Asoprisnil (J867): a selective progesterone receptor modulator for gynecological therapy

DeManno, Deborah A.; Elger, W.; Garg, Ramesh C.; Lee, Ronald; Schneider, Birgitt; Hess‐Stumpp, Holger; Schubert, G.; Chwalisż, Kristof

doi:10.1016/j.steroids.2003.09.008

Cited by 111 publications

(92 citation statements)

References 12 publications

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“…Two important co-repressor proteins that will be discussed below are nuclear receptor co-repressor (N-CoR) and silencing mediator of retinoid and thyroid hormone receptors (SMRT). Asoprisnil (J867) [95] is a steroidal selective progesterone receptor (PR) modulator (SPRM) in clinical development against endometriosis. It displays mostly antagonist behavior but also weak agonist effects in fluorescence polarization and mammalian twohybrid assays.…”

Section: Stabilizers Of Nuclear-receptor-corepressor Interactionsmentioning

confidence: 99%

Stabilization of protein–protein interactions by small molecules

Giordanetto¹,

Schäfer

Ottmann

2014

Drug Discovery Today

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Section: Stabilizers Of Nuclear-receptor-corepressor Interactionsmentioning

confidence: 99%

Stabilization of protein–protein interactions by small molecules

Giordanetto¹,

Schäfer

Ottmann

2014

Drug Discovery Today

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“…The triazole derivatives (32a-32k) exhibited considerably higher cytotoxic activity in mammary cancer cell line MCF-7 as compared to that of the pyrazole derivatives (33f-33o). The difference in this activity could be attributed to the ability of the triazole (three nitrogen atoms) to form stronger hydrogen bonds with the active site of some proteins (receptor or enzyme) of the cell 57 . Compounds 32f-32k having an aromatic ester at C-3 showed that an enhanced cytotoxic activity as compared to their aliphatic counterpart 32a-32e.…”

Section: Novel Structure Of Progestinsmentioning

confidence: 99%

Recent advances in structure of progestins and their binding to progesterone receptors

Cabeza

Heuze

Sánchez

et al. 2014

Journal of Enzyme Inhibition and Medicinal Chemistry

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The role of progesterone in women's cancers as well as the knowledge of the progesterone receptor (PR) structure has prompted the design of different therapies. The aim of this review is to describe the basic structure of PR agonists and antagonists as well as the recent treatments for illness associated with the progesterone receptor. The rational design for potent and effective drugs for the treatment of female cancer must consider the structural changes of the androgen and progestogen skeleton which are an indicator of their activity as progestins or antiprogestins. The presence of a hydroxyl group at C-17 in the progesterone skeleton brings about a loss of progestational activity whereas acetylation induces a progestational effect. The incorporation of an ethynyl functional group to the testosterone framework results in a loss of androgenic activity with a concomitant enhancement of the progestational effect. On the other hand, an ester function at C-3 of dehydroepiandrosterone skeleton induces partial antagonism to the PR.

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“…It induces amenorrhea and reduces uterine fibroid volume in a dose-dependent manner [54,55], and it reduces uterine artery blood flow [56]. Asoprisnil has marginal abortifacient activity and no antiglucocorticoid effect [57][58][59][60]. This drug does not induce estrogen deprivation symptoms or breakthrough bleeding.…”

Section: Selective Progesterone Receptor Modulatorsmentioning

confidence: 99%

Medical Management of Uterine Fibroids

Parsanezhad

Jahromi

2012

Curr Obstet Gynecol Rep

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Uterine leiomyomas are the most common benign tumors of the uterus. Though benign, they can affect the quality of life for many women. Compared with the standard surgical treatments, medical therapy is attractive and avoids possible surgery-related complications. No medical therapy currently exists that can induce rapid regression of the myoma and symptoms with minimal side effects without affecting fertility. This review evaluates medical treatments that are currently available for the treatment of uterine fibroids.

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Asoprisnil (J867): a selective progesterone receptor modulator for gynecological therapy

Cited by 111 publications

References 12 publications

Stabilization of protein–protein interactions by small molecules

Stabilization of protein–protein interactions by small molecules

Recent advances in structure of progestins and their binding to progesterone receptors

Medical Management of Uterine Fibroids

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