Identification of β-strand mediated protein–protein interaction inhibitors using ligand-directed fragment ligation-Reference-Cited by-同舟云学术

Identification of β-strand mediated protein–protein interaction inhibitors using ligand-directed fragment ligation

Published:2021 Issue:6 Volume:12 Page:2286-2293
ISSN:2041-6520
Container-title:Chemical Science
language:en
Short-container-title:Chem. Sci.

Author:

Hegedüs Zsófia¹²³⁴^ORCID,Hóbor Fruzsina⁵²³⁴⁶^ORCID,Shoemark Deborah K.⁷⁸⁹¹⁰⁴^ORCID,Celis Sergio¹²³⁴^ORCID,Lian Lu-Yun¹¹¹²¹³¹⁴⁴^ORCID,Trinh Chi H.⁵²³⁴⁶^ORCID,Sessions Richard B.⁷⁸⁹¹⁰⁴^ORCID,Edwards Thomas A.⁵²³⁴⁶^ORCID,Wilson Andrew J.¹²³⁴⁵^ORCID

Affiliation:

1. School of Chemistry

2. University of Leeds

3. Leeds LS2 9JT

4. UK

5. Astbury Centre for Structural Molecular Biology

6. School of Molecular and Cellular Biology

7. School of Biochemistry

8. Biomedical Sciences Building

9. University of Bristol

10. Bristol

11. Institute of Systems

12. Molecular and Integrative Biology

13. University of Liverpool

14. Liverpool L69 3BX

Abstract

Dynamic ligation screening is used to identify acylhydrazone-linked peptide-fragment hybrids which bind to the SHANK1 PDZ domain with comparable affinity to the native GKAP peptide as shown by biophysical and structural analyses.

Funder

H2020 Marie Skłodowska-Curie Actions

Engineering and Physical Sciences Research Council

Royal Society

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2021/SC/D0SC05694D

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1. Allostery in Disease and in Drug Discovery