David J Hosfield
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Explore the profile of David J Hosfield including associated specialties, affiliations and a list of published articles.
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17
Citations
925
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Recent Articles
1.
Hosfield D, Weber S, Li N, Sauvage M, Joiner C, Hancock G, et al.
Elife
. 2022 May;
11.
PMID: 35575456
Chemical manipulation of estrogen receptor alpha ligand binding domain structural mobility tunes receptor lifetime and influences breast cancer therapeutic activities. Selective estrogen receptor modulators (SERMs) extend estrogen receptor alpha (ERα)...
2.
Fanning S, Jeselsohn R, Dharmarajan V, Mayne C, Karimi M, Buchwalter G, et al.
Elife
. 2018 Nov;
7.
PMID: 30489256
Acquired resistance to endocrine therapy remains a significant clinical burden for breast cancer patients. Somatic mutations in the (estrogen receptor alpha (ERα)) gene ligand-binding domain (LBD) represent a recognized mechanism...
3.
Bennett M, Wu Y, Boloor A, Matuszkiewicz J, OConnell S, Shi L, et al.
Bioorg Med Chem Lett
. 2018 Apr;
28(10):1811-1816.
PMID: 29657099
The bromodomain and extra-terminal (BET) family of epigenetic proteins has attracted considerable attention in drug discovery given its involvement in regulating gene transcription. Screening a focused small molecule library based...
4.
West D, Kocherginsky M, Tonsing-Carter E, Dolcen D, Hosfield D, Lastra R, et al.
Clin Cancer Res
. 2018 Apr;
24(14):3433-3446.
PMID: 29636357
Although high glucocorticoid receptor (GR) expression in early-stage estrogen receptor (ER)-negative breast cancer is associated with shortened relapse-free survival (RFS), how associated GR transcriptional activity contributes to aggressive breast cancer...
5.
Nie Z, Shi L, Lai C, OConnell S, Xu J, Stansfield R, et al.
Bioorg Med Chem Lett
. 2018 Apr;
28(9):1490-1494.
PMID: 29627262
Histone lysine demethylases (KDMs) play a key role in epigenetic regulation and KDM5A and KDM5B have been identified as potential anti-cancer drug targets. Using structural information from known KDM4 and...
6.
Chen Y, Bonaldi T, Cuomo A, Del Rosario J, Hosfield D, Kanouni T, et al.
ACS Med Chem Lett
. 2017 Aug;
8(8):869-874.
PMID: 28835804
Histone lysine demethylases (KDMs) play a vital role in the regulation of chromatin-related processes. Herein, we describe our discovery of a series of potent KDM4 inhibitors that are both cell...
7.
Balbas M, Evans M, Hosfield D, Wongvipat J, Arora V, Watson P, et al.
Elife
. 2013 Apr;
2:e00499.
PMID: 23580326
The second-generation antiandrogen enzalutamide was recently approved for patients with castration-resistant prostate cancer. Despite its success, the duration of response is often limited. For previous antiandrogens, one mechanism of resistance...
8.
Tomita N, Hayashi Y, Suzuki S, Oomori Y, Aramaki Y, Matsushita Y, et al.
Bioorg Med Chem Lett
. 2013 Feb;
23(6):1779-85.
PMID: 23414845
In order to develop potent and selective focal adhesion kinase (FAK) inhibitors, synthetic studies on pyrazolo[4,3-c][2,1]benzothiazines targeted for the FAK allosteric site were carried out. Based on the X-ray structural...
9.
Tsutakawa S, Shin D, Mol C, Izumi T, Arvai A, Mantha A, et al.
J Biol Chem
. 2013 Jan;
288(12):8445-8455.
PMID: 23355472
Non-coding apurinic/apyrimidinic (AP) sites in DNA form spontaneously and as DNA base excision repair intermediates are the most common toxic and mutagenic in vivo DNA lesion. For repair, AP sites...
10.
Iwatani M, Iwata H, Okabe A, Skene R, Tomita N, Hayashi Y, et al.
Eur J Med Chem
. 2012 Jul;
61:49-60.
PMID: 22819505
Focal adhesion kinase (FAK) regulates cell survival and proliferation pathways. Here we report the discovery of a highly selective series of 1,5-dihydropyrazolo[4,3-c][2,1]benzothiazines that demonstrate a novel mode of allosteric inhibition...