Estrogen Receptor and Breast Cancer: Celebrating the 60th Anniversary of the Discovery of ER PDF
Preview Estrogen Receptor and Breast Cancer: Celebrating the 60th Anniversary of the Discovery of ER
Cancer Drug Discovery and Development Xiaoting Zhang Editor Estrogen Receptor and Breast Cancer Celebrating the 60th Anniversary of the Discovery of ER Cancer Drug Discovery and Development Series editor: Beverly A. Teicher Bethesda, MD, USA The Cancer Drug Discovery and Development series (Beverly A Teicher, series editor) is the definitive book series in cancer research and oncology, providing comprehensive coverage of specific topics and the field. Volumes cover the process of drug discovery, preclinical models in cancer research, specific drug target groups and experimental and approved therapeutic agents. The volumes are current and timely, anticipating areas where experimental agents are reaching FDA approval. Each volume is edited by an expert in the field covered and chapters are authored by renowned scientists and physicians in their fields of interest. More information about this series at http://www.springer.com/series/7625 Xiaoting Zhang Editor Estrogen Receptor and Breast Cancer Celebrating the 60th Anniversary of the Discovery of ER Editor Xiaoting Zhang Department of Cancer Biology Vontz Center for Molecular Studies University of Cincinnati College of Medicine Cincinnati, OH, USA ISSN 2196-9906 ISSN 2196-9914 (electronic) Cancer Drug Discovery and Development ISBN 978-3-319-99349-2 ISBN 978-3-319-99350-8 (eBook) https://doi.org/10.1007/978-3-319-99350-8 Library of Congress Control Number: 2018958481 © Springer Nature Switzerland AG 2019 This work is subject to copyright. All rights are reserved by the Publisher, whether the whole or part of the material is concerned, specifically the rights of translation, reprinting, reuse of illustrations, recitation, broadcasting, reproduction on microfilms or in any other physical way, and transmission or information storage and retrieval, electronic adaptation, computer software, or by similar or dissimilar methodology now known or hereafter developed. The use of general descriptive names, registered names, trademarks, service marks, etc. in this publication does not imply, even in the absence of a specific statement, that such names are exempt from the relevant protective laws and regulations and therefore free for general use. The publisher, the authors and the editors are safe to assume that the advice and information in this book are believed to be true and accurate at the date of publication. Neither the publisher nor the authors or the editors give a warranty, express or implied, with respect to the material contained herein or for any errors or omissions that may have been made. The publisher remains neutral with regard to jurisdictional claims in published maps and institutional affiliations. This Humana Press imprint is published by the registered company Springer Nature Switzerland AG The registered company address is: Gewerbestrasse 11, 6330 Cham, Switzerland Preface A lady with growth neoplastic Thought castration was just a bit drastic. She preferred that her ill could be cured with a pill. Today it’s no longer fantastic. —Elwood V. Jensen, Ph.D. (1920–2012) Breast cancer is one of the most frequent cancers and a leading cause of death for women with an estimated one in eight women in the USA diagnosed in their life- time and more than 1.7 million new cases worldwide each year. Estrogen receptor (ER) is the key functional mediator of estrogen and plays prominent roles in breast cancer with about 75% of all breast cancer diagnosed as ER positive breast cancer. The discovery of ER by Dr. Elwood Jensen 60 years ago in 1958 through his “alter- native thinking approach” mirrored his successful climbing of the mountain Matterhorn in the Swiss Alps. His enchantment of implementing unconventional approaches has not only led to the birth of a whole new nuclear receptor research field but also made a rapid, direct, and long-lasting impact on the diagnosis, treat- ment, and prevention of breast cancer. As appropriately illustrated in the limerick excerpt above by Dr. Jensen himself and further noted by the Lasker Foundation: “The work transformed the treatment of breast cancer patients and saves or prolongs more than a 100,000 lives annually.” Since this landmark discovery, tremendous progress has been made in our understanding of the molecular functions of ER and in the development of targeted therapies against ER pathways for breast cancer treatment. However, there is currently no book available addressing these discover- ies and the recent advancements in a historical and systematic fashion. I appreciate the kind and timely invitation from Mr. William Helms, Associate Editor of Cancer Research, and Dr. Beverly Teicher for the task of spearheading this book. My goal for the book is to celebrate the 60th anniversary of the discovery of ER and the great achievements that have followed by providing comprehensive and most up-to-date information on the history and recent advancement of the field spanning from basic research to clinical practice. The chapters are contributed by world-renowned leaders in the field and include the history behind the discovery of v vi Preface ER (Khan); physiological and pathological roles of ER (Korach); recent advancement of our understanding of ER-mediated gene transcription and cistrome (Zhang), Cryo-EM structural insights into ER coactivators (O’Malley), ER transcriptome (Kraus) and its regulation of newly classified noncoding RNAs in breast cancer (Nephew); personal account of the development of Tamoxifen as the first targeted cancer therapy and new generation of antiestrogens for breast cancer treatment (Jordan) and their current practice in clinics (Ellis); structural basis of ER and anti- estrogen actions (Burris); molecular insights into endocrine resistance (Schiff and Osborne); the role of