tailieunhanh - báo cáo khoa hoc : Inhibition mechanism of human galectin-7 by a novel galactose-benzylphosphate inhibitor

Galectins are involved in many cellular processes due to their ability to bind carbohydrates. Understanding their functions has shown the necessity for potent and specific galectin inhibitors. Human galectin-7 (hGal-7), in particular, has been highlighted as an important marker in many types of cancer by either inhibiting or promoting tumour growth. | IFEBS Journal Inhibition mechanism of human galectin-7 by a novel galactose-benzylphosphate inhibitor rr It JI 1 -I- I . I I 1 I-. I -I- A I 2 I m 3iiiriki-i 2 I Geoffrey Masuyer Talat Jabeen Christopher T. Oberg Hakon Leffler Ulf J. Nilsson and K. Ravi Acharya1 1 Department of Biology and Biochemistry University of Bath UK 2 Organic Chemistry Lund University Sweden 3 Section MIG Department of Laboratory Medicine Lund University Sweden Keywords drug design galactoside inhibitor galectin-7 lectin Galectins are involved in many cellular processes due to their ability to bind carbohydrates. Understanding their functions has shown the necessity for potent and specific galectin inhibitors. Human galectin-7 hGal-7 in Correspondence K. R. Acharya Department of Biology and Biochemistry University of Bath Claverton Down Bath BA2 7AY UK Fax 44 1225 386779 Tel 44 1225 386238 E-mail bsskra@ particular has been highlighted as an important marker in many types of cancer by either inhibiting or promoting tumour growth. Producing ligands able to selectively target hGal-7 will offer promising tools for deciphering cancer processes in which hGal-7 is involved as well as present potential solutions for future therapeutics. Here we report the high resolution crystal structure of hGal-7 in complex with a synthetic 2-O-benzylphosphate-galac-toside inhibitor which is 60-fold more potent than its parent galacto- Re-use of this article is permitted in accordance with the Terms and Conditions set out at http onlineopen OnlineOpen_Terms side . The high resolution crystallographic analysis highlights the validity of using saccharide derivatives conserving properties of the galactose binding while enhanced affinity and specificity is provided by the added phosphate group. This structural information will allow the design of further inhibitors with improved potency and specificity. Received 19 August 2011 revised 31 October 2011 accepted 2 November 2011 Database

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