2010年菲利普·S·波托盖斯药物化学讲座：探讨雌激素受体配体设计中的“核心问题” - Suppr

Suppr

超能文献

The 2010 Philip S. Portoghese Medicinal Chemistry Lectureship: addressing the "core issue" in the design of estrogen receptor ligands.

作者信息

Katzenellenbogen John A

机构信息

Department of Chemistry, University of Illinois, Urbana, Illinois 61801, United States.

出版信息

J Med Chem. 2011 Aug 11;54(15):5271-82. doi: 10.1021/jm200801h. Epub 2011 Jul 11.

DOI:10.1021/jm200801h

PMID:21707083

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3150643/

Abstract

摘要

相似文献

The 2010 Philip S. Portoghese Medicinal Chemistry Lectureship: addressing the "core issue" in the design of estrogen receptor ligands.

J Med Chem. 2011 Aug 11;54(15):5271-82. doi: 10.1021/jm200801h. Epub 2011 Jul 11.

Synthesis and activity of substituted 4-(indazol-3-yl)phenols as pathway-selective estrogen receptor ligands useful in the treatment of rheumatoid arthritis.

J Med Chem. 2004 Dec 16;47(26):6435-8. doi: 10.1021/jm049194+.

Design and evaluation of fragment-like estrogen receptor tetrahydroisoquinoline ligands from a scaffold-detection approach.

J Med Chem. 2011 Apr 14;54(7):2005-11. doi: 10.1021/jm1011116. Epub 2011 Mar 7.

[Towards bisphenols without hormonal effects].

Med Sci (Paris). 2013 Jan;29(1):14-7. doi: 10.1051/medsci/2013291004. Epub 2013 Jan 25.

Steroidal bivalent ligands for the estrogen receptor: design, synthesis, characterization and binding affinities.

Bioorg Med Chem. 2009 May 15;17(10):3528-35. doi: 10.1016/j.bmc.2009.04.016. Epub 2009 Apr 12.

Computational insights into the mechanism of ligand unbinding and selectivity of estrogen receptors.

J Phys Chem B. 2009 Jul 30;113(30):10436-44. doi: 10.1021/jp903785h.

Salicylaldoxime moiety as a phenolic "A-Ring" substitute in estrogen receptor ligands.

J Med Chem. 2001 Nov 22;44(24):4288-91. doi: 10.1021/jm010948j.

Protein structure-based design, synthesis strategy and in vitro pharmacological characterization of estrogen receptor alpha and beta selective compounds.

Ernst Schering Res Found Workshop. 2004(46):47-62. doi: 10.1007/978-3-662-05386-7_4.

Synthesis and crystal structure of a phosphorylated estrogen receptor ligand binding domain.

Chembiochem. 2010 Nov 2;11(16):2251-4. doi: 10.1002/cbic.201000532.

Aliphatic substitution of o-carboranyl phenols enhances estrogen receptor beta selectivity.

Chem Pharm Bull (Tokyo). 2014;62(4):386-91. doi: 10.1248/cpb.c13-00796.

引用本文的文献

Endocrine-Disrupting Activities of Flavones on Steroid Receptors: Structural Requirements and Synthesis of Novel Flavone with Improved Estrogenic Activity.

Biomedicines. 2025 Mar 19;13(3):748. doi: 10.3390/biomedicines13030748.

Discovery of novel covalent selective estrogen receptor degraders against endocrine-resistant breast cancer.

Acta Pharm Sin B. 2023 Dec;13(12):4963-4982. doi: 10.1016/j.apsb.2023.05.005. Epub 2023 May 12.

A New Chemotype of Chemically Tractable Nonsteroidal Estrogens Based on a Thieno[2,3-]pyrimidine Core.

ACS Med Chem Lett. 2022 Jun 10;13(7):1151-1158. doi: 10.1021/acsmedchemlett.2c00180. eCollection 2022 Jul 14.

Heterodimeric GW7604 Derivatives: Modification of the Pharmacological Profile by Additional Interactions at the Coactivator Binding Site.

J Med Chem. 2021 May 13;64(9):5766-5786. doi: 10.1021/acs.jmedchem.0c02230. Epub 2021 Apr 27.

Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors.

J Med Chem. 2020 Oct 8;63(19):11085-11099. doi: 10.1021/acs.jmedchem.0c01001. Epub 2020 Sep 22.

Rational design and optimization of selenophenes with basic side chains as novel potent selective estrogen receptor modulators (SERMs) for breast cancer therapy.

Medchemcomm. 2017 May 24;8(7):1485-1497. doi: 10.1039/c7md00163k. eCollection 2017 Jul 1.

A trisubstituted pyrazole derivative reduces DMBA-induced mammary tumor growth in rats by inhibiting estrogen receptor-α expression.

Mol Cell Biochem. 2018 Dec;449(1-2):137-144. doi: 10.1007/s11010-018-3350-8. Epub 2018 May 18.

Emerging Estrogenic Pollutants in the Aquatic Environment and Breast Cancer.

Genes (Basel). 2017 Sep 15;8(9):229. doi: 10.3390/genes8090229.

Improved Estrogen Receptor Assessment by PET Using the Novel Radiotracer F-4FMFES in Estrogen Receptor-Positive Breast Cancer Patients: An Ongoing Phase II Clinical Trial.

J Nucl Med. 2018 Feb;59(2):197-203. doi: 10.2967/jnumed.117.194654. Epub 2017 Aug 10.

Adamantyl Antiestrogens with Novel Side Chains Reveal a Spectrum of Activities in Suppressing Estrogen Receptor Mediated Activities in Breast Cancer Cells.

J Med Chem. 2017 Jul 27;60(14):6321-6336. doi: 10.1021/acs.jmedchem.7b00585. Epub 2017 Jul 14.

本文引用的文献

An ADIOL-ERβ-CtBP transrepression pathway negatively regulates microglia-mediated inflammation.

Cell. 2011 May 13;145(4):584-95. doi: 10.1016/j.cell.2011.03.050.

Structure of estradiol metal chelate and estrogen receptor complex: the basis for designing a new class of selective estrogen receptor modulators.

J Med Chem. 2011 May 26;54(10):3575-80. doi: 10.1021/jm200192y. Epub 2011 Apr 19.

Synthesis and investigations on the oxidative degradation of C3/C5-alkyl-1,2,4-triarylpyrroles as ligands for the estrogen receptor.

ChemMedChem. 2011 May 2;6(5):794-803. doi: 10.1002/cmdc.201000537. Epub 2011 Mar 17.

Estrogen receptors: therapies targeted to receptor subtypes.

Clin Pharmacol Ther. 2011 Jan;89(1):44-55. doi: 10.1038/clpt.2010.226. Epub 2010 Dec 1.

Identification of ligand-selective peptide antagonists of the mineralocorticoid receptor using phage display.

Mol Endocrinol. 2011 Jan;25(1):32-43. doi: 10.1210/me.2010-0193. Epub 2010 Nov 24.

Genomic collaboration of estrogen receptor alpha and extracellular signal-regulated kinase 2 in regulating gene and proliferation programs.

Mol Cell Biol. 2011 Jan;31(1):226-36. doi: 10.1128/MCB.00821-10. Epub 2010 Oct 18.

Non-nuclear estrogen receptor alpha signaling promotes cardiovascular protection but not uterine or breast cancer growth in mice.

J Clin Invest. 2010 Jul;120(7):2319-30. doi: 10.1172/JCI38291. Epub 2010 Jun 23.

Estrogen receptor β ligands: recent advances and biomedical applications.

Med Res Rev. 2011 May;31(3):364-442. doi: 10.1002/med.20186.

Genome-wide dynamics of chromatin binding of estrogen receptors alpha and beta: mutual restriction and competitive site selection.

Mol Endocrinol. 2010 Jan;24(1):47-59. doi: 10.1210/me.2009-0252. Epub 2009 Nov 6.

Differential presentation of protein interaction surfaces on the androgen receptor defines the pharmacological actions of bound ligands.

Chem Biol. 2009 Apr 24;16(4):452-60. doi: 10.1016/j.chembiol.2009.01.016.

文献AI研究员

20分钟写一篇综述，助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型，支持多种主流文档格式。

立即体验