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Debler Research

Contact

Name: Erik Debler, PhD
Position: Associate Professor, Department of Biochemistry & Molecular Biology
Organization: Sidney Kimmel Medical College

1020 Locust Street
JAH 411F
Philadelphia, PA 19107

Contact Number(s):

Highlighted Publications

Farkas M, Hashimoto H, Resnick-Silverman L, Bi Y, Davuluri RV, Manfredi JJ, Debler EW, McMahon SB. Distinct mechanisms control genome recognition by p53 at its target genes linked to different cell fates. Nat Commun. 12:484, 2021.

We deciphered the mechanism that governs selective engagement of the tumor suppressor p53 – a master regulatory transcription factor that integrates stress response pathways by triggering different cell fates – with distinct response elements, thereby answering the fundamental and long-standing question of how p53 can turn on distinct gene expression programs

Frisbie VS, Hashimoto H, Xie Y, De Luna Vitorino FN, Baeza J, Nguyen T, Yuan Z, Garcia BA, Debler EW. Two DOT1 enzymes cooperatively mediate efficient ubiquitin-independent histone H3 lysine 76 tri-methylation in kinetoplastids. Nat Commun 15:2467, 2024.

We discovered that the nucleosomal histone lysine methyltransferases DOT1A and DOT1B of the early-branched eukaryote Trypanosoma brucei exhibit distinct methylation kinetics and substrate preferences, enabling them to mediate efficient H3K76 tri-methylation cooperatively and suggesting why T. brucei and related eukaryotes have evolved two DOT1 enzymes.

Farkas M, Hashimoto H, Resnick-Silverman L, Bi Y, Davuluri RV, Manfredi JJ, Debler EW, McMahon SB. Distinct mechanisms control genome recognition by p53 at its target genes linked to different cell fates. Nat Commun. 12:484, 2021.

We deciphered the mechanism that governs selective engagement of the tumor suppressor p53 – a master regulatory transcription factor that integrates stress response pathways by triggering different cell fates – with distinct response elements, thereby answering the fundamental and long-standing question of how p53 can turn on distinct gene expression programs

Jain K, Warmack RA, Debler EW, Hadjikyriacou A, Stavropoulos P, and Clarke SG. Protein Arginine Methyltransferase Product Specificity is Mediated by Distinct Active-Site Architectures. J. Biol. Chem., 291:18299, 2016

We converted a protein arginine methyltransferase, which only produces monomethylarginine, into enzymes capable of asymmetric and symmetric dimethylarginine formation, providing a structural basis and a general model for product specificity in PRMTs.

Debler EW, Jain K, Warmack RA, Feng Y, Clarke SG, Blobel G, and Stavropoulos P. A glutamate/aspartate switch controls product specificity in a protein arginine methyltransferase. Proc. Natl. Acad. Sci. USA, 113:2068, 2016

Structural and biochemical analyses of a protein arginine monomethyltransferase provide insights into the mechanism of action and the exquisite product specificity of this important class of enzymes, linked to a variety of diseases.

Schulz D, Mugnier M, Paulsen EM, Kim HS, Chung CW, Tough DF, Rioja D, Prinjha RK, Papavasiliou FN, and Debler EW. Bromodomain proteins contribute to maintenance of bloodstream form stage identity in the African trypanosome. PLOS Biol., 13: e1002316, 2015

We reveal an unexpected role of trypanosome bromodomains in maintenance of life-cycle stage identity and establish the druggability of this pathway with a small-molecule inhibitor, delineating a novel effective treatment for African sleeping sickness.

Recent Publications

Two DOT1 enzymes cooperatively mediate efficient ubiquitin-independent histone H3 lysine 76 tri-methylation in kinetoplastids

The C-terminal 4CXXC-type zinc finger domain of CDCA7 recognizes hemimethylated DNA and modulates activities of chromatin remodeling enzyme HELLS

Structure of the pre-mRNA leakage 39-kDa protein reveals a single domain of integrated zf-C3HC and Rsm1 modules

Structural enzymology of cholesterol biosynthesis and storage

Coil-to-α-helix transition at the Nup358-BicD2 interface activates BicD2 for dynein recruitment

Distinct mechanisms control genome recognition by p53 at its target genes linked to different cell fates

Structural Basis of Protein Arginine Methyltransferase Activation by a Catalytically Dead Homolog (Prozyme)

Substrate Affinity and Specificity of the ScSth1p Bromodomain Are Fine-Tuned for Versatile Histone Recognition

Role of Coiled-Coil Registry Shifts in the Activation of Human Bicaudal D2 for Dynein Recruitment upon Cargo Binding

A Quantitative Model for BicD2/Cargo Interactions

Trypanosoma brucei PRMT1 is a nucleic acid binding protein with a role in energy metabolism and the starvation stress response

The major protein arginine methyltransferase in Trypanosoma brucei functions as an enzyme-prozyme complex

Protein arginine methyltransferase product specificity is mediated by distinct active-site architectures

A glutamate/aspartate switch controls product specificity in a protein arginine methyltransferase

Bromodomain Proteins Contribute to Maintenance of Bloodstream Form Stage Identity in the African Trypanosome

Structural and functional analysis of an essential nucleoporin heterotrimer on the cytoplasmic face of the nuclear pore complex

The Structure of the nuclear pore complex

Characterization of the membrane-coating nup84 complex: Paradigm for the nuclear pore complex structure

An aspartate and a water molecule mediate efficient acid-base catalysis in a tailored antibody pocket

Structure of a trimeric nucleoporin complex reveals alternate oligomerization states

Structural and functional analysis of Nup120 suggests ring formation of the Nup84 complex

Nuclear transport comes full circle

Structural and functional analysis of the interaction between the nucleoporin Nup214 and the DEAD-box helicase Ddx19

A Fence-like Coat for the Nuclear Pore Membrane

Conformational isomerism can limit antibody catalysis