抗エストロゲン性の

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/09/11 22:04:45」(JST)

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An antiestrogen is a substance that blocks the production or utilization of estrogens,^[1] or inhibits their effects.^[2] Estrogens are the family of hormones that promote the development and maintenance of female sex characteristics.

Although aromatase inhibitors could be considered antiestrogens by some definitions, they are often considered to be a distinct class.^[3] Aromatase inhibitors reduce the production of estrogen, while the term "antiestrogen" is usually reserved for agents reducing the response to estrogen.^[4]

Hot flashes, osteoporosis, breast atrophy, and vaginal dryness can be side effects of antiestrogens.

Specific antiestrogens

Antiestrogens like tamoxifen can promote an invasive phenotype in estrogen receptor (ER)-positive breast cancer cells with deficient intercellular adhesion.

Ethamoxytriphetol (MER-25) was the first antiestrogen to be discovered,^[5] followed by clomifene citrate and tamoxifen.^[6]^[7] Fulvestrant is another antiestrogen, and is the only pure antiestrogen, or silent antagonist of the estrogen receptor, to have been introduced clinically.^[8]^[9]

References

^ "Definition of antiestrogen - NCI Dictionary of Cancer Terms, Definition of antiestrogen - NCI Dictionary of Cancer Terms". ,
^ "antiestrogen" at Dorland's Medical Dictionary
^ Riggins RB, Bouton AH, Liu MC, Clarke R (2005). "Antiestrogens, aromatase inhibitors, and apoptosis in breast cancer". Vitam. Horm. 71: 201–37. doi:10.1016/S0083-6729(05)71007-4. PMID 16112269.
^ Thiantanawat, Apinya; Long, Brian; Brodie, Angela (2003-11-15). "Signaling Pathways of Apoptosis Activated by Aromatase Inhibitors and Antiestrogens". The Journal of Cancer Research. Retrieved 2015-04-13.
^ Philipp Y. Maximov; Russell E. McDaniel; V. Craig Jordan (23 July 2013). Tamoxifen: Pioneering Medicine in Breast Cancer. Springer Science & Business Media. pp. 7–. ISBN 978-3-0348-0664-0.
^ V Craig Jordan (27 May 2013). Estrogen Action, Selective Estrogen Receptor Modulators and Women's Health: Progress and Promise. World Scientific. pp. 7,112. ISBN 978-1-84816-959-3.
^ Walter Sneader (23 June 2005). Drug Discovery: A History. John Wiley & Sons. pp. 198–199. ISBN 978-0-471-89979-2.
^ Eckhard Ottow; Hilmar Weinmann (8 September 2008). Nuclear Receptors as Drug Targets. John Wiley & Sons. pp. 164–165. ISBN 978-3-527-62330-3.
^ Bruce A. Chabner; Dan L. Longo (8 November 2010). Cancer Chemotherapy and Biotherapy: Principles and Practice. Lippincott Williams & Wilkins. pp. 660–. ISBN 978-1-60547-431-1.

External links

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1. 乳癌予防のための選択的エストロゲン受容体調節因子およびアロマターゼ阻害剤 selective estrogen receptor modulators and aromatase inhibitors for breast cancer prevention
2. 非転移性ホルモン受容体陽性乳癌に対する補助内分泌療法 adjuvant endocrine therapy for non metastatic hormone receptor positive breast cancer
3. 選択的エストロゲン受容体モジュレーターの作用機序 mechanisms of action of selective estrogen receptor modulators
4. 転移性ホルモン受容体陽性乳癌に対する治療アプローチ：内分泌療法 treatment approach to metastatic hormone receptor positive breast cancer endocrine therapy
5. Thoracic endometriosis: Pathogenesis, epidemiology, and pathology

English Journal

Assessment of multiple hormone activities of a UV-filter (octocrylene) in zebrafish (Danio rerio).

Zhang QY1, Ma XY1, Wang XC2, Ngo HH3.
Chemosphere.Chemosphere.2016 Sep;159:433-41. doi: 10.1016/j.chemosphere.2016.06.037. Epub 2016 Jun 20.
In this study, zebrafish (Danio rerio) were exposed to a UV-filter-octocrylene (OCT) with elevated concentrations for 28 d. The total body accumulation of OCT in zebrafish was found to reach 2321.01 ("L" level), 31,234.80 ("M" level), and 70,593.38 ng g(-1) ("H" level) when the average OCT exposu
PMID 27337435

Discovery of a sulfamate-based steroid sulfatase inhibitor with intrinsic selective estrogen receptor modulator properties.

Ouellet C1, Maltais R1, Ouellet É1, Barbeau X2, Lagüe P3, Poirier D4.
European journal of medicinal chemistry.Eur J Med Chem.2016 Aug 25;119:169-82. doi: 10.1016/j.ejmech.2016.04.044. Epub 2016 Apr 20.
Steroid sulfatase (STS), the enzyme which converts inactive sulfated steroid precursors into active hormones, is a promising therapeutic target for the treatment of estrogen-sensitive breast cancer. We report herein the synthesis and in vitro study of dual-action STS inhibitors with selective estro
PMID 27155470

Bioactivation of Phytoestrogens: Intestinal Bacteria and Health.

