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Article

Synthesis of calcineurin-resistant derivatives of FK506 and selection of compensatory receptors.

Chemistry & biology - 1 Jan 2002

Clemons Paul A, Gladstone Brian G, Seth Abhinav, Chao Elizabeth D, Foley Michael A, Schreiber Stuart L

Abstract excerpt

We used olefin metathesis to synthesize C40 derivatives of FK506 and measured their ability, when complexed to FKBP12, to inhibit calcineurin's phosphatase activity. We identified modular dimerization domains (CABs) containing segments of the calcineurin A and B polypeptides. These CABs respond to FK506 both when overexpressed in mammalian cells and in yeast or mammalian three-hybrid assays. Using chemical...

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Identifiers

PMID: 11841938
DOI: 10.1016/s1074-5521(02)00085-6

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

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