ER-beta (Thomas and Gustafsson) and environmental estro- gens, especially Bisphenol A (Ben-Jonathan), in breast cancer; and emerging state- of- the-art therapeutic regimens and approaches to overcome treatment resistance (Zhang). I would like to sincerely thank all of the authors for their time, commitment, and highly enthusiastic devotion to this important book despite the short notice, their very busy schedules, and many administrative duties. With the outstanding work done by all of the contributors, I am happy to say that collectively we have fully accomplished our original goal of editing this book. We hope it will provide under- graduate and graduate students, basic scientists, clinical cancer researchers, resi- dents, fellows, as well as clinicians, oncology educators, and the general public with a thorough and authoritative review of the key topics in this vital field of both basic and clinical significance. We would like to hear your feedback and look forward to incorporating those in our next edition of the book with an update of the new and most exciting developments in the field. The past 60 years’ work on estrogen receptor has been extraordinary in not only providing basic insights into estrogen receptor functions but also developing highly effective novel diagnostic and therapeutic approaches for the treatment of this dev- astating disease. With rapid technological advancement in emerging areas such as genomic, single cell and single molecule studies, we will be able to better under- stand estrogen receptor functions, breast cancer therapeutic resistance mechanisms, tumor heterogeneity, and interactions with the tumor microenvironment and immune system at both the individual and population levels. Combining the current develop- ment of creative targeted drug delivery systems and innovative therapeutic approaches, the knowledge gained will likely be translated into clinics more quickly and smoothly to further benefit patient care as well. We fully expect the next 60 years to be just as exciting and groundbreaking. Stay tuned! Cincinnati, OH, USA Xiaoting Zhang Contents Estrogen Receptor and Breast Cancer: A Historical Perspective. . . . . . . . 1 Sohaib Khan Physiological and Pathological Roles of Estrogen Receptor . . . . . . . . . . . . 15 Kenneth S. Korach, Sylvia C. Hewitt, Katherine J. Hamilton, Yin Li, J. Tyler Ramsey, Marleny Garcia, Emilie Mathura, and Yukitomo Arao Estrogen Receptor-Mediated Gene Transcription and Cistrome . . . . . . . . 49 Gregory Bick, Dan Zhao, and Xiaoting Zhang Structural Studies with Coactivators for the Estrogen Receptor . . . . . . . . 71 Ping Yi, Zhao Wang, and Bert W. O’Malley The Estrogen-Regulated Transcriptome: Rapid, Robust, Extensive, and Transient . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 95 Yasmin M. Vasquez and W. Lee Kraus Estrogen Receptor Regulation of MicroRNAs in Breast Cancer . . . . . . . . 129 Nicholas Pulliam, Jessica Tang, and Kenneth P. Nephew The First Targeted Therapy to Treat Cancer: The Tamoxifen Tale . . . . . . 151 Balkees Abderrahman and V. Craig Jordan A Novel Strategy to Improve Women’s Health: Selective Estrogen Receptor Modulators . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 189 Balkees Abderrahman and V. Craig Jordan Endocrine Therapy in Clinical Practice . . . . . . . . . . . . . . . . . . . . . . . . . . . . 215 Tomas Reinert, Ryoichi Matsunuma, Airi Han, and Matthew J. Ellis Structural Insights into Estrogen Receptors and Antiestrogen Therapies . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 241 Ian Mitchelle S. de Vera, Udayanga S. Wanninayake, and Thomas P. Burris vii viii Contents Molecular Mechanisms of Endocrine Resistance . . . . . . . . . . . . . . . . . . . . . 265 Xiaoyong Fu, Carmine De Angelis, Jamunarani Veeraraghavan, C. Kent Osborne, and Rachel Schiff Estrogen Receptor β and Breast Cancer . . . . . . . . . . . . . . . . . . . . . . . . . . . . 309 Christoforos Thomas and Jan-Åke Gustafsson Endocrine Disrupting Chemicals and Breast Cancer: The Saga of Bisphenol A . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 343 Nira Ben-Jonathan Emerging Therapeutic Approaches to Overcome Breast Cancer Endocrine Resistance . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 379 Marissa Leonard, Juan Tan, Yongguang Yang, Mahmoud Charif, Elyse E. Lower, and Xiaoting Zhang Appendix: Photo Gallery . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 405 Index . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 407 Contributors Balkees Abderrahman Department of Breast Medical Oncology, University of Texas, MD Anderson Cancer Center, Houston, TX, USA Yukitomo Arao Receptor Biology Section, Reproductive and Developmental Biology Laboratory, National Institute Environmental Health Sciences, National Institutes of Health, Durham, NC, USA Nira Ben-Jonathan Department of Cancer Biology, University of Cincinnati, Cincinnati, OH, USA Gregory Bick Department of Cancer Biology, University of Cincinnati College of Medicine, Cincinnati, OH, USA Thomas P. Burris Center for Clinical Pharmacology, Washington University School of Medicine and St. Louis College of Pharmacy, St. Louis, MO, USA Mahmoud Charif Division of Hematology and Oncology, Department of Internal Medicine, University of Cincinnati College of Medicine, Cincinnati, OH, USA Carmine De Angelis Lester and Sue Smith Breast Center, Baylor College of Medicine, Houston, TX, USA Dan L. Duncan Comprehensive Cancer Center, Baylor College of Medicine, Houston, TX, USA Ian Mitchelle S. de Vera Department of Pharmacology and Physiology, Saint Louis University School of Medicine, St. Louis, MO, USA Matthew J. Ellis Lester and Sue Smith Breast Center, Baylor College of Medicine, Houston, TX, USA Xiaoyong Fu Lester and Sue Smith Breast Center, Baylor College of Medicine, Houston, TX, USA Dan L. Duncan Comprehensive Cancer Center, Baylor College of Medicine, Houston, TX, USA ix
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