Publications by authors named "Denzil Bernard"

33Publications

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

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.

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

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

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.

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

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.

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

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

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.

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.

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.

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.

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.

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

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

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.

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.

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