serm
Serm
選択的エストロゲン受容体修飾薬
(Serm から転送)
出典: フリー百科事典『ウィキペディア(Wikipedia)』 (2023/07/12 15:00 UTC 版)
選択的エストロゲン受容体修飾薬(Selective estrogen receptor modulator;SERM)[1]は、エストロゲン受容体作動薬/遮断薬(ERAA)[2]としても知られ、エストロゲン受容体(ER)に作用する薬剤の一種である[3]。これらの物質が純粋なER作動薬および遮断薬(即ち、完全作動薬および完全遮断薬)と異なる特徴は、その作用の強さが組織ごとにさまざまに異なるため、多種多様な組織でエストロゲン様作用を選択的に刺激または阻害する可能性があるということである。
- ^ “Ospemifene: less venous thrombosis than other selective estrogen receptor modulators in postmenopausal women with vulvo vaginal atrophy”. Menopause 27 (8): 846–847. (August 2020). doi:10.1097/GME.0000000000001600. PMID 32576803.
- ^ “ERAAs for menopause treatment: Welcome the 'designer estrogens'”. Cleve Clin J Med 84 (6): 463–470. (June 2017). doi:10.3949/ccjm.84a.15140. PMID 28628428.
- ^ a b c d e “Selective estrogen-receptor modulators -- mechanisms of action and application to clinical practice”. The New England Journal of Medicine 348 (7): 618–29. (Feb 2003). doi:10.1056/NEJMra022219. PMID 12584371.
- ^ a b c d e f g h i j k l m n o p q “The discovery and development of selective estrogen receptor modulators (SERMs) for clinical practice”. Current Clinical Pharmacology 8 (2): 135–55. (May 2013). doi:10.2174/1574884711308020006. PMC 3624793. PMID 23062036 .
- ^ a b c d e f g “Selective estrogen receptor modulators and the combination therapy conjugated estrogens/bazedoxifene: A review of effects on the breast”. Post Reproductive Health 21 (3): 112–21. (Sep 2015). doi:10.1177/2053369115599090. PMID 26289836.
- ^ a b c d e f g h i j “Selective estrogen receptor modulators (SERMs): a review of clinical data”. Maturitas 80 (1): 52–7. (Jan 2015). doi:10.1016/j.maturitas.2014.10.010. PMID 25466304.
- ^ a b c d e f g h i j k l m n “SERMs: evolutionary chemistry, revolutionary biology”. Current Pharmaceutical Design 8 (23): 2089–111. (2002). doi:10.2174/1381612023393404. PMID 12171520.
- ^ Cameron, John L.; Cameron, Andrew M (20 November 2013). Current Surgical Therapy. Elsevier Health Sciences. pp. 582–. ISBN 978-0-323-22511-3
- ^ a b Huang, Xianhai; Aslanian, Robert G. (19 April 2012). Case Studies in Modern Drug Discovery and Development. John Wiley & Sons. pp. 392–394. ISBN 978-1-118-21967-6
- ^ Nath, A.; Sitruk-Ware, R. (2009). “Pharmacology and clinical applications of selective estrogen receptor modulators”. Climacteric 12 (3): 188–205. doi:10.1080/13697130802657896. ISSN 1369-7137.
- ^ “SERMs: current status and future trends”. Crit. Rev. Oncol. Hematol. 43 (1): 63–76. (July 2002). doi:10.1016/S1040-8428(02)00022-7. PMID 12098608.
- ^ “Selective estrogen receptor modulators: tissue specificity and clinical utility”. Clin Interv Aging 9: 1437–52. (2014). doi:10.2147/CIA.S66690. PMC 4154886. PMID 25210448 .
- ^ “Selective estrogen receptor modulators (SERMs): a review of clinical data”. Maturitas 80 (1): 52–7. (January 2015). doi:10.1016/j.maturitas.2014.10.010. PMID 25466304.
- ^ “Selective estrogen receptor modulators in clinical practice: a safety overview”. Expert Opin Drug Saf 14 (6): 921–34. (June 2015). doi:10.1517/14740338.2015.1014799. PMID 25936229.
- ^ Barbara L. Hoffman; John O. Schorge; Karen D. Bradshaw; Lisa M. Halvorson; Joseph I. Schaffer; Marlene M. Corton (22 April 2016). Williams Gynecology (Third ed.). McGraw-Hill Education. p. 364. ISBN 978-0-07-184909-8
- ^ “Estrogens and selective estrogen receptor modulators in acromegaly”. Endocrine 54 (2): 306–314. (November 2016). doi:10.1007/s12020-016-1118-z. PMID 27704479.
