analogues of cyclosporin A, modified at the various positions in the 'effector' domain, are equipotent nerve growth agents compared to cyclosporin A. Our results suggest that neurotrophic activity of cyclosporin A and its derivatives resides in the binding domain, and binding to cyclophilin and/or inhibiting rotamase activity may be a necessity for neurotrophic effects of cyclophilin ligands.

AB - In order to exploit cyclophilin as a potential target for neurological drug design, we demonstrate in this presentation that several nonimmunosuppressant analogues of cyclosporin A, modified at the various positions in the 'effector' domain, are equipotent nerve growth agents compared to cyclosporin A. Our results suggest that neurotrophic activity of cyclosporin A and its derivatives resides in the binding domain, and binding to cyclophilin and/or inhibiting rotamase activity may be a necessity for neurotrophic effects of cyclophilin ligands.

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JO - Bioorganic and Medicinal Chemistry Letters

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ER -

Synthesis and neurotrophic activity of nonimmunosuppressant cyclosporin A derivatives

Abstract

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