Literature DB >> 17448658

Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.

Michael Johnson1, An-Rong Li, Jiwen Liu, Zice Fu, Liusheng Zhu, Shichang Miao, Xuemei Wang, Qingge Xu, Alan Huang, Andrew Marcus, Feng Xu, Karen Ebsworth, Emmanuel Sablan, Jay Danao, Jeff Kumer, Dan Dairaghi, Chris Lawrence, Tim Sullivan, George Tonn, Thomas Schall, Tassie Collins, Julio Medina.   

Abstract

A series of quinazolinone-derived inhibitors of the CXCR3 receptor have been synthesized and their affinity for the receptor evaluated. Compounds were evaluated in a (125)I-IP10 displacement assay and in in vitro cell migration assays to IP10, ITAC, and MIG using human peripheral blood mononuclear cells.

Entities:  

Mesh:

Substances:

Year:  2007        PMID: 17448658     DOI: 10.1016/j.bmcl.2007.03.106

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


  22 in total

1.  A combined LS-SVM & MLR QSAR workflow for predicting the inhibition of CXCR3 receptor by quinazolinone analogs.

Authors:  Antreas Afantitis; Georgia Melagraki; Haralambos Sarimveis; Panayiotis A Koutentis; Olga Igglessi-Markopoulou; George Kollias
Journal:  Mol Divers       Date:  2009-05-30       Impact factor: 2.943

2.  CXCL10 and its receptor CXCR3 regulate synovial fibroblast invasion in rheumatoid arthritis.

Authors:  Teresina Laragione; Max Brenner; Barbara Sherry; Pércio S Gulko
Journal:  Arthritis Rheum       Date:  2011-11

3.  Cyclosporin but not everolimus inhibits chemokine receptor expression on CD4+ T cell subsets circulating in the peripheral blood of renal transplant recipients.

Authors:  A Hoerning; S Köhler; C Jun; J Lu; J Fu; B Tebbe; S Dolff; T Feldkamp; A Kribben; P F Hoyer; O Witzke
Journal:  Clin Exp Immunol       Date:  2012-05       Impact factor: 4.330

4.  Expression and agonist responsiveness of CXCR3 variants in human T lymphocytes.

Authors:  Anna Korniejewska; Andrew J McKnight; Zoë Johnson; Malcolm L Watson; Stephen G Ward
Journal:  Immunology       Date:  2011-01-24       Impact factor: 7.397

Review 5.  Chemokine receptor antagonists: overcoming developmental hurdles.

Authors:  Richard Horuk
Journal:  Nat Rev Drug Discov       Date:  2008-12-12       Impact factor: 84.694

6.  Noncompetitive antagonism and inverse agonism as mechanism of action of nonpeptidergic antagonists at primate and rodent CXCR3 chemokine receptors.

Authors:  Dennis Verzijl; Stefania Storelli; Danny J Scholten; Leontien Bosch; Todd A Reinhart; Daniel N Streblow; Cornelis P Tensen; Carlos P Fitzsimons; Guido J R Zaman; James E Pease; Iwan J P de Esch; Martine J Smit; Rob Leurs
Journal:  J Pharmacol Exp Ther       Date:  2008-02-12       Impact factor: 4.030

7.  Gene expression analysis of host innate immune responses during Lethal H5N1 infection in ferrets.

Authors:  Cheryl M Cameron; Mark J Cameron; Jesus F Bermejo-Martin; Longsi Ran; Luoling Xu; Patricia V Turner; Ran Ran; Ali Danesh; Yuan Fang; Pak-Kei M Chan; Nutan Mytle; Timothy J Sullivan; Tassie L Collins; Michael G Johnson; Julio C Medina; Thomas Rowe; David J Kelvin
Journal:  J Virol       Date:  2008-08-06       Impact factor: 5.103

8.  Critical Role of the CXCL10/C-X-C Chemokine Receptor 3 Axis in Promoting Leukocyte Recruitment and Neuronal Injury during Traumatic Optic Neuropathy Induced by Optic Nerve Crush.

Authors:  Yonju Ha; Hua Liu; Shuang Zhu; Panpan Yi; Wei Liu; Jared Nathanson; Rakez Kayed; Bradford Loucas; Jiaren Sun; Laura J Frishman; Massoud Motamedi; Wenbo Zhang
Journal:  Am J Pathol       Date:  2016-12-10       Impact factor: 4.307

9.  CXCR3 antagonism impairs the development of donor-reactive, IFN-gamma-producing effectors and prolongs allograft survival.

Authors:  Joshua M Rosenblum; Qi-Wei Zhang; Gerald Siu; Tassie L Collins; Timothy Sullivan; Daniel J Dairaghi; Julio C Medina; Robert L Fairchild
Journal:  Transplantation       Date:  2009-02-15       Impact factor: 4.939

10.  Inhibition of CXCR3-mediated chemotaxis by the human chemokine receptor-like protein CCX-CKR.

Authors:  J Vinet; M van Zwam; I M Dijkstra; N Brouwer; H R J van Weering; A Watts; M Meijer; M R Fokkens; V Kannan; D Verzijl; H F Vischer; M J Smit; R Leurs; K Biber; H W G M Boddeke
Journal:  Br J Pharmacol       Date:  2013-03       Impact factor: 8.739

View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.