Selective estrogen receptor modulator
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Raloxifene [6-hydroxy 4-hydroxyphenyl -benzothiophenyl]-[4-[2- 1-piperidyl ethoxy]phenyl]-methanone; see figure 9 belongs to the second-generation benzothiophene SERM drugs. It has a high affinity for the ER with potent antiestrogenic activity and tissue-specific effects distinct from estradiol. The advantage of raloxifene over the triphenylethylene tamoxifen is reduced effect on the uterus. The flexible hinge group, as well as the antiestrogenic phenyl 4-piperidinoethoxy side chain, are important for minimizing uterine effects.
The critical role of the intimate relationship between the hydrophobic side chain of raloxifene and the hydrophobic residue of the receptor to change both the shape and charge of the external surface of a SERM-ER complex has been confirmed with raloxifene derivatives. When the interactive distance between raloxifene and Asp is increased from 2. When the piperidine ring of raloxifene is replaced by cyclohexane , the ligand loses antiestrogenic properties and becomes a full agonist.
It relocates helix 12 away from the ligand-binding pocket thereby preventing coactivators from binding to the SERM-ER complex. Third-generation compounds display either no uterine stimulation, improved potency, no significant increases in hot flushes or even a combination of these positive attributes. Modifications of the first dihydronapthalene SERM, nafoxidine see figure 10 that was a clinical candidate for the treatment of breast cancer but had side effects including severe phototoxicity, resulted in lasofoxifene 5R,6S phenyl[4- 2-pyrrolidinyl-ethoxy -phenyl]-5,6,7,8-tetrahydro-naphthalenol; see figure Nafoxidine has all three phenyls constrained in a coplanar arrangement like tamoxifen.
But with hydrogenation, the double bond of nafoxidene were reduced, and both phenyls are cis-oriented. The amine-bearing side chain can then adopt an axial conformation and locate this group orthogonally to the plane of the core, like ralofoxifene and other less uterotropic SERMs.
Lasofoxifene is among the most potent SERMs reported in protection against bone loss and cholesterol reduction. The excellent oral potency of lasofoxifene has been attributed to reduced intestinal glucuronidation of the phenol. The structural requirement is a non-planar topology with the steric bulk close to the plane of a fused bicyclic aromatic system.
Lasofoxifenes large flexible side chain terminates in a pyrrolidine head group and threads its way out toward the surface of the protein, where it interferes directly with the positioning of the AF-2 helix. A salt bridge forms between lasofoxifene and Asp The charge neutralization in this region ER may explain some antiestrogenic effects exerted by lasofoxifene. The indole system has served as a core unit in SERMs, and when an amine is attached to the indole with a benzyloxyethyl, the resultant compounds were shown to have no preclinical uterine activity while sparing rat bone with full efficacy at low doses.
Bazedoxifene 1H-indool,1-[[4-[2 hexahydro-1H-azepinyl ethoxy]methyl]2- hydroxyphenlyl methyl; see figure 10] acetic acid is one of those compounds. The core binding domain consists of a 2-phenylmethyl indole and a hexamethylenamine ring at the side chain affecter region. It is metabolized by glucuronidation, with the absolute bioavailability of 6. It has agonistic effects on bone and lipid metabolism but not on breast and uterine endometrium.
Ospemifene Z 4- 4-chloro-1,2-diphenyl-butenyl phenoxy ethanol; see figure 13 is a triphenylethylene and a known metabolite of toremifene. Ospemifene does not have 2- dimethylamino ethoxy group as tamoxifen. Structure—activity relationship studies shoved that by removing that group of tamoxifen agonistic activity in the uterus was significantly reduced, but not in bone and cardiovascular system.
Preclinical and clinical data show that ospemifene is well tolerated with no major side effects. Benefits that ospemifene may have over other SERMs is its neutral effect on hot flushes and ER-agonist effect on the vagina, improving the symptoms of vaginal dryness. The small differences between the two subtypes of ER have been used to develop subtype-selective ER modulators, but the high similarity between the two receptors make the development very challenging.
In addition, the structure of the ligand must be rigid. Repulsive interactions may otherwise lead to conformational change of the ligand and, therefore, creating alternative binding modes. The receptor recognition of 4-hydroxytamoxifen appears to be controlled by two structural features of 4-hydroxytamoxifen, the phenolic A ring, and the bulky side chain.
The bulky side chain, protruding from the binding cavity, displaces helix 12 from ligand-binding pocket to cover part of the coactivator binding pocket.
The ERhydroxytamoxifen complex formation recruits corepressors proteins. This leads to decreased DNA synthesis and inhibition of estrogen activity. Just like in 4-hydroxytamoxifen, the bulky side chain of raloxifene displaces helix Ospemifene is an oxidative deaminated metabolite of toremifene as has a similar binding to ER as toremifene and tamoxifen.
The discovery of SERMs resulted from attempts to develop new contraceptives. A timeline of when SERMs came on the market is seen in figure 1. Clomifene and tamoxifen prevented conception in rats but did the opposite in humans.
Clomifene successfully induced ovulation in subfertile women and on February 1, , it was approved in the US for the treatment of ovulatory dysfunction in women who were trying to conceive. It was another ten years before tamoxifen was approved in December , not as a contraceptive but as a hormonal treatment to treat and prevent breast cancer.
Raloxifene originally failed as a breast cancer drug due to its poor performance in comparison to tamoxifen in the laboratory  but the estrogenic effects of raloxifene on bone led to its rediscovery and approval in Combined therapy with conjugated estrogens and the SERM bazedoxifene , was approved on October 3, , for the treatment of vasomotor symptoms linked with menopause.
Bazedoxifene is also used in the prevention of postmenopausal osteoporosis. From Wikipedia, the free encyclopedia.
Redirected from Selective estrogen-receptor modulator. Selective estrogen receptor modulator Drug class Tamoxifen , a nonsteroidal triphenylethylene antiestrogen and a widely used drug in the treatment of breast cancer. The New England Journal of Medicine. A review of effects on the breast". The Journal of Pharmacology and Experimental Therapeutics.
Expert Opinion on Drug Discovery. Chemical Research in Toxicology. The Journal of Organic Chemistry. Clinical considerations and new agents". Journal of Medicinal Chemistry. Expert Opinion on Pharmacotherapy. Expert Opinion on Investigational Drugs. Selective estrogen receptor modulators a new brand of multitarget drugs 1st ed. Anastrozole Exemestane Fadrozole Formestane Letrozole.
Mixed mechanism of action: Danazol Gestrinone Androstenedione immunogens: Androvax androstenedione albumin Ovandrotone albumin Fecundin. Retrieved from " https: Hormonal antineoplastic drugs Progonadotropins Selective estrogen receptor modulators. Views Read Edit View history. In other projects Wikimedia Commons.
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