A5076319928- Protein Degradation and Inhibitors
- Advanced Breast Cancer Therapies
- Histone Deacetylase Inhibitors Research
- Chromatin Remodeling and Cancer
- HER2/EGFR in Cancer Research
- Ubiquitin and proteasome pathways
- CAR-T cell therapy research
- Multiple Myeloma Research and Treatments
- Asymmetric Hydrogenation and Catalysis
- Organometallic Complex Synthesis and Catalysis
- Management and Marketing Education
- Lanthanide and Transition Metal Complexes
- Themes in Literature Analysis
- Magnetism in coordination complexes
- Music Technology and Sound Studies
- Carbon dioxide utilization in catalysis
- Business Strategies and Innovation
- Business Strategy and Innovation
- Diverse Musicological Studies
- Coordination Chemistry and Organometallics
- Music History and Culture
- Metal complexes synthesis and properties
Arvinas (United States)
2017-2024
Université de Strasbourg
2015
West Virginia University
2005
Morgantown High School
2002
Proteolysis targeting chimeras (PROTACs) are bifunctional molecules that recruit an E3 ligase to a target protein facilitate ubiquitination and subsequent degradation of protein. While the field targeted degraders is still relatively young, potential for this modality become differentiated therapeutic reality strong, such both academic pharmaceutical institutions now entering interesting area research. In article, we describe broadly applicable process identifying degrader hits based on...
Abstract Purpose: Estrogen receptor (ER) alpha signaling is a known driver of ER-positive (ER+)/human epidermal growth factor 2 negative (HER2−) breast cancer. Combining endocrine therapy (ET) such as fulvestrant with CDK4/6, mTOR, or PI3K inhibitors has become central strategy in the treatment ER+ advanced However, suboptimal ER inhibition and resistance resulting from ESR1 mutation dictates that new therapies are needed. Experimental Design: A medicinal chemistry campaign identified...
The immunomodulatory drugs (IMiDs) thalidomide, pomalidomide, and lenalidomide have been approved for the treatment of multiple myeloma many years. Recently, their use as E3 ligase recruiting elements small-molecule-induced protein degradation has led to a resurgence in interest IMiD synthesis functionalization. Traditional follows stepwise route with purification steps. Herein we describe novel one-pot without that provides rapid access multitude analogues. Binding studies target cereblon...
Efficient synthetic routes for the preparation of electrophilic titanium and zirconium complexes featuring a tridentate diamidoamine ligand have been developed. The five-coordinate dichloride [(MesNCH2CH2)2NR]TiCl2 (R = H (3), SiMe3 (4)) are conveniently prepared from amine elimination reactions triamines (MesNHCH2CH2)2NR (1), (2)) with Ti(NEt2)2Cl2. Treatment Ti(NEt2)4 2 equiv SiMe3Cl offers an effective method corresponding homologues [(MesNCH2CH2)2NR]ZrCl2 (5), (6)) synthesized via...
<div>AbstractPurpose:<p>Estrogen receptor (ER) alpha signaling is a known driver of ER-positive (ER<sup>+</sup>)/human epidermal growth factor 2 negative (HER2<sup>−</sup>) breast cancer. Combining endocrine therapy (ET) such as fulvestrant with CDK4/6, mTOR, or PI3K inhibitors has become central strategy in the treatment ER<sup>+</sup> advanced However, suboptimal ER inhibition and resistance resulting from <i>ESR1</i> mutation...
Well said by Will Durant - "The future never simply happened. It was made". A business association needs to characterize its aggressive technique guide and center choices, increase maintainable upper hand over adversaries make the effective in long run. Authoritative results are outcomes of choices made pioneers. The system that aides centers situating is called focused methodology. reason for procedure practical adversaries. In this article, we will go through nomenclature contextual...
<p>Supplementary Tables S1-S4 and Figures S1-S16</p>
<p>Extended Methods</p>
<div>AbstractPurpose:<p>Estrogen receptor (ER) alpha signaling is a known driver of ER-positive (ER<sup>+</sup>)/human epidermal growth factor 2 negative (HER2<sup>−</sup>) breast cancer. Combining endocrine therapy (ET) such as fulvestrant with CDK4/6, mTOR, or PI3K inhibitors has become central strategy in the treatment ER<sup>+</sup> advanced However, suboptimal ER inhibition and resistance resulting from <i>ESR1</i> mutation...
<p>Extended Methods</p>
<p>Supplementary Tables S1-S4 and Figures S1-S16</p>
Abstract The mammalian SWI/SNF complex catalyzes the remodeling of chromatin through helicase activity two mutually-exclusive, paralogous subunits, BRG1 and BRM. is frequently mutated in cancer its inactivation results a cellular dependence on Despite attractiveness BRM as synthetic lethal therapeutic target, selective inhibition represents considerable challenge due to high degree homology between BRG1. Furthermore, published data indicate that achieving such selectivity likely essential...