Literature DB >> 15454236

Small molecule antagonists of the CCR2b receptor. Part 2: Discovery process and initial structure-activity relationships of diamine derivatives.

Wilna J Moree1, Ken-ichiro Kataoka, Michele M Ramirez-Weinhouse, Tatsuki Shiota, Minoru Imai, Masaki Sudo, Takaharu Tsutsumi, Noriaki Endo, Yumiko Muroga, Takahiko Hada, Hiroko Tanaka, Takuya Morita, Jonathan Greene, Doug Barnum, John Saunders, Yoshinori Kato, Peter L Myers, Christine M Tarby.   

Abstract

Structure-activity relationships (SAR) of a weakly active class of CCR2b inhibitors were utilized to initiate a lead evolution program employing the Drug Discovery Engine. Several alternative structural series have been discovered that display nanomolar activity in the CCR2b binding and CCR2b-mediated chemotaxis assays.

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Year:  2004        PMID: 15454236     DOI: 10.1016/j.bmcl.2004.08.009

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


  2 in total

1.  Ligand supported homology modeling and docking evaluation of CCR2: docked pose selection by consensus scoring.

Authors:  Jong-Hoon Kim; Jee Woong Lim; Seung-Woo Lee; Kyoungrak Kim; Kyoung Tai No
Journal:  J Mol Model       Date:  2011-01-07       Impact factor: 1.810

2.  Targeted delivery of CCR2 antagonist to activated pulmonary endothelium prevents metastasis.

Authors:  Marko Roblek; Manuela Calin; Martin Schlesinger; Daniela Stan; Reiner Zeisig; Maya Simionescu; Gerd Bendas; Lubor Borsig
Journal:  J Control Release       Date:  2015-10-30       Impact factor: 9.776

  2 in total

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