- ^ “Clinical uses of antiestrogens”. Obstet Gynecol Surv 51 (1): 45–59. (January 1996). PMID 8657397 .
- ^ Bryant, Henry U. (2008). “Chapter 41 – The Pharmacology of Selective Estrogen Receptor Modulators”. Principles of Bone Biology. pp. 887–919. doi:10.1016/B978-0-12-373884-4.00058-6
- ^ “The effect of selective estrogen receptor modulator administration on the hypothalamic-pituitary-testicular axis in men with idiopathic oligozoospermia”. Fertil. Steril. 91 (4 Suppl): 1427–30. (April 2009). doi:10.1016/j.fertnstert.2008.06.002. PMID 18692782.
- ^ “The effect of selective estrogen receptor modulators on parameters of the hypothalamic-pituitary-gonadal axis”. Ann. N. Y. Acad. Sci. 949: 251–8. (December 2001). doi:10.1111/j.1749-6632.2001.tb04029.x. PMID 11795360.
- ^ “The future of the new selective estrogen receptor modulators”. Menopause Int 13 (1): 27–34. (March 2007). doi:10.1258/175404507780456791. PMID 17448265.
- ^ “Pharmacokinetics, pharmacodynamics and clinical efficacy of ospemifene for the treatment of dyspareunia and genitourinary syndrome of menopause”. Expert Opin Drug Metab Toxicol 12 (10): 1233–46. (October 2016). doi:10.1080/17425255.2016.1218847. PMID 27476551.
- ^ “Effects of Toremifene, a Selective Estrogen Receptor Modulator, on Spontaneous and Stimulated GH Secretion, IGF-I, and IGF-Binding Proteins in Healthy Elderly Subjects”. J Endocr Soc 2 (2): 154–165. (February 2018). doi:10.1210/js.2017-00457. PMC 5789038. PMID 29383334 .
- ^ “A double-blind, randomized, ascending, multiple-dose study of bazedoxifene in healthy postmenopausal women”. Clin Pharmacol Drug Dev 3 (4): 262–9. (July 2014). doi:10.1002/cpdd.102. PMID 27128831.
- ^ Trost, Landon W.; Khera, Mohit (2014). “Alternative Treatment Modalities for the Hypogonadal Patient”. Current Urology Reports 15 (7). doi:10.1007/s11934-014-0417-2. ISSN 1527-2737.
- ^ a b c d “Panning for SNuRMs: using cofactor profiling for the rational discovery of selective nuclear receptor modulators”. Drug Discovery Today 12 (19–20): 860–9. (Oct 2007). doi:10.1016/j.drudis.2007.07.025. PMID 17933688.
- ^ a b c d e f g h i “Structure-based approach for the discovery of novel selective estrogen receptor modulators”. Current Medicinal Chemistry 18 (8): 1188–94. (2011). doi:10.2174/092986711795029645. PMID 21291367.
- ^ a b c d “Development of subtype-selective oestrogen receptor-based therapeutics”. Nature Reviews. Drug Discovery 10 (10): 778–92. (Oct 2011). doi:10.1038/nrd3551. PMID 21921919.
- ^ “Reflections on the discovery and significance of estrogen receptor beta”. Endocrine Reviews 26 (3): 465–78. (May 2005). doi:10.1210/er.2004-0027. PMID 15857973.
- ^ “Molecular mechanisms of selective estrogen receptor modulator (SERM) action”. The Journal of Pharmacology and Experimental Therapeutics 295 (2): 431–7. (Nov 2000). PMID 11046073 .
- ^ “Discovery of estrogen receptor modulators: a review of virtual screening and SAR efforts”. Expert Opinion on Drug Discovery 5 (1): 21–31. (Jan 2010). doi:10.1517/17460440903490395. PMID 22823969.
- ^ “Molecular basis of agonism and antagonism in the oestrogen receptor”. Nature 389 (6652): 753–8. (1997). doi:10.1038/39645. PMID 9338790.
- ^ “The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen”. Cell 95 (7): 927–37. (1998). doi:10.1016/S0092-8674(00)81717-1. PMID 9875847.
- ^ a b c d e f g h i “Medicinal chemistry and emerging strategies applied to the development of selective estrogen receptor modulators (SERMs)”. Current Medicinal Chemistry 14 (11): 1249–61. (2007). doi:10.2174/092986707780598023. PMID 17504144.
