A5040694487- Intraocular Surgery and Lenses
- Corneal surgery and disorders
- Glaucoma and retinal disorders
- Ophthalmology and Visual Impairment Studies
- Corneal Surgery and Treatments
- Estrogen and related hormone effects
- Ocular Surface and Contact Lens
- Ocular Infections and Treatments
- Lymphatic System and Diseases
- Retinal and Macular Surgery
- Computational Drug Discovery Methods
- Retinal and Optic Conditions
- Ocular Diseases and Behçet’s Syndrome
- Bioactive Compounds and Antitumor Agents
- Retinoids in leukemia and cellular processes
- Traumatic Ocular and Foreign Body Injuries
- Ocular Disorders and Treatments
- Global Healthcare and Medical Tourism
- Receptor Mechanisms and Signaling
- Retinal Diseases and Treatments
- Ocular Oncology and Treatments
- Angiogenesis and VEGF in Cancer
- Synthesis and biological activity
- MicroRNA in disease regulation
- Prostate Cancer Treatment and Research
University Hospital Ayr
2012-2023
Creative Commons
2023
Alcon (United States)
2023
Cataract and Refractive Institute of Florida
2023
University of Almería
2023
Medicon
2023
October 6 University
2022
Phipps Houses
2022
Bridge University
2022
Dr. Jose N. Rodriguez Memorial Hospital
2022
The estrogen-dependent inflammatory and neuroangiogenic activities that drive endometriosis can be suppressed by estrogen receptor ligands in mice.
Resveratrol has beneficial effects on aging, inflammation and metabolism, which are thought to result from activation of the lysine deacetylase, sirtuin 1 (SIRT1), cAMP pathway, or AMP-activated protein kinase. In this study, we report that resveratrol acts as a pathway-selective estrogen receptor-α (ERα) ligand modulate inflammatory response but not cell proliferation. A crystal structure ERα ligand-binding domain (LBD) complex with revealed unique perturbation coactivator-binding surface,...
Abstract A subset of nuclear receptors (NRs) function as obligate heterodimers with retinoid X receptor (RXR), allowing integration ligand-dependent signals across the dimer interface via an unknown structural mechanism. Using magnetic resonance (NMR) spectroscopy, x-ray crystallography and hydrogen/deuterium exchange (HDX) mass spectrometry, here we show allosteric mechanism through which RXR co-operates a permissive partner, peroxisome proliferator-activated (PPAR)-γ, while rendered...
Human vascular malformations cause disease as a result of changes in blood flow and hemodynamic forces. Although the genetic mutations that underlie formation many human are known, extent to which abnormal can subsequently influence program natural history is not. Loss SH2 domain–containing leukocyte protein 76 kDa (SLP76) resulted malformation directed through mesenteric lymphatic vessels after birth mice. Mesenteric position congenital mature Slp76-null mice lacked identity expressed...
To probe the importance of heterocyclic core estrogen receptor (ER) ligands, we prepared a series thiophene-core ligands by Suzuki cross-coupling aryl boronic acids with bromo-thiophenes and assessed their binding cell biological activities. The disposition phenol substituents on thiophene core, at alternate or adjacent sites, nature these phenols, all contribute to affinity subtype selectivity. Most bis(hydroxyphenyl)-thiophenes were ERβ selective, whereas tris(hydroxyphenyl)-thiophenes ERα...
Abstract Some estrogen receptor‐α ( ER α)‐targeted breast cancer therapies such as tamoxifen have tissue‐selective or cell‐specific activities, while others similar activities in different cell types. To identify biophysical determinants of signaling and proliferation, we synthesized 241 α ligands based on 19 chemical scaffolds, compared ligand response using quantitative bioassays for canonical X‐ray crystallography. Ligands that regulate the dynamics stability coactivator‐binding site...
In this study we report that deletion of E6-associated protein (E6-AP) in mice results a smaller prostate gland compared with normal wild-type animals. To investigate the mechanism(s) by which E6-AP affects growth and development, carried out both vitro vivo experiments. show interacts androgen receptor (AR) hormone-dependent manner enhances transactivation function AR. Our data from E6-AP-null glands level AR is elevated while target protein, probasin, decreased. contrast, decreased, its...
Significance To address the unmet clinical need for effectively suppressing estrogen receptor (ER) activity with both de novo resistance and in advanced ER-positive breast cancers that are resistant to standard-of-care antiestrogens, we have developed dual-mechanism ER inhibitors (DMERIs) employ two distinct ER-targeting moieties. These DMERI elicited noncanonical structural perturbations of ligand-binding domain stabilized multiple antagonist substates within dimer generate highly...