Journal Article (Review Article)

DZNE-2020-04636

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png Targeting intrinsically disordered proteins in rational drug discovery.

Ambadipudi, S. (First author)DZNE* ; Zweckstetter, M. (Last author)DZNE*

2016
Taylor & Francis Group Abingdon

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Please use a persistent id in citations: doi:10.1517/17460441.2016.1107041

Abstract: 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.

Keyword(s): Animals (MeSH) ; Drug Design (MeSH) ; Drug Discovery: methods (MeSH) ; Humans (MeSH) ; Intrinsically Disordered Proteins: metabolism (MeSH) ; Models, Molecular (MeSH) ; Molecular Targeted Therapy (MeSH) ; Protein Conformation (MeSH) ; Intrinsically Disordered Proteins

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Contributing Institute(s):

1. Structural Biology in Dementia (AG Zweckstetter)

Research Program(s):

1. 342 - Disease Mechanisms and Model Systems (POF3-342) (POF3-342)

Appears in the scientific report 2016

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Database coverage:
; ; ; Clarivate Analytics Master Journal List ; Current Contents - Life Sciences ; IF < 5 ; JCR ; NCBI Molecular Biology Database ; Nationallizenz ; SCOPUS ; Science Citation Index Expanded ; Web of Science Core Collection

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