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Discovery and optimisation of wt-RET/KDR-selective inhibitors of RET V804M kinase
DOI:
10.1021/acsmedchemlett.9b00615
Authors:
Rebecca
Newton
(Cancer Research UK Manchester Institute - University of Manchester)
,
Bohdan
Waszkowycz
(Cancer Research UK Manchester Institute - University of Manchester)
,
Chitra
Seewooruthun
(University of Leicester)
,
Daniel
Burschowsky
(University of Leicester)
,
Mark
Richards
(University of Leeds)
,
Samantha
Hitchin
(Cancer Research UK Manchester Institute - University of Manchester)
,
Habiba
Begum
(Cancer Research UK Manchester Institute - University of Manchester)
,
Amanda
Watson
(Cancer Research UK Manchester Institute - University of Manchester)
,
Eleanor
French
(Cancer Research UK Manchester Institute - University of Manchester)
,
Niall
Hamilton
(Cancer Research UK Manchester Institute - University of Manchester)
,
Stuart
Jones
(Cancer Research UK Manchester Institute - University of Manchester)
,
Li-Ying
Lin
(Leicester Drug Discovery & Diagnostics Centre)
,
Ian
Waddell
(Cancer Research UK Manchester Institute - University of Manchester)
,
Aude
Echalier
(University of Leicester)
,
Richard
Bayliss
(University of Leeds)
,
Allan M.
Jordan
(Cancer Research UK Manchester Institute - University of Manchester)
,
Donald
Ogilvie
(Cancer Research UK Manchester Institute - University of Manchester)
Co-authored by industrial partner:
No
Type:
Journal Paper
Journal:
Acs Medicinal Chemistry Letters
State:
Published (Approved)
Published:
February 2020
Diamond Proposal Number(s):
8997

Abstract: A combination of focussed library and virtual screening, hit expansion and rational design has resulted in the development of a series of inhibitors of RETV804M kinase, the anticipated drug-resistant mutant of RET kinase. These agents do not inhibit the wild-type isoforms of RET or KDR and therefore offer a potential adjunct to RET inhibitors currently undergoing clinical evaluation.
Journal Keywords: RET; KDR; kinase inhibitor; virtual screening
Diamond Keywords: Lung Cancer
Subject Areas:
Biology and Bio-materials,
Chemistry,
Medicine
Instruments:
I04-1-Macromolecular Crystallography (fixed wavelength)
,
I04-Macromolecular Crystallography
Added On:
02/03/2020 12:00
Documents:
fgh5dbddd.pdf
Discipline Tags:
Non-Communicable Diseases
Health & Wellbeing
Cancer
Biochemistry
Chemistry
Structural biology
Organic Chemistry
Drug Discovery
Life Sciences & Biotech
Technical Tags:
Diffraction
Macromolecular Crystallography (MX)