Selective Estrogen Receptor Degraders (SERDs): A Promising Strategy for Estrogen Receptor Positive Endocrine-Resistant Breast Cancer.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c00913
Abstract: Estrogen receptor (ER) plays important roles in gene transcription and the proliferation of ER positive breast cancers. Selective modulation of ER has been a therapeutic target for this specific type of breast cancer for more… read more here.
Keywords: estrogen receptor; estrogen; selective estrogen; breast cancer ... See more keywords
Discovery of Thieno[2,3-e]indazole Derivatives as Novel Oral Selective Estrogen Receptor Degraders with Highly Improved Antitumor Effect and Favorable Druggability.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00008
Abstract: Endocrine therapies in the treatment of early and metastatic estrogen receptor α positive (ERα+) breast cancer (BC) are greatly limited by de novo and acquired resistance. Selective estrogen receptor degraders (SERDs) like fulvestrant provide new… read more here.
Keywords: estrogen receptor; estrogen; receptor degraders; selective estrogen ... See more keywords
Discovery of a Potent and Orally Bioavailable Zwitterionic Series of Selective Estrogen Receptor Degrader-Antagonists.
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DOI: 10.1021/acs.jmedchem.2c01964
Abstract: 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 modeling and NMR to favor… read more here.
Keywords: estrogen receptor; series; series selective; receptor degrader ... See more keywords
Molecular Docking Study of Isoxazole Indole Derivatives (B2A2 Series) as Promising Selective Estrogen Receptor Modulators & Anticancer Drugs
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DOI: 10.1055/a-1958-3823
Abstract: Abstract A series of 7 compounds with isoxazole – indole – γ-resorcylic acid scaffold, segregated into B2 & A2 series, wherein, B2 comprises Compounds: 13, 14, 15 & 16 and A2 comprises Compounds: 10, 11… read more here.
Keywords: series; estrogen receptor; isoxazole indole; selective estrogen ... See more keywords
Ospemifene: less venous thrombosis than other selective estrogen receptor modulators in postmenopausal women with vulvo vaginal atrophy.
Sign Up to like & getrecommendations! Published in 2020 at "Menopause"
DOI: 10.1097/gme.0000000000001600
Abstract: O spemifene, raloxifene, bazedoxifene, lasofoxifene, clomiphene, and tamoxifen are unique molecules that are active via the estrogen receptor. Estrone, estradiol, and estriol are classic endogenous estrogens whose estrogenic efficacy is related to both concentration and… read more here.
Keywords: estrogen receptor; ospemifene less; estrogen; selective estrogen ... See more keywords
Beneficial effects of switching to denosumab from bisphosphonates or selective estrogen receptor modulators in postmenopausal women with type 2 diabetes and osteopenia/osteoporosis
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DOI: 10.1111/jdi.13458
Abstract: Patients with type 2 diabetes mellitus have a higher bone fracture risk than patients without diabetes. Although denosumab (Dmab) is a potent bone resorption inhibitor, its efficacy in patients with type 2 diabetes mellitus has… read more here.
Keywords: selective estrogen; effects switching; denosumab; type diabetes ... See more keywords
A tissue-selective estrogen complex as treatment of osteoporosis in experimental lupus
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DOI: 10.1177/09612033211067984
Abstract: Osteoporosis is a common secondary complication in patients with systemic lupus erythematosus (SLE). Current osteoporosis treatment with bisphosphonates has some negative side effects and there is a lack of data regarding newer treatments options for… read more here.
Keywords: disease; osteoporosis; selective estrogen; treatment ... See more keywords
Bazedoxifene, a selective estrogen receptor modulator, reduces cerebral aneurysm rupture in Ovariectomized rats
Sign Up to like & getrecommendations! Published in 2017 at "Journal of Neuroinflammation"
DOI: 10.1186/s12974-017-0966-7
Abstract: BackgroundEstrogen deficiency is thought to be responsible for the higher frequency of aneurysmal subarachnoid hemorrhage in post- than premenopausal women. Estrogen replacement therapy appears to reduce this risk but is associated with significant side effects.… read more here.
Keywords: selective estrogen; rupture; ovariectomized rats; rupture ovariectomized ... See more keywords
Incidence and Risk of Venous Thromboembolism in Bisphosphonates and Selective Estrogen Receptor Modulators Treatment in Korea
Sign Up to like & getrecommendations! Published in 2021 at "Journal of Korean Medical Science"
DOI: 10.3346/jkms.2021.36.e186
Abstract: Background Selective estrogen receptor modulators (SERMs) were associated with an increased risk of venous thromboembolism (VTE) due to the estrogen effect. In this study, we investigated the effect of SERMs on VTE compared to bisphosphonates… read more here.
Keywords: risk venous; risk; selective estrogen; estrogen ... See more keywords