9 results about "Estrogen receptor activity" patented technology

Described herein are pinoxifene compositions comprising novel compounds and methods of use thereof. Methods of synthesizing the compositions are described herein. The odoxifene compositions described herein may exhibit aromatase inhibitory activity or estrogen receptor activity. The odoxifene compositions described herein can be used to treat a condition, such as cancer, in a subject.

The present disclosure provides 1) an enantiomerically purified compound SRR G-1, or a derivative thereof, including specific crystal forms, salts and co-crystals that modulates G protein-coupled estrogen receptor activity, 2) pharmaceutical and cosmetic compositions comprising an enantiomerically purified SRR G-1, or a derivative thereof, and 3) methods of treating or preventing disease states and conditions and cosmetic conditions mediated through these receptors and related methods thereof in humans and animals.

The invention discloses a novel application of oxymatrine in improving psoriasis symptoms by activating PPP2CA to inhibit ERalpha activity. The novel application comprises the following steps: animal experiments; cell experiments; determining the activity of the CCK-8 cell; carrying out Giemsa staining; the ELISA kit is used for detecting inflammatory cytokines IL-17 and IL-23; carrying out DIA proteomics; carrying out PPP2CA target verification; a PPP2CA siRNA knockout experiment is carried out; a PPP2CA overexpression plasmid experiment is carried out; evaluating the curative effect of the PPP2CA inhibitor; chemical proteomics; molecular docking; determining the enzyme activity of the PPP2CA; carrying out a thermal drift experiment (CETSA) / Western Blot experiment; phosphorylated proteomics; an estrogen signal channel key protein siRNA knock-down experiment; determining the ERalpha activity through a dual-luciferase reporter gene experiment; and statistical analysis. According to the invention, oxymatrine can be promoted to directly activate PPP2CA, so that phosphorylation in estrogen signal cascade is reduced, and the activity of an estrogen receptor alpha (ER alpha) is reduced.

Described herein are endoxifen compositions comprising novel compounds and methods of use thereof. Methods of synthesis for the compositions are described herein. The endoxifen compositions described herein may exhibit aromatase inhibition activity or estrogen receptor activity. The endoxifen compositions described herein may be useful in the treatment of a condition in a subject, such as cancer.

Described herein are pharmaceutical compounds and compositions and methods of making thereof. Methods of synthesis for the compounds are described herein. The compounds or compositions described herein may exhibit aromatase inhibition activity or estrogen receptor activity. The compounds and compositions described herein may be useful in the treatment of a condition in a subject.

Pharmaceutical compounds, pharmaceutical compositions, and methods for their preparation are described herein. Methods of synthesis of these compounds are described herein. The compounds or compositions described herein may have aromatase inhibitory activity or estrogen receptor activity. The compounds and compositions described herein may contribute to the treatment of a condition in a subject.

Described herein are compositions and methods for treating Duchenne muscular dystrophy (DMD) in a subject with DMD or a carrier of the DMD gene using (Z)-endoxifen. (Z)-endoxifen modulates estrogen receptor activity and protein kinase signaling, stabilizes calcium levels, and reduces oxidative stress, which mitigate muscle deterioration associated with DMD. A therapeutically effective amount of (Z)-endoxifen is administered, either alone or in combination with other treatments such as corticosteroids or ataluren, in various formulations including oral, topical, and inhalation forms. The (Z)-endoxifen may be formulated as sustained or delayed-release to enhance therapeutic efficacy.

The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, ester, isomer, solvate, prodrug or isotopically labeled compound thereof. The structure of the compound of formula (I) is as follows: The compound has excellent inhibitory ability for selectively inhibiting estrogen receptor activity and anti-proliferative activity against human breast cancer cell line MCF-7 cell line of estrogen receptor wild type, Y537S and D538G mutants. The compound provided by the present invention can be used for preventing and / or treating estrogen receptor-mediated or -dependent diseases and disorders.