Abstract:
:Using a biologically relevant peptide or protein structure as a starting point for lead identification represents one of the most powerful approaches in modern drug discovery. Here, we focus on the protein epitope mimetic (PEM) approach, where folded 3D structures of peptides and proteins are taken as starting points for the design of synthetic molecules that mimic key epitopes involved in protein-protein and protein-nucleic acid interactions. By transferring the epitope from a recombinant to a synthetic scaffold that can be produced by parallel combinatorial methods, it is possible to optimize target affinity and specificity as well as other drug-like ADMET properties. The PEM technology is a powerful tool for target validation, and for the development of novel PEM-based drugs.
journal_name
Drug Discov Todayjournal_title
Drug discovery todayauthors
Robinson JA,Demarco S,Gombert F,Moehle K,Obrecht Ddoi
10.1016/j.drudis.2008.07.008subject
Has Abstractpub_date
2008-11-01 00:00:00pages
944-51issue
21-22eissn
1359-6446issn
1878-5832pii
S1359-6446(08)00276-6journal_volume
13pub_type
杂志文章,评审abstract::Post-translational modifications, such as acetylation or phosphorylation, play a crucial role in the regulation of gene transcription in eukaryotes. Different subtypes of histone acetyl transferases (HATs) catalyze the acetylation of histones on specific lysine residues. A potential role of HATs in the pathology of ca...
journal_title:Drug discovery today
pub_type: 杂志文章,评审
doi:10.1016/j.drudis.2009.06.008
更新日期:2009-10-01 00:00:00
abstract::Immunoinformatics has recently emerged as a critical field for accelerating immunology research. Although still an evolving process, computational models now play instrumental roles, not only in directing the selection of key experiments, but also in the formulation of new testable hypotheses through detailed analysis...
journal_title:Drug discovery today
pub_type: 杂志文章,评审
doi:10.1016/j.drudis.2009.04.001
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journal_title:Drug discovery today
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journal_title:Drug discovery today
pub_type: 杂志文章,评审
doi:10.1016/j.drudis.2014.10.001
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journal_title:Drug discovery today
pub_type: 杂志文章,评审
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journal_title:Drug discovery today
pub_type: 杂志文章,评审
doi:10.1016/j.drudis.2018.09.003
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journal_title:Drug discovery today
pub_type: 杂志文章,评审
doi:10.1016/j.drudis.2007.07.024
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abstract::Annotating the druggable genome estimates the potential maximum size of the playing field for current small-molecule drug design but It does not consider biologicals or future breakthroughs in medicinal chemistry or biology. ...
journal_title:Drug discovery today
pub_type: 杂志文章
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更新日期:2005-12-01 00:00:00
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journal_title:Drug discovery today
pub_type: 杂志文章,评审
doi:10.1016/j.drudis.2017.09.009
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journal_title:Drug discovery today
pub_type: 杂志文章,评审
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journal_title:Drug discovery today
pub_type: 新闻
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更新日期:2003-03-15 00:00:00
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journal_title:Drug discovery today
pub_type: 历史文章,杂志文章
doi:10.1016/j.drudis.2008.07.002
更新日期:2009-02-01 00:00:00
abstract::Functional proteomics approaches aim to characterize comprehensively the function of gene products, and provide a first-level understanding of cellular mechanisms. Here, we review recent techniques for the construction and prediction of large-scale protein-interaction networks, with a particular emphasis on computatio...
journal_title:Drug discovery today
pub_type: 杂志文章,评审
doi:10.1016/s1359-6446(02)02281-x
更新日期:2002-06-01 00:00:00
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journal_title:Drug discovery today
pub_type: 历史文章,杂志文章
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更新日期:2017-05-01 00:00:00
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journal_title:Drug discovery today
pub_type: 杂志文章
doi:10.1016/S1359-6446(05)03650-0
更新日期:2005-11-15 00:00:00
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journal_title:Drug discovery today
pub_type: 杂志文章
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更新日期:2017-06-01 00:00:00
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journal_title:Drug discovery today
pub_type: 杂志文章,评审
doi:10.1016/j.drudis.2018.01.005
更新日期:2018-05-01 00:00:00
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journal_title:Drug discovery today
pub_type: 杂志文章
doi:10.1016/j.drudis.2014.09.001
更新日期:2016-01-01 00:00:00
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journal_title:Drug discovery today
pub_type: 杂志文章,评审
doi:10.1016/j.drudis.2020.07.003
更新日期:2020-09-01 00:00:00
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journal_title:Drug discovery today
pub_type: 杂志文章,评审
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journal_title:Drug discovery today
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journal_title:Drug discovery today
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journal_title:Drug discovery today
pub_type: 杂志文章,评审
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journal_title:Drug discovery today
pub_type: 杂志文章,评审
doi:10.1016/j.drudis.2010.11.007
更新日期:2011-01-01 00:00:00
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journal_title:Drug discovery today
pub_type: 杂志文章,评审
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更新日期:2004-04-01 00:00:00
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journal_title:Drug discovery today
pub_type: 杂志文章
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journal_title:Drug discovery today
pub_type: 杂志文章,评审
doi:10.1016/j.drudis.2016.04.005
更新日期:2016-08-01 00:00:00
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journal_title:Drug discovery today
pub_type: 杂志文章,评审
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更新日期:2006-07-01 00:00:00
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journal_title:Drug discovery today
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更新日期:2013-04-01 00:00:00
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journal_title:Drug discovery today
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