Search results for "SERD"
showing 3 items of 3 documents
Balanced dual acting compounds targeting aromatase and estrogen receptor α as an emerging therapeutic opportunity to counteract estrogen responsive b…
2021
Abstract Breast Cancer (BC) is a leading cause of death in women, currently affecting 13% of female population worldwide. First-line clinical treatments against Estrogen Receptor positive (ER+) BC rely on suppressing estrogen production, by inhibiting the aromatase (AR) enzyme, or on blocking estrogen-dependent pro-oncogenic signaling, by targeting Estrogen Receptor (ER) α with selective Modulators/Degraders (SERMs/SERDs). The development of dual acting molecules targeting AR and ERα represents a tantalizing alternative strategy to fight ER + BC, reducing the incidence of adverse effects and resistance onset that limit the effectiveness of these gold-standard therapies. Here, in silico desi…
La svolta galeriana prima e dopo l’editto di Serdica
2016
The crisis of the third century helped to create conditions for a change in terms of relations between the Roman Empire and Christianity, whose spread resulted, in the upper echelons of the State, in an awareness of the extent of the phenomenon. The measures that Roman State authorities took against Christianity were a reaction to this dangerous threat; among them, in the specific case of this paper, we focus on the persecution triggered – according to Lactantius – by the Caesar Galerius under the senior Augustus Diocletian. The same Galerius as Augustus was responsible for the formal act that put an end to persecutions: the edict of Serdica (or of Nicomedia), issued on 30 April of year 311…
Structural, Thermodynamic, and Kinetic Traits of Antiestrogen-Compounds Selectively Targeting the Y537S Mutant Estrogen Receptor α Transcriptional Ac…
2019
The most frequently diagnosed cancers in women are the estrogen receptor (ER)-positive breast cancer subtypes, which are characterized by estrogen dependency for their growth. The mainstay of clinical treatment for this tumor relies on the modulation of ER action or on the suppression of estrogen biosynthesis via the administration of Selective ERα Modulators/Down-regulators (SERMs/SERDs) or aromatase inhibitors, respectively. Nevertheless, de novo and acquired resistance to these therapies frequently occurs and represents a major clinical concern for patient survival. Recently, somatic mutations affecting the hormone-binding domain of ERα (i. e. Y537S, Y537N, D538G) have been associated w…