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Cyclophilin Succumbs to a Macrocyclic Chameleon
Monash Univ, Dept Med Chem, MIPS, 381 Royal Parade, Parkville, Vic 3052, Australia.
Uppsala University, Disciplinary Domain of Science and Technology, Chemistry, Department of Chemistry - BMC, Organic Chemistry.ORCID iD: 0000-0002-4205-6040
2018 (English)In: Journal of Medicinal Chemistry, ISSN 0022-2623, E-ISSN 1520-4804, Vol. 61, no 21, p. 9469-9472Article in journal (Refereed) Published
Abstract [en]

Targets that have large and groove-shaped binding sites, such as cyclophilin, are difficult to drug with small molecules. Macrocycles of natural product origin can be ideal starting points for such targets as illustrated by the transformation of sanglifehrin A into an orally bioavailable potential candidate drug. Optimization benefits from development of convergent, modular synthetic routes in combination with structure and property based methods for lead optimization.

Place, publisher, year, edition, pages
AMER CHEMICAL SOC , 2018. Vol. 61, no 21, p. 9469-9472
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Medicinal Chemistry
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URN: urn:nbn:se:uu:diva-371501DOI: 10.1021/acs.jmedchem.8b01555ISI: 000449889200005PubMedID: 30359012OAI: oai:DiVA.org:uu-371501DiVA, id: diva2:1273562
Available from: 2018-12-21 Created: 2018-12-21 Last updated: 2018-12-21Bibliographically approved

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Kihlberg, Jan

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