Paul R J Davey
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Explore the profile of Paul R J Davey including associated specialties, affiliations and a list of published articles.
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7
Citations
83
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Recent Articles
1.
Scott J, Stead D, Barlaam B, Breed J, Carbajo R, Chiarparin E, et al.
J Med Chem
. 2023 Feb;
66(4):2918-2945.
PMID: 36727211
Herein, we report the optimization of a meta-substituted series of selective estrogen receptor degrader (SERD) antagonists for the treatment of ER+ breast cancer. Structure-based design together with the use of...
2.
Winter-Holt J, Bardelle C, Chiarparin E, Dale I, Davey P, Davies N, et al.
J Med Chem
. 2022 Feb;
65(4):3306-3331.
PMID: 35133824
ATAD2 is an epigenetic bromodomain-containing target which is overexpressed in many cancers and has been suggested as a potential oncology target. While several small molecule inhibitors have been described in...
3.
Wendt M, Bellavita R, Gerber A, Efrem N, van Ramshorst T, Pearce N, et al.
Angew Chem Int Ed Engl
. 2021 Mar;
60(25):13937-13944.
PMID: 33783110
Protein complexes are defined by the three-dimensional structure of participating binding partners. Knowledge about these structures can facilitate the design of peptidomimetics which have been applied for example, as inhibitors...
4.
Scott J, Moss T, Barlaam B, Davey P, Fairley G, Gangl E, et al.
ACS Med Chem Lett
. 2020 Dec;
11(12):2519-2525.
PMID: 33335676
Herein we describe our efforts using a late stage functionalization together with more traditional synthetic approaches to generate fluorinated analogues of the clinical candidate AZD9833. The effects of the addition...
5.
Eddershaw A, Stubbs C, Edwardes L, Underwood E, Hamm G, Davey P, et al.
Biochemistry
. 2020 Dec;
59(50):4775-4786.
PMID: 33274632
Protein arginine methyltransferases (PRMTs) are of great interest for the development of therapeutics due to their involvement in a number of malignancies, such as lung and colon cancer. PRMT5 catalyzes...
6.
Scott J, Moss T, Balazs A, Barlaam B, Breed J, Carbajo R, et al.
J Med Chem
. 2020 Sep;
63(23):14530-14559.
PMID: 32910656
Herein we report the optimization of a series of tricyclic indazoles as selective estrogen receptor degraders (SERD) and antagonists for the treatment of ER breast cancer. Structure based design together...
7.
Scott J, Bailey A, Buttar D, Carbajo R, Curwen J, Davey P, et al.
J Med Chem
. 2019 Jan;
62(3):1593-1608.
PMID: 30640465
Herein, we report the identification and synthesis of a series of tricyclic indazoles as a novel class of selective estrogen receptor degrader antagonists. Replacement of a phenol, present in our...