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Structural basis of HMCES interactions with abasic DNA and multivalent substrate recognition

Crystal structures of the human HMCES SRAP ___domain in complex with DNA substrates demonstrate how the SRAP ___domain interacts with a variety of single-strand- and double-strand-containing DNA structures found at DNA-damage sites.

Levon Halabelian
Mani Ravichandran
Cheryl H Arrowsmith
Research24 Jun 2019
Nature Structural & Molecular Biology

Volume: 26, P: 607-612
Crystal structures of DCAF1-PROTAC-WDR5 ternary complexes provide insight into DCAF1 substrate specificity

The authors show that DCAF1, a substrate receptor of CUL4 and EDVP E3 ligases, can be recruited by PROTACs to degrade the cancer drug target, WDR5. They also report the crystal structures of PROTAC ternary complexes that reveal a significant role for loops in DCAF1 substrate recognition, a potential mechanism behind the diverse substrate specificity of DCAF1.

Mark F. Mabanglo
Brian Wilson
Masoud Vedadi
ResearchOpen Access23 Nov 2024
Nature Communications

Volume: 15, P: 1-17
Potent and selective SETDB1 covalent negative allosteric modulator reduces methyltransferase activity in cells

Design of cysteine-targeting analogs of a reversible SETDB1 triple Tudor ___domain (3TD) ligand, UNC6535, led to UNC10013, a potent covalent ligand with high selectivity. UNC10013 demonstrated allosteric inhibition of SETDB1-mediated Akt methylation in cells, a promising approach to SETDB1 therapeutics.

Mélanie Uguen
Devan J. Shell
Stephen V. Frye
ResearchOpen Access24 Feb 2025
Nature Communications

Volume: 16, P: 1-16
Structure and activity of human TMPRSS2 protease implicated in SARS-CoV-2 activation

The first crystal structure of human TMPRSS2, a proteolytic driver of SARS-CoV-2 infection in airways and an antiviral target, reveals structural features of viral spike protein and protease inhibitor binding.

Bryan J. Fraser
Serap Beldar
François Bénard
Research08 Jun 2022
Nature Chemical Biology

Volume: 18, P: 963-971
A covalent homodimer probing early oligomers along amyloid aggregation

Levon Halabelian
Annalisa Relini
Stefano Ricagno
ResearchOpen Access30 Sept 2015
Scientific Reports

Volume: 5, P: 1-12
Author Correction: Pharmacological inhibition of PRMT7 links arginine monomethylation to the cellular stress response

Magdalena M. Szewczyk
Yoshinori Ishikawa
Dalia Barsyte-Lovejoy
Amendments and CorrectionsOpen Access26 May 2020
Nature Communications

Volume: 11, P: 1
Big data and benchmarking initiatives to bridge the gap from AlphaFold to drug design

AlphaFold is a breakthrough in protein structure prediction, but limitations in its application to computation- and structure-guided drug discovery remain. As with structure prediction, public-___domain data and benchmarking initiatives will be essential to advance the field of computational drug design.

Matthieu Schapira
Levon Halabelian
Rachel J. Harding
Comments & Opinion08 Mar 2024
Nature Chemical Biology

Volume: 20, P: 937-940
Loss-of-function mutation in PRMT9 causes abnormal synapse development by dysregulation of RNA alternative splicing

Mutations in protein arginine methyltransferase 9 (PRMT9) are linked to intellectual disability. Here, the authors show that mutant PRMT9 fails to methylate its primary substrate SF3B2, causing aberrant RNA splicing and abnormal synapse development.

Lei Shen
Xiaokuang Ma
Yanzhong Yang
ResearchOpen Access01 Apr 2024
Nature Communications

Volume: 15, P: 1-20
Affinity-matured HLA class II dimers for robust staining of antigen-specific CD4⁺ T cells

CD4⁺ T cells are readily detected with class II MHC dimers.

Kenji Sugata
Yukiko Matsunaga
Naoto Hirano
Research01 Mar 2021
Nature Biotechnology

Volume: 39, P: 958-967
Discovery of a chemical probe for PRDM9

PRDM9 is a PR ___domain containing histone methyl transferase which expression is normally restricted to the germline that has also been linked to a number of somatic cancers. Here the authors describe the identification of a small molecule that selectivity inhibits the methyltransferase activity of PRDM9 in biochemical and cellular assays

Abdellah Allali-Hassani
Magdalena M. Szewczyk
Masoud Vedadi
ResearchOpen Access17 Dec 2019
Nature Communications

Volume: 10, P: 1-11
Pharmacological inhibition of PRMT7 links arginine monomethylation to the cellular stress response

Protein arginine methyltransferases (PRMTs) are increasingly recognized as potential therapeutic targets but PRMT7 remains an understudied member of this enzyme family. Here, the authors develop a chemical probe for PRMT7 and apply it to elucidate the role of PRMT7 in the cellular stress response.

Magdalena M. Szewczyk
Yoshinori Ishikawa
Dalia Barsyte-Lovejoy
ResearchOpen Access14 May 2020
Nature Communications

Volume: 11, P: 1-15
The dual methyltransferase METTL13 targets N terminus and Lys55 of eEF1A and modulates codon-specific translation rates

Eukaryotic elongation factor 1 alpha (eEF1A) is subject to extensive post-translational methylation but not all responsible enzymes are known. Here, the authors identify METTL13 as an eEF1A methyltransferase with dual specificity, which is involved in the codon-specific modulation of mRNA translation.

Magnus E. Jakobsson
Jędrzej M. Małecki
Pål Ø. Falnes
ResearchOpen Access24 Aug 2018
Nature Communications

Volume: 9, P: 1-15
A ligand discovery toolbox for the WWE ___domain family of human E3 ligases

Six WWE ___domain-containing proteins also contain domains with E3 ubiquitin ligase activity. We report structures, biophysical and biochemical assays for the discovery of novel WWE ___domain binders and their respective application.

Lena Münzker
Serah W. Kimani
Jark Böttcher
ResearchOpen Access24 Jul 2024
Communications Biology

Volume: 7, P: 1-15
The co-crystal structure of Cbl-b and a small-molecule inhibitor reveals the mechanism of Cbl-b inhibition

Structural and biophysical characterization of a small molecule binding to Cbl-b E3 ligase reveals an intramolecular glue mechanism locking the protein in an inactive state.

Serah W. Kimani
Sumera Perveen
Levon Halabelian
ResearchOpen Access16 Dec 2023
Communications Biology

Volume: 6, P: 1-10
Histone lysine methacrylation is a dynamic post-translational modification regulated by HAT1 and SIRT2

Kyle Delaney
Minjia Tan
Yingming Zhao
ResearchOpen Access28 Dec 2021
Cell Discovery

Volume: 7, P: 1-14

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