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Structural basis for molecular recognition of folic acid by folate receptors

Author

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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
    National University of Singapore Graduate School for Integrative Science and Engineering, National University of Singapore)

  • 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
    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)

  • Karsten Melcher

    (Program for Structural Biology and Drug Discovery, Van Andel Research Institute, 333 Bostwick Avenue North East, Grand Rapids, Michigan 49503, USA)

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.

Suggested Citation

  • Chen Chen & Jiyuan Ke & X. Edward Zhou & Wei Yi & Joseph S. Brunzelle & Jun Li & Eu-Leong Yong & H. Eric Xu & Karsten Melcher, 2013. "Structural basis for molecular recognition of folic acid by folate receptors," Nature, Nature, vol. 500(7463), pages 486-489, August.
    • Handle: RePEc:nat:nature:v:500:y:2013:i:7463:d:10.1038_nature12327
    DOI: 10.1038/nature12327
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    Cited by:

    1. Olga A. Balashova & Alexios A. Panoutsopoulos & Olesya Visina & Jacob Selhub & Paul S. Knoepfler & Laura N. Borodinsky, 2024. "Noncanonical function of folate through folate receptor 1 during neural tube formation," Nature Communications, Nature, vol. 15(1), pages 1-17, December.
    2. Yaxian Zhou & Chunrong Li & Xuankun Chen & Yuan Zhao & Yaxian Liao & Penghsuan Huang & Wenxin Wu & Nicholas S. Nieto & Lingjun Li & Weiping Tang, 2024. "Development of folate receptor targeting chimeras for cancer selective degradation of extracellular proteins," Nature Communications, Nature, vol. 15(1), pages 1-14, December.
    3. Samuel C. Griffiths & Rebekka A. Schwab & Kamel El Omari & Benjamin Bishop & Ellen J. Iverson & Tomas Malinauskas & Ramin Dubey & Mingxing Qian & Douglas F. Covey & Robert J. C. Gilbert & Rajat Rohatg, 2021. "Hedgehog-Interacting Protein is a multimodal antagonist of Hedgehog signalling," Nature Communications, Nature, vol. 12(1), pages 1-13, December.

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