Anna Aparicio
Overview
Explore the profile of Anna Aparicio including associated specialties, affiliations and a list of published articles.
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Articles
11
Citations
443
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0
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Recent Articles
1.
Kahraman M, Govek S, Nagasawa J, Lai A, Bonnefous C, Douglas K, et al.
ACS Med Chem Lett
. 2019 Jan;
10(1):50-55.
PMID: 30655946
The further optimization of ER-α degradation efficacy of a series of ER modulators by refining side-chain substitution led to efficacious selective estrogen receptor degraders (SERDs). A fluoromethyl azetidine group was...
2.
Joseph J, Darimont B, Zhou W, Arrazate A, Young A, Ingalla E, et al.
Elife
. 2019 Jan;
8.
PMID: 30614786
No abstract available.
3.
Nagasawa J, Govek S, Kahraman M, Lai A, Bonnefous C, Douglas K, et al.
J Med Chem
. 2018 Aug;
61(17):7917-7928.
PMID: 30086626
About 75% of breast cancers are estrogen receptor alpha (ER-α) positive, and women typically initially respond well to antihormonal therapies such as tamoxifen and aromatase inhibitors, but resistance often emerges....
4.
Joseph J, Darimont B, Zhou W, Arrazate A, Young A, Ingalla E, et al.
Elife
. 2016 Jul;
5.
PMID: 27410477
ER-targeted therapeutics provide valuable treatment options for patients with ER+ breast cancer, however, current relapse and mortality rates emphasize the need for improved therapeutic strategies. The recent discovery of prevalent...
5.
Lai A, Kahraman M, Govek S, Nagasawa J, Bonnefous C, Julien J, et al.
J Med Chem
. 2015 Apr;
58(12):4888-904.
PMID: 25879485
Approximately 80% of breast cancers are estrogen receptor alpha (ER-α) positive, and although women typically initially respond well to antihormonal therapies such as tamoxifen and aromatase inhibitors, resistance often emerges....
6.
Clegg N, Wongvipat J, Joseph J, Tran C, Ouk S, Dilhas A, et al.
Cancer Res
. 2012 Jan;
72(6):1494-503.
PMID: 22266222
Continued reliance on the androgen receptor (AR) is now understood as a core mechanism in castration-resistant prostate cancer (CRPC), the most advanced form of this disease. While established and novel...
7.
Pontillo J, Wu D, Ching B, Hudson S, Genicot M, Gao Y, et al.
Bioorg Med Chem Lett
. 2008 Oct;
18(23):6151-5.
PMID: 18954981
The design synthesis and SAR of a series of chiral ring-constrained norepinephrine reuptake inhibitors with improved physicochemical properties is described. Typical compounds are potent (IC(50)s<10 nM), selective against the other...
8.
Hudson S, Kiankarimi M, Eccles W, Dwight W, Mostofi Y, Genicot M, et al.
Bioorg Med Chem Lett
. 2008 Aug;
18(16):4491-4.
PMID: 18672364
The synthesis and SAR of a series of chiral heterocyclic ring-constrained norepinephrine reuptake inhibitors are described. The best compounds compare favorably with atomoxetine in potency (IC(50)s<10 nM), selectivity against the...
9.
Vickers T, Dyck B, Tamiya J, Zhang M, Jovic F, Grey J, et al.
Bioorg Med Chem Lett
. 2008 May;
18(11):3230-5.
PMID: 18468895
A series of milnacipran analogs containing a heteroaromatic group were synthesized and studied as monoamine transporter inhibitors. Many compounds exhibited higher potency than milnacipran at NET and NET/SERT with no...
10.
Tamiya J, Dyck B, Zhang M, Phan K, Fleck B, Aparicio A, et al.
Bioorg Med Chem Lett
. 2008 May;
18(11):3328-32.
PMID: 18445525
A series of milnacipran analogs were synthesized and studied as monoamine transporter inhibitors, and several potent compounds with moderate lipophilicity were identified from the 1S,2R-isomers. Thus, 15l exhibited IC(50) values...