Small-molecule inhibitors of protein-protein interactions

Zhiqing Liu, H. Chen, E. A. Wold, Jia Zhou

Research output: Chapter in Book/Report/Conference proceedingChapter

2 Citations (Scopus)

Abstract

Targeting protein-protein interactions (PPIs) for therapeutic development was once considered undruggable due to the large and flat interactive surfaces that lack cavities. Facilitated by the development of new concepts, such as hotspots, screening techniques, and computational tools, various small molecules modulating PPIs have been achieved with a number of them having progressed into different phases of clinical trials and a portion recently reaching the market. In this article, we discuss the critical role of PPIs associated with various human diseases and different approaches to the identification of small molecular inhibitors targeting PPIs. We also highlight recent advances in developing such modulators as novel therapeutics.

Original languageEnglish (US)
Title of host publicationDrug Discovery Technologies
PublisherElsevier Inc.
Pages329-353
Number of pages25
Volume2-8
ISBN (Electronic)9780128032008
ISBN (Print)9780128032015
DOIs
StatePublished - Jun 3 2017

Fingerprint

Molecules
Proteins
Modulators
Screening

Keywords

  • Allosteric sites
  • Cancer therapy
  • CNS disorders
  • Drug development
  • Drug discovery
  • Drug target
  • Fragment-based drug design
  • High-throughput screening
  • Hotspots
  • Inflammation
  • Interactive surface
  • Peptidomimetics
  • Protein-protein interaction inhibitors
  • Protein-protein interactions
  • Virtual screening

ASJC Scopus subject areas

  • Chemistry(all)

Cite this

Liu, Z., Chen, H., Wold, E. A., & Zhou, J. (2017). Small-molecule inhibitors of protein-protein interactions. In Drug Discovery Technologies (Vol. 2-8, pp. 329-353). Elsevier Inc.. https://doi.org/10.1016/B978-0-12-409547-2.12326-1

Small-molecule inhibitors of protein-protein interactions. / Liu, Zhiqing; Chen, H.; Wold, E. A.; Zhou, Jia.

Drug Discovery Technologies. Vol. 2-8 Elsevier Inc., 2017. p. 329-353.

Research output: Chapter in Book/Report/Conference proceedingChapter

Liu, Z, Chen, H, Wold, EA & Zhou, J 2017, Small-molecule inhibitors of protein-protein interactions. in Drug Discovery Technologies. vol. 2-8, Elsevier Inc., pp. 329-353. https://doi.org/10.1016/B978-0-12-409547-2.12326-1
Liu Z, Chen H, Wold EA, Zhou J. Small-molecule inhibitors of protein-protein interactions. In Drug Discovery Technologies. Vol. 2-8. Elsevier Inc. 2017. p. 329-353 https://doi.org/10.1016/B978-0-12-409547-2.12326-1
Liu, Zhiqing ; Chen, H. ; Wold, E. A. ; Zhou, Jia. / Small-molecule inhibitors of protein-protein interactions. Drug Discovery Technologies. Vol. 2-8 Elsevier Inc., 2017. pp. 329-353
@inbook{36b70437e9cb4fef8ae37e3d40df95aa,
title = "Small-molecule inhibitors of protein-protein interactions",
abstract = "Targeting protein-protein interactions (PPIs) for therapeutic development was once considered undruggable due to the large and flat interactive surfaces that lack cavities. Facilitated by the development of new concepts, such as hotspots, screening techniques, and computational tools, various small molecules modulating PPIs have been achieved with a number of them having progressed into different phases of clinical trials and a portion recently reaching the market. In this article, we discuss the critical role of PPIs associated with various human diseases and different approaches to the identification of small molecular inhibitors targeting PPIs. We also highlight recent advances in developing such modulators as novel therapeutics.",
keywords = "Allosteric sites, Cancer therapy, CNS disorders, Drug development, Drug discovery, Drug target, Fragment-based drug design, High-throughput screening, Hotspots, Inflammation, Interactive surface, Peptidomimetics, Protein-protein interaction inhibitors, Protein-protein interactions, Virtual screening",
author = "Zhiqing Liu and H. Chen and Wold, {E. A.} and Jia Zhou",
year = "2017",
month = "6",
day = "3",
doi = "10.1016/B978-0-12-409547-2.12326-1",
language = "English (US)",
isbn = "9780128032015",
volume = "2-8",
pages = "329--353",
booktitle = "Drug Discovery Technologies",
publisher = "Elsevier Inc.",

}

TY - CHAP

T1 - Small-molecule inhibitors of protein-protein interactions

AU - Liu, Zhiqing

AU - Chen, H.

AU - Wold, E. A.

AU - Zhou, Jia

PY - 2017/6/3

Y1 - 2017/6/3

N2 - Targeting protein-protein interactions (PPIs) for therapeutic development was once considered undruggable due to the large and flat interactive surfaces that lack cavities. Facilitated by the development of new concepts, such as hotspots, screening techniques, and computational tools, various small molecules modulating PPIs have been achieved with a number of them having progressed into different phases of clinical trials and a portion recently reaching the market. In this article, we discuss the critical role of PPIs associated with various human diseases and different approaches to the identification of small molecular inhibitors targeting PPIs. We also highlight recent advances in developing such modulators as novel therapeutics.

AB - Targeting protein-protein interactions (PPIs) for therapeutic development was once considered undruggable due to the large and flat interactive surfaces that lack cavities. Facilitated by the development of new concepts, such as hotspots, screening techniques, and computational tools, various small molecules modulating PPIs have been achieved with a number of them having progressed into different phases of clinical trials and a portion recently reaching the market. In this article, we discuss the critical role of PPIs associated with various human diseases and different approaches to the identification of small molecular inhibitors targeting PPIs. We also highlight recent advances in developing such modulators as novel therapeutics.

KW - Allosteric sites

KW - Cancer therapy

KW - CNS disorders

KW - Drug development

KW - Drug discovery

KW - Drug target

KW - Fragment-based drug design

KW - High-throughput screening

KW - Hotspots

KW - Inflammation

KW - Interactive surface

KW - Peptidomimetics

KW - Protein-protein interaction inhibitors

KW - Protein-protein interactions

KW - Virtual screening

UR - http://www.scopus.com/inward/record.url?scp=85046114971&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=85046114971&partnerID=8YFLogxK

U2 - 10.1016/B978-0-12-409547-2.12326-1

DO - 10.1016/B978-0-12-409547-2.12326-1

M3 - Chapter

SN - 9780128032015

VL - 2-8

SP - 329

EP - 353

BT - Drug Discovery Technologies

PB - Elsevier Inc.

ER -