- ^ a b c d e f “Selective estrogen receptor modulators (SERMs): mechanisms of anticarcinogenesis and drug resistance”. Mutation Research 591 (1–2): 247–63. (Dec 2005). doi:10.1016/j.mrfmmm.2005.02.028. PMID 16083919.
- ^ a b “Nuclear receptor modulation--role of coregulators in selective estrogen receptor modulator (SERM) actions”. Steroids 90: 39–43. (Nov 2014). doi:10.1016/j.steroids.2014.06.008. PMC 4192004. PMID 24945111 .
- ^ a b c d e “Structure-activity relationships for a large diverse set of natural, synthetic, and environmental estrogens”. Chemical Research in Toxicology 14 (3): 280–94. (Mar 2001). doi:10.1021/tx000208y. PMID 11258977.
- ^ a b c “The agonistic-antagonistic properties of clomiphene: a review”. Pharmacology & Therapeutics 15 (3): 467–519. (1981). doi:10.1016/0163-7258(81)90055-3. PMID 7048350.
- ^ a b c d e “The estrogen receptor: a model for molecular medicine”. Clinical Cancer Research 9 (6): 1980–9. (Jun 2003). PMID 12796359.
- ^ “Tamoxifen: important considerations of a multi-functional compound with organ-specific properties”. Cancer Treatment Reviews 33 (2): 91–100. (Apr 2007). doi:10.1016/j.ctrv.2006.09.008. PMID 17178195.]
- ^ a b c “Pharmacokinetics of selective estrogen receptor modulators”. Clinical Pharmacokinetics 42 (4): 361–72. (2012-09-30). doi:10.2165/00003088-200342040-00004. PMID 12648026.
- ^ a b “Multiple targeting by the antitumor drug tamoxifen: a structure-activity study”. Current Medicinal Chemistry. Anti-Cancer Agents 4 (6): 491–508. (Nov 2004). doi:10.2174/1568011043352696. PMID 15579015.
- ^ “New Highly Stereoselective Synthesis of (Z)-4-Hydroxytamoxifen and (Z)-4-Hydroxytoremifene via McMurry Reaction”. The Journal of Organic Chemistry 61 (11): 3890–3893. (May 1996). doi:10.1021/jo952279l. PMID 11667248.
- ^ a b “Antiestrogens and selective estrogen receptor modulators as multifunctional medicines. 2. Clinical considerations and new agents”. Journal of Medicinal Chemistry 46 (7): 1081–111. (Mar 2003). doi:10.1021/jm020450x. PMID 12646017.
- ^ a b “The 2.0 A crystal structure of the ERalpha ligand-binding domain complexed with lasofoxifene”. Protein Science 16 (5): 897–905. (May 2007). doi:10.1110/ps.062729207. PMC 2206632. PMID 17456742 .
- ^ a b “Bazedoxifene: a new selective estrogen receptor modulator for the treatment of postmenopausal osteoporosis”. Expert Opinion on Pharmacotherapy 10 (8): 1377–85. (Jun 2009). doi:10.1517/14656560902980228. PMID 19445558.
- ^ “Ospemifene use in postmenopausal women”. Expert Opinion on Investigational Drugs 18 (6): 839–49. (Jun 2009). doi:10.1517/13543780902953715. PMID 19466874.
- ^ a b “Toremifene--a promising therapy for the prevention of prostate cancer and complications of androgen deprivation therapy”. Expert Opinion on Investigational Drugs 15 (3): 293–305. (Mar 2006). doi:10.1517/13543784.15.3.293. PMID 16503765.
- ^ Palacios, Santiago (2006). “Endometrial Effects of SERMs”. Selective estrogen receptor modulators a new brand of multitarget drugs (1st ed.). Berlin: Springer. pp. 282–3. doi:10.1007/3-540-34742-9_11. ISBN 978-3-540-24227-7
- ^ “Senshio (ospemifene)”. The European Medicines Agency (EMA). 2015年11月2日閲覧。
- ^ “Fareston”. European Medicines Agency (EMA). 2015年11月2日閲覧。
- ^ “Fablyn”. The European Medicines Agency (EMA). 2015年11月2日閲覧。
- 1 選択的エストロゲン受容体修飾薬とは
- 2 選択的エストロゲン受容体修飾薬の概要
- 3 構造上の特徴
- 4 歴史
- 5 関連項目
- Sermのページへのリンク