Publications by authors named "Denzil Bernard"

33Publications

Follicular lymphoma-associated BTK mutations are inactivating resulting in augmented AKT activation.

Authors:
Nan Hu Fangyang Wang Tianyu Sun Zhengfan Xu Jing Zhang Denzil Bernard Shilin Xu Shaomeng Wang Mark S Kaminski Sumana Devata Tycel Phillips Sami Malek

Clin Cancer Res 2021 Jan 8. Epub 2021 Jan 8.

Med-Hematology/ Oncology, University of Michigan–Ann Arbor

View Article and Find Full Text PDF
January 2021

Small molecules block the interaction between porcine reproductive and respiratory syndrome virus and CD163 receptor and the infection of pig cells.

Authors:
Chang Huang Denzil Bernard Jiaqi Zhu Radha Charan Dash Alexander Chu Alec Knupp Anna Hakey M Kyle Hadden Antonio Garmendia Young Tang

Virol J 2020 07 30;17(1):116. Epub 2020 Jul 30.

Department of Animal Science, Institute for Systems Genomics, University of Connecticut, 1390 Storrs Rd, Storrs, CT, 06269, USA.

View Article and Find Full Text PDF
July 2020

Discovery of Potent Small-Molecule Inhibitors of MLL Methyltransferase.

Authors:
Ting-Rong Chern Liu Liu Elyse Petrunak Jeanne A Stuckey Mi Wang Denzil Bernard Haibin Zhou Shirley Lee Yali Dou Shaomeng Wang

ACS Med Chem Lett 2020 Jun 14;11(6):1348-1352. Epub 2020 May 14.

Department of Medicinal Chemistry, Department of Internal Medicine, Department of Pharmacology, Department of Pathology, and Life Sciences Institute, University of Michigan, Ann Arbor, Michigan 48109, United States.

View Article and Find Full Text PDF
June 2020

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

Follicular lymphoma-associated mutations in vacuolar ATPase ATP6V1B2 activate autophagic flux and mTOR.

Authors:
Fangyang Wang Damián Gatica Zhang Xiao Ying Luke F Peterson Peter Kim Denzil Bernard Kamlai Saiya-Cork Shaomeng Wang Mark S Kaminski Alfred E Chang Tycel Phillips Daniel J Klionsky Sami N Malek

J Clin Invest 2019 03 4;129(4):1626-1640. Epub 2019 Mar 4.

Department of Internal Medicine, Division of Hematology and Oncology.

View Article and Find Full Text PDF
March 2019

High-Affinity Peptidomimetic Inhibitors of the DCN1-UBC12 Protein-Protein Interaction.

Authors:
Haibin Zhou Weihua Zhou Bing Zhou Liu Liu Ting-Rong Chern Krishnapriya Chinnaswamy Jianfeng Lu Denzil Bernard Chao-Yie Yang Shasha Li Mi Wang Jeanne Stuckey Yi Sun Shaomeng Wang

J Med Chem 2018 03 26;61(5):1934-1950. Epub 2018 Feb 26.

Institute of Translational Medicine , Zhejiang University School of Medicine , Hangzhou , Zhejiang 310029 , China.

View Article and Find Full Text PDF
March 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

A potent small-molecule inhibitor of the DCN1-UBC12 interaction that selectively blocks cullin 3 neddylation.

Authors:
Haibin Zhou Jianfeng Lu Liu Liu Denzil Bernard Chao-Yie Yang Ester Fernandez-Salas Krishnapriya Chinnaswamy Stephanie Layton Jeanne Stuckey Qing Yu Weihua Zhou Zhenqiang Pan Yi Sun Shaomeng Wang

Nat Commun 2017 10 27;8(1):1150. Epub 2017 Oct 27.

Department of Internal Medicine, University of Michigan, Ann Arbor, Michigan, 48109, USA.

View Article and Find Full Text PDF
October 2017

Discovery of a Highly Potent, Cell-Permeable Macrocyclic Peptidomimetic (MM-589) Targeting the WD Repeat Domain 5 Protein (WDR5)-Mixed Lineage Leukemia (MLL) Protein-Protein Interaction.