Landete JM1, Arqués J1, Medina M1, Gaya P1, de Las Rivas B2, Muñoz R2.
Critical reviews in food science and nutrition.Crit Rev Food Sci Nutr.2016 Aug 17;56(11):1826-43. doi: 10.1080/10408398.2013.789823.
Phytoestrogens are polyphenols similar to human estrogens found in plants or derived from plant precursors. Phytoestrogens are found in high concentration in soya, flaxseed and other seeds, fruits, vegetables, cereals, tea, chocolate, etc. They comprise several classes of chemical compounds (stilben
PMID 25848676

Japanese Journal

多環芳香族炭化水素誘導体が示す毒性作用

戸次加奈江,鳥羽陽,唐寧 [他],亀田貴之,早川和一
産業医科大学雑誌 35(1), 17-24, 2013-03-01
多環芳香族炭化水素類(PAHs)は大気粉塵などの多種類の環境汚染物質に含まれ,長年の研究によって多様な生体影響を引き起こすことが知られている.一方で,PAHsは生体内での代謝反応や,大気中での化学反応によって多種多様な誘導体を生成することが知られている.近年では,PAHだけでなくPAH誘導体の毒性影響が着目されており,エストロゲン様/抗エストロゲン作用,酸化ストレス反応など,PAHとは異なる誘導体 …
NAID 110009593197

多環芳香族炭化水素類の生体影響に対し輸送及び生体内代謝がどのように関与しているのか

戸次加奈江,鳥羽陽,唐寧 [他],亀田貴之,滝上英孝,鈴木剛,早川和一
YAKUGAKU ZASSHI 132(3), 325-329, 2012
… Additionally, strongly mutagenic nitrated PAHs (NPAHs), estrogenic/antiestrogenic PAH hydroxides (PAHOHs) and reactive oxygen species-producing PAH quinones (PAHQs) are formed from PAHs by the chemical reaction during the transport. …
NAID 130001872028

Mutagenicities and Endocrine-disrupting Activities of 1-Hydroxy-2-nitropyrene and 1-Hydroxy-5-nitropyrene

Kameda Takayuki,Akiyama Ayuko,Yoshita Morio [他],Tachikawa Chihiro,Toriba Akira,Tang Ning,Hayakawa Kazuichi
Journal of Health Science 57(4), 372-377, 2011
… 1-OH-5-NP exhibited stronger antiestrogenic and antiandrogenic activities than 1-OH-2-NP. …
NAID 130001001083

「antiestrogen」

　　[★]

抗エストロゲン剤、抗女性ホルモン剤

関: estrogen receptor modulator

関: spe- cific agents

[urlDefinition_of_antiestrogen_-_NCI_Dictionary_of_Cancer_Terms.2C_Definition_of_antiestrogen_-_NCI_Dictionary_of_Cancer_Terms-1] "Definition of antiestrogen - NCI Dictionary of Cancer Terms, Definition of antiestrogen - NCI Dictionary of Cancer Terms". ,

[2] "antiestrogen" at Dorland's Medical Dictionary

[pmid16112269-3] Riggins RB, Bouton AH, Liu MC, Clarke R (2005). "Antiestrogens, aromatase inhibitors, and apoptosis in breast cancer". Vitam. Horm. 71: 201–37. doi:10.1016/S0083-6729(05)71007-4. PMID 16112269.

[4] Thiantanawat, Apinya; Long, Brian; Brodie, Angela (2003-11-15). "Signaling Pathways of Apoptosis Activated by Aromatase Inhibitors and Antiestrogens". The Journal of Cancer Research. Retrieved 2015-04-13.

[MaximovMcDaniel2013-5] Philipp Y. Maximov; Russell E. McDaniel; V. Craig Jordan (23 July 2013). Tamoxifen: Pioneering Medicine in Breast Cancer. Springer Science & Business Media. pp. 7–. ISBN 978-3-0348-0664-0.

[Jordan2013-6] V Craig Jordan (27 May 2013). Estrogen Action, Selective Estrogen Receptor Modulators and Women's Health: Progress and Promise. World Scientific. pp. 7,112. ISBN 978-1-84816-959-3.

[Sneader2005-7] Walter Sneader (23 June 2005). Drug Discovery: A History. John Wiley & Sons. pp. 198–199. ISBN 978-0-471-89979-2.

[OttowWeinmann2008-8] Eckhard Ottow; Hilmar Weinmann (8 September 2008). Nuclear Receptors as Drug Targets. John Wiley & Sons. pp. 164–165. ISBN 978-3-527-62330-3.

[ChabnerLongo2010-9] Bruce A. Chabner; Dan L. Longo (8 November 2010). Cancer Chemotherapy and Biotherapy: Principles and Practice. Lippincott Williams & Wilkins. pp. 660–. ISBN 978-1-60547-431-1.

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antiestrogenic

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