Publications by authors named "Donna McEachern"

39Publications

Discovery of CJ-2360 as a Potent and Orally Active Inhibitor of Anaplastic Lymphoma Kinase Capable of Achieving Complete Tumor Regression.

Authors:
Jianyong Chen Yunlong Zhou Xuyuan Dong Liu Liu Longchuan Bai Donna McEachern Sally Przybranowski Chao-Yie Yang Jeanne Stuckey Xiaoqin Li Bo Wen Ting Zhao Siwei Sun Duxin Sun Lingling Jiao Yu Jing Ming Guo Dajun Yang Shaomeng Wang

J Med Chem 2020 11 13;63(22):13994-14016. Epub 2020 Nov 13.

Rogel Cancer Center and Departments of Internal Medicine, Pharmacology, and Medicinal Chemistry, University of Michigan, Ann Arbor, Michigan 48109, United States.

View Article and Find Full Text PDF
November 2020

A highly potent PROTAC androgen receptor (AR) degrader ARD-61 effectively inhibits AR-positive breast cancer cell growth in vitro and tumor growth in vivo.

Authors:
Lijie Zhao Xin Han Jianfeng Lu Donna McEachern Shaomeng Wang

Neoplasia 2020 10;22(10):522-532

Department of Internal Medicine, University of Michigan, Ann Arbor, MI 48109, United States; Department of Pharmacology, University of Michigan, Ann Arbor, MI 48109, United States; Department of Medicinal Chemistry, University of Michigan, Ann Arbor, MI 48109, United States; Rogel Cancer Center, University of Michigan, Ann Arbor, MI 48109, United States. Electronic address:

View Article and Find Full Text PDF
October 2020

EEDi-5285: An Exceptionally Potent, Efficacious, and Orally Active Small-Molecule Inhibitor of Embryonic Ectoderm Development.

Authors:
Rohan Kalyan Rej Changwei Wang Jianfeng Lu Mi Wang Elyse Petrunak Kaitlin P Zawacki Donna McEachern Ester Fernandez-Salas Chao-Yie Yang Lu Wang Ruiting Li Krishnapriya Chinnaswamy Bo Wen Duxin Sun Jeanne Stuckey Yunlong Zhou Jianyong Chen Guozhi Tang Shaomeng Wang

J Med Chem 2020 07 24;63(13):7252-7267. Epub 2020 Jun 24.

Rogel Cancer Center, Departments of Internal Medicine and Pharmacology, Medical School, and Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor, Michigan 48109, United States.

View Article and Find Full Text PDF
July 2020

Discovery of M-808 as a Highly Potent, Covalent, Small-Molecule Inhibitor of the Menin-MLL Interaction with Strong Antitumor Activity.

Authors:
Shilin Xu Angelo Aguilar Liyue Huang Tianfeng Xu Ke Zheng Donna McEachern Sally Przybranowski Caroline Foster Kaitlin Zawacki Zhaomin Liu Krishnapriya Chinnaswamy Jeanne Stuckey Shaomeng Wang

J Med Chem 2020 05 27;63(9):4997-5010. Epub 2020 Apr 27.

View Article and Find Full Text PDF
May 2020

Structure-Based Discovery of SD-36 as a Potent, Selective, and Efficacious PROTAC Degrader of STAT3 Protein.

Authors:
Haibin Zhou Longchuan Bai Renqi Xu Yujun Zhao Jianyong Chen Donna McEachern Krishnapriya Chinnaswamy Bo Wen Lipeng Dai Praveen Kumar Chao-Yie Yang Zhaomin Liu Mi Wang Liu Liu Jennifer L Meagher Han Yi Duxin Sun Jeanne A Stuckey Shaomeng Wang

J Med Chem 2019 12 10;62(24):11280-11300. Epub 2019 Dec 10.

View Article and Find Full Text PDF
December 2019

A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo.

Authors:
Longchuan Bai Haibin Zhou Renqi Xu Yujun Zhao Krishnapriya Chinnaswamy Donna McEachern Jianyong Chen Chao-Yie Yang Zhaomin Liu Mi Wang Liu Liu Hui Jiang Bo Wen Praveen Kumar Jennifer L Meagher Duxin Sun Jeanne A Stuckey Shaomeng Wang

Cancer Cell 2019 11;36(5):498-511.e17

Rogel Cancer Center, University of Michigan, Ann Arbor, MI 48109, USA; Department of Internal Medicine, University of Michigan, Ann Arbor, MI 48109, USA; Department of Pharmacology, University of Michigan, Ann Arbor, MI 48109, USA; Department of Medicinal Chemistry, University of Michigan, Ann Arbor, MI 48109, USA. Electronic address:

View Article and Find Full Text PDF
November 2019

Structure-Based Discovery of M-89 as a Highly Potent Inhibitor of the Menin-Mixed Lineage Leukemia (Menin-MLL) Protein-Protein Interaction.

