David Hargreaves
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Explore the profile of David Hargreaves including associated specialties, affiliations and a list of published articles.
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38
Citations
556
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Recent Articles
1.
McCoull W, Thomson C, Braybrooke E, Chan C, Colclough N, Cortes Gonzalez M, et al.
J Med Chem
. 2025 Jan;
68(3):3700-3748.
PMID: 39869768
Despite recent advances in the inhibition of EGFR (epidermal growth factor receptor), there remains a clinical need for new EGFR Exon20 insertion (Ex20Ins) inhibitors that spare EGFR WT. Herein, we...
2.
Palisse A, Cheung T, Blokhuis A, Cogswell T, Martins B, Riemens R, et al.
J Med Chem
. 2024 Dec;
67(24):22055-22079.
PMID: 39641779
BFL1, a member of the antiapoptotic BCL2 family, has been relatively understudied compared to its counterparts despite evidence of its overexpression in various hematological malignancies. Across two articles, we describe...
3.
Thomson C, Braybrooke E, Colclough N, Davies N, Floch N, Greenwood R, et al.
J Med Chem
. 2024 Sep;
PMID: 39340451
Herein, we report the optimization of a series of epidermal growth factor receptor (EGFR) Exon20 insertion (Ex20Ins) inhibitors using structure-based drug design (SBDD), leading to the discovery of compound ,...
4.
Lucas S, Blackwell J, Borjesson U, Hargreaves D, Milbradt A, Bostock M, et al.
J Med Chem
. 2024 Sep;
67(18):16455-16479.
PMID: 39291659
Bfl-1, a member of the Bcl-2 family of proteins, plays a crucial role in apoptosis regulation and has been implicated in cancer cell survival and resistance to venetoclax therapy. Due...
5.
Ormiston R, Hargreaves D
J Shoulder Elbow Surg
. 2024 Aug;
34(1):114-121.
PMID: 39142433
Background: Surgical techniques for terrible triad injuries developed 20 years ago. Good and excellent short- and medium-term functional results have been reported. No long-term (over 10 years) functional outcomes have...
6.
Lucas S, Milbradt A, Blackwell J, Bonomo S, Brierley A, Cassar D, et al.
J Med Chem
. 2024 Jun;
67(13):11209-11225.
PMID: 38916990
Covalent hit identification is a viable approach to identify chemical starting points against difficult-to-drug targets. While most researchers screen libraries of <2k electrophilic fragments, focusing on lead-like compounds can be...
7.
Lucas S, Blackwell J, Borjesson U, Hargreaves D, Milbradt A, Ahmed S, et al.
ACS Med Chem Lett
. 2024 Jun;
15(6):791-797.
PMID: 38894895
Bfl-1 is overexpressed in both hematological and solid tumors; therefore, inhibitors of Bfl-1 are highly desirable. A DNA-encoded chemical library (DEL) screen against Bfl-1 identified the first known reversible covalent...
8.
Stoneham A, Lindisfarne E, Hargreaves D, Heifner J
JBJS Case Connect
. 2024 Jun;
14(2).
PMID: 38870329
Case: A 14-year-old adolescent boy with SCN1B mutation experienced frequent seizures and recurrent elbow dislocation, occurring up to 30 times per day. Following failed conservative treatment, the decision was made...
9.
Thomson C, Barton P, Braybrooke E, Colclough N, Dong Z, Evans L, et al.
J Med Chem
. 2024 May;
67(11):8988-9027.
PMID: 38770784
Herein, we report the identification and optimization of a series of potent inhibitors of EGFR Exon20 insertions with significant selectivity over wild-type EGFR. A strategically designed HTS campaign, multiple iterations...
10.
Hargreaves D, Carbajo R, Bodnarchuk M, Embrey K, Rawlins P, Packer M, et al.
Proc Natl Acad Sci U S A
. 2023 May;
120(21):e2221967120.
PMID: 37186857
The structure-based design of small-molecule inhibitors targeting protein-protein interactions (PPIs) remains a huge challenge as the drug must bind typically wide and shallow protein sites. A PPI target of high...