Publications by authors named "Angelo Aguilar"

18Publications

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.

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May 2020

Simple Structural Modifications Converting a Bona fide MDM2 PROTAC Degrader into a Molecular Glue Molecule: A Cautionary Tale in the Design of PROTAC Degraders.

Authors:
Jiuling Yang Yangbing Li Angelo Aguilar Zhaomin Liu Chao-Yie Yang Shaomeng Wang

J Med Chem 2019 11 21;62(21):9471-9487. Epub 2019 Oct 21.

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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.

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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.

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January 2019

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.

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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.

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February 2018

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.

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April 2017

Targeting the MDM2-p53 Protein-Protein Interaction for New Cancer Therapy: Progress and Challenges.

Authors:
Shaomeng Wang Yujun Zhao Angelo Aguilar Denzil Bernard Chao-Yie Yang

Cold Spring Harb Perspect Med 2017 May 1;7(5). Epub 2017 May 1.

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

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May 2017

Chemical synthesis of tetracyclic terpenes and evaluation of antagonistic activity on endothelin-A receptors and voltage-gated calcium channels.

Authors:
Jianyu Lu Angelo Aguilar Bende Zou Weier Bao Serkan Koldas Aibin Shi John Desper Philine Wangemann Xinmin Simon Xie Duy H Hua

Bioorg Med Chem 2015 Sep 27;23(17):5985-98. Epub 2015 Jun 27.

Department of Chemistry, Kansas State University, Manhattan, KS 66506, USA. Electronic address:

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September 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.

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December 2014

Small-molecule inhibitors of the MDM2-p53 protein-protein interaction (MDM2 Inhibitors) in clinical trials for cancer treatment.

Authors:
Yujun Zhao Angelo Aguilar Denzil Bernard Shaomeng Wang

J Med Chem 2015 Feb 14;58(3):1038-52. Epub 2014 Nov 14.

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

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February 2015

SAR405838: an optimized inhibitor of MDM2-p53 interaction that induces complete and durable tumor regression.

Authors:
Shaomeng Wang Wei Sun Yujun Zhao Donna McEachern Isabelle Meaux Cédric Barrière Jeanne A Stuckey Jennifer L Meagher Longchuan Bai Liu Liu Cassandra Gianna Hoffman-Luca Jianfeng Lu Sanjeev Shangary Shanghai Yu Denzil Bernard Angelo Aguilar Odette Dos-Santos Laurent Besret Stéphane Guerif Pascal Pannier Dimitri Gorge-Bernat Laurent Debussche

Cancer Res 2014 Oct 21;74(20):5855-65. Epub 2014 Aug 21.

Sanofi Oncology, Vitry-sur-Seine, France.

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October 2014

BM-1197: a novel and specific Bcl-2/Bcl-xL inhibitor inducing complete and long-lasting tumor regression in vivo.

Authors:
Longchuan Bai Jianfang Chen Donna McEachern Liu Liu Haibin Zhou Angelo Aguilar Shaomeng Wang

PLoS One 2014 5;9(6):e99404. Epub 2014 Jun 5.

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

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October 2015

A potent and highly efficacious Bcl-2/Bcl-xL inhibitor.

Authors:
Angelo Aguilar Haibin Zhou Jianfang Chen Liu Liu Longchuan Bai Donna McEachern Chao-Yie Yang Jennifer Meagher Jeanne Stuckey Shaomeng Wang

J Med Chem 2013 Apr 22;56(7):3048-3067. Epub 2013 Mar 22.

Comprehensive Cancer Center and Departments of Internal Medicine, Pharmacology and Medicinal Chemistry, University of Michigan, 1500 E. Medical Center Drive, Ann Arbor, MI 48109-0934, USA.

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April 2013

Structure-based discovery of BM-957 as a potent small-molecule inhibitor of Bcl-2 and Bcl-xL capable of achieving complete tumor regression.

Authors:
Jianfang Chen Haibin Zhou Angelo Aguilar Liu Liu Longchuan Bai Donna McEachern Chao-Yie Yang Jennifer L Meagher Jeanne A Stuckey Shaomeng Wang

J Med Chem 2012 Oct 2;55(19):8502-14. Epub 2012 Oct 2.

Comprehensive Cancer Center, University of Michigan, 1500 East Medical Center Drive, Ann Arbor, MI 48109-0934, USA.

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October 2012

Structure-based design of potent Bcl-2/Bcl-xL inhibitors with strong in vivo antitumor activity.

Authors:
Haibin Zhou Angelo Aguilar Jianfang Chen Longchuan Bai Liu Liu Jennifer L Meagher Chao-Yie Yang Donna McEachern Xin Cong Jeanne A Stuckey Shaomeng Wang

J Med Chem 2012 Jul 2;55(13):6149-61. Epub 2012 Jul 2.

Comprehensive Cancer Center and Departments of Internal Medicine, Pharmacology and Medicinal Chemistry, University of Michigan, Ann Arbor, MI 48109-0934, USA.

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July 2012

Correction to Design of Bcl-2 and Bcl-xL Inhibitors with Subnanomolar Binding Affinities Based upon a New Scaffold.

Authors:
Haibin Zhou Jianfang Chen Jennifer L Meagher Chao-Yie Yang Angelo Aguilar Liu Liu Longchuan Bai Xin Cong Qian Cai Xueliang Fang Jeanne A Stuckey Shaomeng Wang

J Med Chem 2012 Jun 7;55(12):5987. Epub 2012 Jun 7.

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June 2012

Design of Bcl-2 and Bcl-xL inhibitors with subnanomolar binding affinities based upon a new scaffold.

Authors:
Haibin Zhou Jianfang Chen Jennifer L Meagher Chao-Yie Yang Angelo Aguilar Liu Liu Longchuan Bai Xin Cong Qian Cai Xueliang Fang Jeanne A Stuckey Shaomeng Wang

J Med Chem 2012 May 10;55(10):4664-82. Epub 2012 May 10.

Comprehensive Cancer Center and Department of Internal Medicine, University of Michigan , 1500 East Medical Center Drive, Ann Arbor, Michigan 48109-0934, United States.

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May 2012