Identification of non-conventional small molecule degraders and stabilizers of squalene synthase-Reference-Cited by-同舟云学术

Identification of non-conventional small molecule degraders and stabilizers of squalene synthase

Published:2023 Issue:45 Volume:14 Page:12973-12983
ISSN:2041-6520
Container-title:Chemical Science
language:en
Short-container-title:Chem. Sci.

Author:

Hoock Joseph G. F.¹^ORCID,Rossetti Cecilia¹,Bilgin Mesut²,Depta Laura¹^ORCID,Enemark-Rasmussen Kasper¹,Christianson John C.³,Laraia Luca¹^ORCID

Affiliation:

1. Department of Chemistry, Technical University of Denmark, Kemitorvet 207, Kongens Lyngby 2800, Denmark

2. Lipidomics Core Facility, Danish Cancer Institute, Strandboulevarden 49, Copenhagen 2100, Denmark

3. Nuffield Department of Rheumatology, Orthopaedics, and Musculoskeletal Sciences, Botnar Research Centre, University of Oxford, Headington, Oxford OX3 7LD, UK

Abstract

Small molecule degraders and stabilizers of squalene synthase based on the same scaffold are reported, which respectively accelerate or block its natural degradation.

Funder

Novo Nordisk Fonden

Danmarks Frie Forskningsfond

Cancer Research UK

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2023/SC/D3SC04064J

Reference50 articles.

1. Structural insights into the catalytic mechanism of human squalene synthase

2. R.Heidasch , D.Avci , C.Lüchtenborg , D.Kale , H.Beard , T.Mentrup , M.Barniol-Xicota , B.Schröder , S.Verhelst , B.Brügger and M. K.Lemberg , 2022, preprint , 10.1101/2021.07.19.452877

3. Chemical Genetics Reveals a Role of Squalene Synthase in TGFβ Signaling and Cardiomyogenesis

4. Plasma cholesterol-lowering and transient liver dysfunction in mice lacking squalene synthase in the liver

5. Squalene Synthase Deficiency: Clinical, Biochemical, and Molecular Characterization of a Defect in Cholesterol Biosynthesis