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024 7 _ |a 10.1517/17460441.2016.1107041
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024 7 _ |a 1746-0441
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024 7 _ |a 1746-045X
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037 _ _ |a DZNE-2020-04636
041 _ _ |a English
082 _ _ |a 610
100 1 _ |a Ambadipudi, Susmitha
|0 P:(DE-2719)2811405
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|e First author
|u dzne
245 _ _ |a Targeting intrinsically disordered proteins in rational drug discovery.
260 _ _ |a Abingdon
|c 2016
|b Taylor & Francis Group
264 _ 1 |3 online
|2 Crossref
|b Informa Healthcare
|c 2015-11-07
264 _ 1 |3 print
|2 Crossref
|b Informa Healthcare
|c 2016-01-02
336 7 _ |a article
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520 _ _ |a Intrinsically disordered proteins (IDPs) and intrinsically disordered protein regions (IDPRs) have gained wide recognition over the past decade due to their versatile roles in cell physiology and pathology. A large repertoire of IDPs/IDPRs has been implicated in numerous diseases, making them potential targets for therapeutic intervention. Recent advances in experimental methods and computational approaches have enabled detection and characterization of these highly dynamic proteins at atomistic detail, thus facilitating disorder/dynamic-based drug discovery.This article presents an overview of the functional relevance and pathological implications of IDPs/IDPRs in cells. The authors outline the currently available experimental methods employed for structural characterization of these proteins. They also exemplify the practical limitations encountered during such characterization and ways to overcome them. Taken together, the article discusses the plausibility of exploiting protein disorder for drug targeting.Disorder-based drug targeting is gearing up in the realm of novel drug discovery approaches. Tools for probing the molecular features of IDPs and IDPRs are rapidly improving and start to provide accurate descriptions of the complex ensembles populated by IDPs/IDPRs. They thus pave the way for the development of drug molecules, which specifically target disease-associated disorder.
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542 _ _ |i 2015-11-07
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588 _ _ |a Dataset connected to CrossRef, PubMed,
650 _ 7 |a Intrinsically Disordered Proteins
|2 NLM Chemicals
650 _ 2 |a Animals
|2 MeSH
650 _ 2 |a Drug Design
|2 MeSH
650 _ 2 |a Drug Discovery: methods
|2 MeSH
650 _ 2 |a Humans
|2 MeSH
650 _ 2 |a Intrinsically Disordered Proteins: metabolism
|2 MeSH
650 _ 2 |a Models, Molecular
|2 MeSH
650 _ 2 |a Molecular Targeted Therapy
|2 MeSH
650 _ 2 |a Protein Conformation
|2 MeSH
700 1 _ |a Zweckstetter, Markus
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773 1 8 |a 10.1517/17460441.2016.1107041
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773 _ _ |a 10.1517/17460441.2016.1107041
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|t Papers of special note have been highlighted as either of interest (•) or of considerable interest (••) to readers
|o Papers of special note have been highlighted as either of interest (•) or of considerable interest (••) to readers
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LibraryCollectionCLSMajorCLSMinorLanguageAuthor
Marc 21