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@ARTICLE{Ambadipudi:138314,
author = {Ambadipudi, Susmitha and Zweckstetter, Markus},
title = {{T}argeting intrinsically disordered proteins in rational
drug discovery.},
journal = {Expert opinion on drug discovery},
volume = {11},
number = {1},
issn = {1746-0441},
address = {Abingdon},
publisher = {Taylor $\&$ Francis Group},
reportid = {DZNE-2020-04636},
pages = {65-77},
year = {2016},
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.},
subtyp = {Review Article},
keywords = {Animals / Drug Design / Drug Discovery: methods / Humans /
Intrinsically Disordered Proteins: metabolism / Models,
Molecular / Molecular Targeted Therapy / Protein
Conformation / Intrinsically Disordered Proteins (NLM
Chemicals)},
cin = {AG Zweckstetter},
ddc = {610},
cid = {I:(DE-2719)1410001},
pnm = {342 - Disease Mechanisms and Model Systems (POF3-342)},
pid = {G:(DE-HGF)POF3-342},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:26549326},
doi = {10.1517/17460441.2016.1107041},
url = {https://pub.dzne.de/record/138314},
}