The war on hTG2: warhead optimization in small molecule human tissue transglutaminase inhibitors

Lavleen Mader, Sarah K. I. Watt, Harish R. Iyer, Linh Nguyen, Harpreet Kaur and Jeffrey W. Keillor

RSC Med. Chem., 2023, 14, 277
DOI: 10.1039/D2MD00378C

Novel irreversible peptidic inhibitors of transglutaminase 2

Nicholas J. Cundy, Jane Arciszewski, Eric W. J. Gates, Sydney L. Acton, Kyle D. Passley, Ernest Awoonor-Williams, Elizabeth K. Boyd, Nancy Xu, Élise Pierson, Catalina Fernandez-Ansieta, Marie R. Albert, Nicole M. R. McNeil, Gautam Adhikary, Richard L. Eckert and Jeffrey W. Keillor

RSC Med. Chem., 2023, 14, 378
DOI: 10.1039/D2MD00417H

High-Affinity Fluorogenic Substrate for Tissue Transglutaminase Reveals Enzymatic Hysteresis

Eric W. J. Gates, Adrien Prince-Hallée, Yasaman Heidari, Abootaleb Sedighi and Jeffrey W. Keillor

Biochemistry, 2023, 62, 3085
DOI: 10.1021/acs.biochem.3c00337

Preclinical evaluation of an 18F-labeled Nε-acryloyllysine piperazide for covalent targeting of transglutaminase 2

Robert Wodtke, Markus Laube, Sandra Hauser, Sebastian Meister, Friedrich-Alexander Ludwig, Steffen Fischer, Klaus Kopka, Jens Pietzsch and Reik Löser

EJNMMI radiopharm. chem., 2024, 9
DOI: 10.1186/s41181-023-00231-1

Cell-Impermeable Inhibitors Confirm That Intracellular Human Transglutaminase 2 Is Responsible for the Transglutaminase-Associated Cancer Phenotype

Eric W. J. Gates, Nicholas D. Calvert, Nicholas J. Cundy, Federica Brugnoli, Pauline Navals, Alexia Kirby, Nicoletta Bianchi, Gautam Adhikary, Adam J. Shuhendler, Richard L. Eckert and Jeffrey W. Keillor

IJMS, 2023, 24, 12546
DOI: 10.3390/ijms241612546

Conformational Modulation of Tissue Transglutaminase via Active Site Thiol Alkylating Agents: Size Does Not Matter

Pauline Navals, Alana M. M. Rangaswamy, Petr Kasyanchyk, Maxim V. Berezovski and Jeffrey W. Keillor

Biomolecules, 2024, 14, 496
DOI: 10.3390/biom14040496

Diamino variants of piperazine-based tissue transglutaminase inhibitors

Brianna Ryan, Alana M.M. Rangaswamy, Sammir Shad and Jeffrey W. Keillor

Bioorganic & Medicinal Chemistry Letters, 2025, 119, 130078
DOI: 10.1016/j.bmcl.2024.130078

Peptidic Inhibitors and a Fluorescent Probe for the Selective Inhibition and Labelling of Factor XIIIa Transglutaminase

Eric W. J. Gates, Kian Mansour, Sahar Ebrahimi Samani, Sammir Shad, Mari T. Kaartinen and Jeffrey W. Keillor

Molecules, 2023, 28, 1634
DOI: 10.3390/molecules28041634

A peptide-based fluorescent bioprobe for EphA2-overexpressing tumor targeting and image-guided surgical resection

Xudong Yu, Jianfei Jin, Yun Si, Huanmin Zhang and Zhegang Song

Bioorganic & Medicinal Chemistry, 2025, 120, 118090
DOI: 10.1016/j.bmc.2025.118090

Metabolic characterisation of transglutaminase 2 inhibitor effects in breast cancer cell lines

Mariana Gallo, Elena Ferrari, Anna Terrazzan, Federica Brugnoli, Alberto Spisni, Cristian Taccioli, Gianluca Aguiari, Alessandro Trentini, Stefano Volinia, Jeffrey W. Keillor, Carlo M. Bergamini, Nicoletta Bianchi and Thelma A. Pertinhez

The FEBS Journal, 2023, 290, 5411
DOI: 10.1111/febs.16931

Structural analysis and evaluation of natural compounds for thrombotic disorder management: ADMET profiling, docking, dynamics, and post-dynamic assessment

Nikhil Kumar, Bhavya Sharma, Chandraprakash Gond, Shivani Daksh, Pooja Srivastava, Himanshu Ojha and Anupama Datta

Chem. Pap., 2025, 79, 1823
DOI: 10.1007/s11696-025-03890-3