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Structures of Human Transglutaminase 2: Finding Clues for Interference in Cross-linking Mediated Activity

College of Pharmacy, Chung-Ang University, Seoul 06974, Korea
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Int. J. Mol. Sci. 2020, 21(6), 2225; https://doi.org/10.3390/ijms21062225
Received: 17 February 2020 / Revised: 19 March 2020 / Accepted: 20 March 2020 / Published: 23 March 2020
Human transglutaminase 2 (TGase2) has various functions, including roles in various cellular processes such as apoptosis, development, differentiation, wound healing, and angiogenesis, and is linked to many diseases such as cancer. Although TGase2 has been considered an optimized drug target for the treatment of cancer, fibrosis, and neurodegenerative disorders, it has been difficult to generate TGase2-targeted drugs for clinical use because of the relatively flat and broad active site on TGase2. To design more specific and powerful inhibitors, detailed structural information about TGase2 complexed with various effector and inhibitor molecules is required. In this review, we summarized the current structural studies on TGase2, which will aid in designing drugs that can overcome the aforementioned limitations. View Full-Text
Keywords: transglutaminase 2; structure-based drug design; protein structure; peptide mimetic transglutaminase 2; structure-based drug design; protein structure; peptide mimetic
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Kim, G.E.; Park, H.H. Structures of Human Transglutaminase 2: Finding Clues for Interference in Cross-linking Mediated Activity. Int. J. Mol. Sci. 2020, 21, 2225.

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