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Structural basis for molecular recognition of folic acid by folate receptors

Chen Chen, Jiyuan Ke, X. Edward Zhou, Wei Yi, Joseph S. Brunzelle, Jun Li, Eu-Leong Yong, H. Eric Xu () and Karsten Melcher ()
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Chen Chen: Program for Structural Biology and Drug Discovery, Van Andel Research Institute, 333 Bostwick Avenue North East, Grand Rapids, Michigan 49503, USA
Jiyuan Ke: Program for Structural Biology and Drug Discovery, Van Andel Research Institute, 333 Bostwick Avenue North East, Grand Rapids, Michigan 49503, USA
X. Edward Zhou: Program for Structural Biology and Drug Discovery, Van Andel Research Institute, 333 Bostwick Avenue North East, Grand Rapids, Michigan 49503, USA
Wei Yi: VARI/SIMM Center, Center for Structure and Function of Drug Targets, CAS-Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
Joseph S. Brunzelle: Life Sciences Collaborative Access Team, Synchrotron Research Center, Northwestern University, Argonne, Illinois 60439, USA
Jun Li: National University Hospital, Yong Loo Lin School of Medicine, National University of Singapore
Eu-Leong Yong: National University Hospital, Yong Loo Lin School of Medicine, National University of Singapore
H. Eric Xu: Program for Structural Biology and Drug Discovery, Van Andel Research Institute, 333 Bostwick Avenue North East, Grand Rapids, Michigan 49503, USA
Karsten Melcher: Program for Structural Biology and Drug Discovery, Van Andel Research Institute, 333 Bostwick Avenue North East, Grand Rapids, Michigan 49503, USA

Nature, 2013, vol. 500, issue 7463, 486-489

Abstract: Folate receptor-α (FRα) is overexpressed in many cancer cells and is therefore an important therapeutic target: here the X-ray crystal structure of folate-bound FRα is presented, revealing details of the ligand-binding pocket that may be useful in the development of small-molecule inhibitors for anticancer therapy.

Date: 2013
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DOI: 10.1038/nature12327

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