Authors:
Angelo Aguilar Ke Zheng Tianfeng Xu Shilin Xu Liyue Huang Ester Fernandez-Salas Liu Liu Denzil Bernard Kaitlin P Harvey Caroline Foster Donna McEachern Jeanne Stuckey Krishnapriya Chinnaswamy James Delproposto Jeff W Kampf Shaomeng Wang

J Med Chem 2019 07 22;62(13):6015-6034. Epub 2019 Jun 22.

View Article and Find Full Text PDF
July 2019

Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression.

Authors:
Yangbing Li Jiuling Yang Angelo Aguilar Donna McEachern Sally Przybranowski Liu Liu Chao-Yie Yang Mi Wang Xin Han Shaomeng Wang

J Med Chem 2019 01 10;62(2):448-466. Epub 2018 Dec 10.

View Article and Find Full Text PDF
January 2019

Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression.

Authors:
Chong Qin Yang Hu Bing Zhou Ester Fernandez-Salas Chao-Yie Yang Liu Liu Donna McEachern Sally Przybranowski Mi Wang Jeanne Stuckey Jennifer Meagher Longchuan Bai Zhuo Chen Mei Lin Jiuling Yang Danya N Ziazadeh Fuming Xu Jiantao Hu Weiguo Xiang Liyue Huang Siwei Li Bo Wen Duxin Sun Shaomeng Wang

J Med Chem 2018 Aug 18;61(15):6685-6704. Epub 2018 Jul 18.

View Article and Find Full Text PDF
August 2018

Compliance With the National SEP-1 Quality Measure and Association With Sepsis Outcomes: A Multicenter Retrospective Cohort Study.

Authors:
Chanu Rhee Michael R Filbin Anthony F Massaro Amy L Bulger Donna McEachern Kathleen A Tobin Barrett T Kitch Bert Thurlo-Walsh Aran Kadar Alexandra Koffman Anupam Pande Yasir Hamad David K Warren Travis M Jones Cara O'Brien Deverick J Anderson Rui Wang Michael Klompas

Crit Care Med 2018 10;46(10):1585-1591

Department of Population Medicine, Harvard Medical School/Harvard Pilgrim Health Care Institute, Boston, MA.

View Article and Find Full Text PDF
October 2018

Structure-Based Discovery of CF53 as a Potent and Orally Bioavailable Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitor.

Authors:
Yujun Zhao Bing Zhou Longchuan Bai Liu Liu Chao-Yie Yang Jennifer L Meagher Jeanne A Stuckey Donna McEachern Sally Przybranowski Mi Wang Xu Ran Angelo Aguilar Yang Hu Jeff W Kampf Xiaoqin Li Ting Zhao Siwei Li Bo Wen Duxin Sun Shaomeng Wang

J Med Chem 2018 07 17;61(14):6110-6120. Epub 2018 Jul 17.

View Article and Find Full Text PDF
July 2018

Design of the First-in-Class, Highly Potent Irreversible Inhibitor Targeting the Menin-MLL Protein-Protein Interaction.

Authors:
Shilin Xu Angelo Aguilar Tianfeng Xu Ke Zheng Liyue Huang Jeanne Stuckey Krishnapriya Chinnaswamy Denzil Bernard Ester Fernández-Salas Liu Liu Mi Wang Donna McEachern Sally Przybranowski Caroline Foster Shaomeng Wang

Angew Chem Int Ed Engl 2018 02 15;57(6):1601-1605. Epub 2018 Jan 15.

Comprehensive Cancer and Departments of Internal Medicine, Pharmacology and Medicinal Chemistry, University of Michigan, 1600 Huron Parkway, Ann Arbor, MI, 48109, USA.

View Article and Find Full Text PDF
February 2018

Structure-Based Discovery of 4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole (CD161) as a Potent and Orally Bioavailable BET Bromodomain Inhibitor.

Authors:
Yujun Zhao Longchuan Bai Liu Liu Donna McEachern Jeanne A Stuckey Jennifer L Meagher Chao-Yie Yang Xu Ran Bing Zhou Yang Hu Xiaoqin Li Bo Wen Ting Zhao Siwei Li Duxin Sun Shaomeng Wang

J Med Chem 2017 05 2;60(9):3887-3901. Epub 2017 May 2.

Comprehensive Cancer Center and Departments of Internal Medicine, Pharmacology, and Medicinal Chemistry, University of Michigan , Ann Arbor, Michigan 48109, United States.

View Article and Find Full Text PDF
May 2017

Discovery of 4-((3'R,4'S,5'R)-6″-Chloro-4'-(3-chloro-2-fluorophenyl)-1'-ethyl-2″-oxodispiro[cyclohexane-1,2'-pyrrolidine-3',3″-indoline]-5'-carboxamido)bicyclo[2.2.2]octane-1-carboxylic Acid (AA-115/APG-115): A Potent and Orally Active Murine Double Minute 2 (MDM2) Inhibitor in Clinical Development.

