Literature DB >> 9359109

Structure-based design and characterization of exocyclic peptidomimetics that inhibit TNF alpha binding to its receptor.

W Takasaki1, Y Kajino, K Kajino, R Murali, M I Greene.   

Abstract

Exocyclic small peptidomimetics corresponding to three critical binding sites of tumor necrosis factor (TNF)-receptor(I) have been designed based on atomic features deduced from the crystal structures of TNF alpha and the TNF beta/TNF-receptor(I) complex and a model of an anti-TNF alpha monoclonal antibody. TNF alpha antagonistic activities were evaluated by binding assays using soluble receptor or intact receptor on cells as well as an apoptosis/cytotoxicity assay. The most critical interaction site for rational design of peptidomimetics was localized to the loop1/domain3 of the TNF-receptor. The best antagonist showed 5 microM inhibition in the binding assay. Biologically, the mimetics inhibited TNF alpha-mediated apoptosis.

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Year:  1997        PMID： 9359109     DOI： 10.1038/nbt1197-1266

Source DB:  PubMed          Journal:  Nat Biotechnol        ISSN： 1087-0156            Impact factor:   54.908


  41 in total

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7.  A novel small-molecule tumor necrosis factor α inhibitor attenuates inflammation in a hepatitis mouse model.

Authors:  Li Ma; Haiyan Gong; Haiyan Zhu; Qing Ji; Pei Su; Peng Liu; Shannan Cao; Jianfeng Yao; Linlin Jiang; Mingzhe Han; Xiaotong Ma; Dongsheng Xiong; Hongbo R Luo; Fei Wang; Jiaxi Zhou; Yuanfu Xu
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8.  A TNF receptor loop peptide mimic blocks RANK ligand-induced signaling, bone resorption, and bone loss.

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9.  Fas-disabling small exocyclic peptide mimetics limit apoptosis by an unexpected mechanism.

Authors:  Akihiro Hasegawa; Xin Cheng; Kiichi Kajino; Alan Berezov; Kaoru Murata; Toshinori Nakayama; Hideo Yagita; Ramachandran Murali; Mark I Greene
Journal:  Proc Natl Acad Sci U S A       Date:  2004-04-14       Impact factor: 11.205

10.  Thermodynamic additivity of sequence variations: an algorithm for creating high affinity peptides without large libraries or structural information.

Authors:  Matthew P Greving; Paul E Belcher; Chris W Diehnelt; Maria J Gonzalez-Moa; Jack Emery; Jinglin Fu; Stephen Albert Johnston; Neal W Woodbury
Journal:  PLoS One       Date:  2010-11-11       Impact factor: 3.240
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