Literature DB >> 22579418

Pharmacophore-based small molecule CXCR4 ligands.

Tetsuo Narumi1, Tomohiro Tanaka, Chie Hashimoto, Wataru Nomura, Haruo Aikawa, Akira Sohma, Kyoko Itotani, Miyako Kawamata, Tsutomu Murakami, Naoki Yamamoto, Hirokazu Tamamura.   

Abstract

Low molecular weight CXCR4 ligands were developed based on the peptide T140, which has previously been identified as a potent CXCR4 antagonist. Some compounds with naphthyl, fluorobenzyl and pyridyl moieties as pharmacophore groups in the molecule showed significant CXCR4-binding activity and anti-HIV activity. Structure-activity relationships were studied and characteristics of each of these three moieties necessary for CXCR4 binding were defined. In this way, CXCR4 ligands with two types of recognition modes for CXCR4 have been found.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 22579418     DOI: 10.1016/j.bmcl.2012.04.032

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

Review 1.  Structural Analysis of Chemokine Receptor-Ligand Interactions.

Authors:  Marta Arimont; Shan-Liang Sun; Rob Leurs; Martine Smit; Iwan J P de Esch; Chris de Graaf
Journal:  J Med Chem       Date:  2017-03-10       Impact factor: 7.446

2.  T140 blocks the SDF-1/CXCR4 signaling pathway and prevents cartilage degeneration in an osteoarthritis disease model.

Authors:  Kun Wang; Yanlin Li; Rui Han; Guofeng Cai; Chuan He; Guoliang Wang; Di Jia
Journal:  PLoS One       Date:  2017-04-20       Impact factor: 3.240

3.  Potential use of compounds from sea cucumbers as MDM2 and CXCR4 inhibitors to control cancer cell growth.

Authors:  Teresa Liliana Wargasetia; Sofy Permana; Nashi Widodo
Journal:  Exp Ther Med       Date:  2018-08-07       Impact factor: 2.447

  3 in total

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