Authors:
Angelo Aguilar Jianfeng Lu Liu Liu Ding Du Denzil Bernard Donna McEachern Sally Przybranowski Xiaoqin Li Ruijuan Luo Bo Wen Duxin Sun Hengbang Wang Jianfeng Wen Guangfeng Wang Yifan Zhai Ming Guo Dajun Yang Shaomeng Wang

J Med Chem 2017 04 24;60(7):2819-2839. Epub 2017 Mar 24.

University of Michigan Comprehensive Cancer Center, and Departments of Internal Medicine, Pharmacology, and Medicinal Chemistry, University of Michigan , 1600 Huron Parkway, Ann Arbor, Michigan 48109, United States.

View Article and Find Full Text PDF
April 2017

Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression.

Authors:
Bing Zhou Jiantao Hu Fuming Xu Zhuo Chen Longchuan Bai Ester Fernandez-Salas Mei Lin Liu Liu Chao-Yie Yang Yujun Zhao Donna McEachern Sally Przybranowski Bo Wen Duxin Sun Shaomeng Wang

J Med Chem 2018 01 24;61(2):462-481. Epub 2017 Mar 24.

University of Michigan Comprehensive Cancer Center, and Departments of ‡Internal Medicine, §Pathology, ∥Pharmaceutical Sciences, ⊥Medicinal Chemistry, and #Pharmacology, University of Michigan , Ann Arbor, Michigan 48109, United States.

View Article and Find Full Text PDF
January 2018

Targeted Degradation of BET Proteins in Triple-Negative Breast Cancer.

Authors:
Longchuan Bai Bing Zhou Chao-Yie Yang Jiao Ji Donna McEachern Sally Przybranowski Hui Jiang Jiantao Hu Fuming Xu Yujun Zhao Liu Liu Ester Fernandez-Salas Jing Xu Yali Dou Bo Wen Duxin Sun Jennifer Meagher Jeanne Stuckey Daniel F Hayes Shunqiang Li Matthew J Ellis Shaomeng Wang

Cancer Res 2017 05 16;77(9):2476-2487. Epub 2017 Feb 16.

University of Michigan Comprehensive Cancer Center, University of Michigan, Ann Arbor, Michigan.

View Article and Find Full Text PDF
May 2017

Reactivation of p53 by MDM2 Inhibitor MI-77301 for the Treatment of Endocrine-Resistant Breast Cancer.

Authors:
Jianfeng Lu Donna McEachern Shunqiang Li Matthew J Ellis Shaomeng Wang

Mol Cancer Ther 2016 12 7;15(12):2887-2893. Epub 2016 Oct 7.

Department of Internal Medicine, University of Michigan Comprehensive Cancer Center, University of Michigan, Ann Arbor, Michigan.

View Article and Find Full Text PDF
December 2016

Significant Differences in the Development of Acquired Resistance to the MDM2 Inhibitor SAR405838 between In Vitro and In Vivo Drug Treatment.

Authors:
C Gianna Hoffman-Luca Chao-Yie Yang Jianfeng Lu Daniel Ziazadeh Donna McEachern Laurent Debussche Shaomeng Wang

PLoS One 2015 12;10(6):e0128807. Epub 2015 Jun 12.

University of Michigan Comprehensive Cancer Center, Ann Arbor, Michigan, United States of America; Department of Pharmacology, University of Michigan, Ann Arbor, Michigan, United States of America; Department of Internal Medicine, University of Michigan, Ann Arbor, Michigan, United States of America; Department of Medicinal Chemistry, University of Michigan, Ann Arbor, Michigan, United States of America.

View Article and Find Full Text PDF
April 2016

Elucidation of Acquired Resistance to Bcl-2 and MDM2 Inhibitors in Acute Leukemia In Vitro and In Vivo.

Authors:
C Gianna Hoffman-Luca Daniel Ziazadeh Donna McEachern Yujun Zhao Wei Sun Laurent Debussche Shaomeng Wang

Clin Cancer Res 2015 Jun 9;21(11):2558-68. Epub 2015 Mar 9.

University of Michigan Comprehensive Cancer Center, Ann Arbor, Michigan. Department of Pharmacology, University of Michigan, Ann Arbor, Michigan. Department of Internal Medicine, University of Michigan, Ann Arbor, Michigan. Department of Medicinal Chemistry, University of Michigan, Ann Arbor, Michigan.

View Article and Find Full Text PDF
June 2015

Design of chemically stable, potent, and efficacious MDM2 inhibitors that exploit the retro-mannich ring-opening-cyclization reaction mechanism in spiro-oxindoles.

Authors:
Angelo Aguilar Wei Sun Liu Liu Jianfeng Lu Donna McEachern Denzil Bernard Jeffrey R Deschamps Shaomeng Wang

J Med Chem 2014 Dec 12;57(24):10486-98. Epub 2014 Dec 12.

University of Michigan Comprehensive Cancer Center and Departments of Internal Medicine, Pharmacology, and Medicinal Chemistry, University of Michigan , 1500 East Medical Center Drive, Ann Arbor, Michigan 48109, United States.

View Article and Find Full Text PDF
December 2014