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Int. J. Mol. Sci. 2018, 19(2), 392; https://doi.org/10.3390/ijms19020392

Dissecting the Structure–Activity Relationship of Galectin–Ligand Interactions

1,2,3,†
,
1,†
,
1,†
,
1
,
1,4
and
1,2,4,5,6,*
1
Institute of Biological Chemistry, Academia Sinica, No. 128, Academia Road Section 2, Nan-Kang, Taipei 11529, Taiwan
2
Taiwan International Graduate Program (TIGP), Sustainable Chemical Science and Technology (SCST), Academia Sinica, Taipei 11529, Taiwan
3
Department of Applied Chemistry, National Chiao Tung University, Hsinchu 300, Taiwan
4
Institute of Biochemical Sciences, National Taiwan University, Taipei 10617, Taiwan
5
Department of Chemistry, National Taiwan University, Taipei 10617, Taiwan
6
The Genomics Research Center, Academia Sinica, Taipei 11529, Taiwan
These authors have equal contribution to this work.
*
Author to whom correspondence should be addressed.
Received: 17 December 2017 / Revised: 18 January 2018 / Accepted: 24 January 2018 / Published: 29 January 2018
(This article belongs to the Special Issue Galectins in Cancer and Translational Medicine)
View Full-Text   |   Download PDF [21581 KB, uploaded 15 March 2018]   |  

Abstract

Galectins are β-galactoside-binding proteins. As carbohydrate-binding proteins, they participate in intracellular trafficking, cell adhesion, and cell–cell signaling. Accumulating evidence indicates that they play a pivotal role in numerous physiological and pathological activities, such as the regulation on cancer progression, inflammation, immune response, and bacterial and viral infections. Galectins have drawn much attention as targets for therapeutic interventions. Several molecules have been developed as galectin inhibitors. In particular, TD139, a thiodigalactoside derivative, is currently examined in clinical trials for the treatment of idiopathic pulmonary fibrosis. Herein, we provide an in-depth review on the development of galectin inhibitors, aiming at the dissection of the structure–activity relationship to demonstrate how inhibitors interact with galectin(s). We especially integrate the structural information established by X-ray crystallography with several biophysical methods to offer, not only in-depth understanding at the molecular level, but also insights to tackle the existing challenges. View Full-Text
Keywords: binding interaction; galectin; inhibitor; isothermal titration calorimetry; NMR (Nuclear Magnetic Resonance); thiodigalactoside; X-ray crystallography binding interaction; galectin; inhibitor; isothermal titration calorimetry; NMR (Nuclear Magnetic Resonance); thiodigalactoside; X-ray crystallography
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Chan, Y.-C.; Lin, H.-Y.; Tu, Z.; Kuo, Y.-H.; Hsu, S.-T.D.; Lin, C.-H. Dissecting the Structure–Activity Relationship of Galectin–Ligand Interactions. Int. J. Mol. Sci. 2018, 19, 392.

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