Synthesis and neurotrophic activity of nonimmunosuppressant cyclosporin A derivatives.

Article Details

Citation

Copy to clipboard

Wei L, Steiner JP, Hamilton GS, Wu YQ

Synthesis and neurotrophic activity of nonimmunosuppressant cyclosporin A derivatives.

Bioorg Med Chem Lett. 2004 Sep 6;14(17):4549-51.

PubMed ID

15357990 [ View in PubMed

]

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Cyclosporine	Peptidyl-prolyl cis-trans isomerase A	Ki (nM)	10	N/A	N/A	Details
Cyclosporine	Peptidyl-prolyl cis-trans isomerase A	Ki (nM)	20	N/A	N/A	Details