Discovery of novel covalent selective estrogen receptor degraders against endocrine-resistant breast cancer
Open Access
- 11 May 2023
- journal article
- research article
- Published by Elsevier in Acta Pharmaceutica Sinica B
- Vol. 13 (12) , 4963-4982
Abstract
No abstract availableKeywords
Funding Information
- National Key Research and Development Program of China (2020YFA0908800, 2021YFC2100300)
- Fundamental Research Funds for the Central Universities (2042022kf0056)
- China Postdoctoral Science Foundation (2020M672435)
- National Natural Science Foundation of China (81773557, 82073690, 82103994, 82173676, 82273774)
This publication has 44 references indexed in Scilit:
- High-Throughput Screening Assays for Estrogen Receptor by Using Coumestrol, a Natural Fluorescence CompoundSLAS Discovery, 2014
- Discovery of a Potent and Isoform-Selective Targeted Covalent Inhibitor of the Lipid Kinase PI3KαJournal of Medicinal Chemistry, 2013
- Strategies for the discovery and development of therapies for metastatic breast cancerNature Reviews Drug Discovery, 2012
- Development of Selective Estrogen Receptor Modulator (SERM)‐Like Activity Through an Indirect Mechanism of Estrogen Receptor Antagonism: Defining the Binding Mode of 7‐Oxabicyclo[2.2.1]hept‐5‐ene Scaffold Core LigandsChemMedChem, 2012
- Incidence of Breast Cancer in the United States: Current and Future TrendsJNCI: Journal of the National Cancer Institute, 2011
- The 2010 Philip S. Portoghese Medicinal Chemistry Lectureship: Addressing the “Core Issue” in the Design of Estrogen Receptor LigandsJournal of Medicinal Chemistry, 2011
- The resurgence of covalent drugsNature Reviews Drug Discovery, 2011
- Quantitative reactivity profiling predicts functional cysteines in proteomesNature, 2010
- Synthesis and Evaluation of Estrogen Receptor Ligands with Bridged Oxabicyclic Cores Containing a Diarylethylene Motif: Estrogen Antagonists of Unusual StructureJournal of Medicinal Chemistry, 2005
- Cysteine 530 of the Human Estrogen Receptor α Is the Main Covalent Attachment Site of 11β-(Aziridinylalkoxyphenyl)estradiolsBiochemistry, 1999