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      The Binding Center of Leucine Aminopeptidase

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          Abstract

          As shown by kinetic experiments with competitive inhibitors like Thr(Bu<sup>t</sup>)-Phe-X peptide ligands are bound by hydrophobic interactions at two nonpolar subsites S<sub>1</sub> and S<sub>2</sub>. This contact region prefers with high selectivity L-configuration in P<sub>1</sub> and P<sub>2</sub> position. The additional binding P<sub>3</sub>-S<sub>3</sub> differs in polarity and stereospecifical requirement. The nitroxide-labelled inhibitor Thr(Bu<sup>t</sup> > Phe-SL is competitively bound at two types of binding sites. The main type, obtained from electron spin resonance spectroscopy, is in agreement with results from kinetic studies and represents the binding of two inhibitor molecules per subunit of the enzyme.

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          Author and article information

          Journal
          ORE
          Ophthalmic Res
          10.1159/issn.0030-3747
          Ophthalmic Research
          S. Karger AG
          978-3-8055-0862-9
          978-3-318-02127-1
          0030-3747
          1423-0259
          1979
          1979
          03 December 2009
          : 11
          : 5-6
          : 381-385
          Affiliations
          Institute of Physiological Chemistry, Martin Luther University, Halle/Saale, and Central Institute for Molecular Biology, Academy of Science, Berlin-Buch
          Article
          265038 Ophthalmic Res 1979;11:381–385
          10.1159/000265038
          8c0a1d0f-92fa-406b-9ebb-c9c91b3aa75e
          © 1979 S. Karger AG, Basel

          Copyright: All rights reserved. No part of this publication may be translated into other languages, reproduced or utilized in any form or by any means, electronic or mechanical, including photocopying, recording, microcopying, or by any information storage and retrieval system, without permission in writing from the publisher. Drug Dosage: The authors and the publisher have exerted every effort to ensure that drug selection and dosage set forth in this text are in accord with current recommendations and practice at the time of publication. However, in view of ongoing research, changes in government regulations, and the constant flow of information relating to drug therapy and drug reactions, the reader is urged to check the package insert for each drug for any changes in indications and dosage and for added warnings and precautions. This is particularly important when the recommended agent is a new and/or infrequently employed drug. Disclaimer: The statements, opinions and data contained in this publication are solely those of the individual authors and contributors and not of the publishers and the editor(s). The appearance of advertisements or/and product references in the publication is not a warranty, endorsement, or approval of the products or services advertised or of their effectiveness, quality or safety. The publisher and the editor(s) disclaim responsibility for any injury to persons or property resulting from any ideas, methods, instructions or products referred to in the content or advertisements.

          History
          Page count
          Pages: 5
          Categories
          Growth Control, Differentiation, and Ageing of the Eye Lens

          Vision sciences,Ophthalmology & Optometry,Pathology
          Leucine aminopeptidase,Binding site,Competitive inhibitors,Spin-labεlled compounds,Active center

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