Authors:
Hacer Karatas Yangbing Li Liu Liu Jiao Ji Shirley Lee Yong Chen Jiuling Yang Liyue Huang Denzil Bernard Jing Xu Elizabeth C Townsend Fang Cao Xu Ran Xiaoqin Li Bo Wen Duxin Sun Jeanne A Stuckey Ming Lei Yali Dou Shaomeng Wang

J Med Chem 2017 06 12;60(12):4818-4839. Epub 2017 Jun 12.

Department of Medicinal Chemistry, ‡Department of Internal Medicine, §Comprehensive Cancer Center, ∥Department of Pathology, ⊥Howard Hughes Medical Institute, #Department of Biological Chemistry, ∇Department of Pharmaceutical Sciences, ○Department of Pharmacology, and ¶Life Sciences Institute, University of Michigan , Ann Arbor, Michigan 48109, United States.

View Article and Find Full Text PDF
June 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

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.

View Article and Find Full Text PDF
May 2017

Recurrent Mutations in the MTOR Regulator RRAGC in Follicular Lymphoma.

Authors:
Zhang Xiao Ying Meiyan Jin Luke F Peterson Denzil Bernard Kamlai Saiya-Cork Mehmet Yildiz Shaomeng Wang Mark S Kaminski Alfred E Chang Daniel J Klionsky Sami N Malek

Clin Cancer Res 2016 Nov 7;22(21):5383-5393. Epub 2016 Jun 7.

Division of Hematology and Oncology, Department of Internal Medicine, University of Michigan, Ann Arbor, Michigan.

View Article and Find Full Text PDF
November 2016

Case Study: discovery of inhibitors of the MDM2-p53 protein-protein interaction.

Authors:
Liu Liu Denzil Bernard Shaomeng Wang

Methods Mol Biol 2015 ;1278:567-85

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

View Article and Find Full Text PDF
December 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

Activating STAT6 mutations in follicular lymphoma.

Authors:
Mehmet Yildiz Hongxiu Li Denzil Bernard Nisar A Amin Peter Ouillette Siân Jones Kamlai Saiya-Cork Brian Parkin Kathryn Jacobi Kerby Shedden Shaomeng Wang Alfred E Chang Mark S Kaminski Sami N Malek

Blood 2015 Jan 26;125(4):668-79. Epub 2014 Nov 26.

Department of Internal Medicine, Division of Hematology and Oncology, University of Michigan, Ann Arbor, MI;

View Article and Find Full Text PDF
January 2015

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.

View Article and Find Full Text PDF
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.

View Article and Find Full Text PDF
October 2014

A potent small-molecule inhibitor of the MDM2-p53 interaction (MI-888) achieved complete and durable tumor regression in mice.

Authors:
Yujun Zhao Shanghai Yu Wei Sun Liu Liu Jianfeng Lu Donna McEachern Sanjeev Shargary Denzil Bernard Xiaoqin Li Ting Zhao Peng Zou Duxin Sun Shaomeng Wang

J Med Chem 2013 Jul 20;56(13):5553-61. Epub 2013 Jun 20.

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
July 2013

Diastereomeric spirooxindoles as highly potent and efficacious MDM2 inhibitors.

Authors:
Yujun Zhao Liu Liu Wei Sun Jianfeng Lu Donna McEachern Xiaoqin Li Shanghai Yu Denzil Bernard Philippe Ochsenbein Vincent Ferey Jean-Christophe Carry Jeffrey R Deschamps Duxin Sun Shaomeng Wang

J Am Chem Soc 2013 May 3;135(19):7223-34. Epub 2013 May 3.

Comprehensive Cancer Center and Department of Internal Medicine, University of Michigan, 1500 East Medical Center Drive, Ann Arbor, Michigan 48109, USA.

View Article and Find Full Text PDF
May 2013

Structure-based design of high-affinity macrocyclic peptidomimetics to block the menin-mixed lineage leukemia 1 (MLL1) protein-protein interaction.

Authors:
Haibin Zhou Liu Liu Jing Huang Denzil Bernard Hacer Karatas Alexandro Navarro Ming Lei Shaomeng Wang

J Med Chem 2013 Feb 17;56(3):1113-23. Epub 2013 Jan 17.

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

View Article and Find Full Text PDF
February 2013