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Decarboxy-histidine, which can be placed at the C-terminus of a peptide replacing natural histidine. This building block has been found in potent agonists of histamine H2 receptors (H2R), histamine H4 receptors (H4R) and inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Interaction pattern of histidine, carnosine and histamine with methylglyoxal and other carbonyl compounds; R. G. Zadeh, V. Yaylayan; Food Chem 2021; 358: 129884. https://doi.org/10.1016/j.foodchem.2021.129884.
[(3)H]UR-DEBa176: A 2,4-Diaminopyrimidine-Type Radioligand Enabling Binding Studies at the Human, Mouse, and Rat Histamine H4 Receptors; E. Bartole, T. Littmann, M. Tanaka, T. Ozawa, A. Buschauer and G. Bernhardt; Journal of medicinal chemistry 2019; 62: 8338-8356. https://doi.org/10.1021/acs.jmedchem.9b01342
Crystal structure of the GLP-1 receptor bound to a peptide agonist; A. Jazayeri, M. Rappas, A. J. H. Brown, J. Kean, J. C. Errey, N. J. Robertson, C. Fiez-Vandal, S. P. Andrews, M. Congreve, A. Bortolato, J. S. Mason, A. H. Baig, I. Teobald, A. S. Dore, M. Weir, R. M. Cooke and F. H. Marshall; Nature 2017; 546: 254-258. https://doi.org/10.1038/nature22800
Acylguanidines as bioisosteres of guanidines: NG-acylated imidazolylpropylguanidines, a new class of histamine H2 receptor agonists; P. Ghorai, A. Kraus, M. Keller, C. Gotte, P. Igel, E. Schneider, D. Schnell, G. Bernhardt, S. Dove, M. Zabel, S. Elz, R. Seifert and A. Buschauer; Journal of medicinal chemistry 2008; 51: 7193-204. https://doi.org/10.1021/jm800841w
Potent inhibitors of farnesyltransferase and geranylgeranyltransferase-I; D. N. Nguyen, C. A. Stump, E. S. Walsh, C. Fernandes, J. P. Davide, M. Ellis-Hutchings, R. G. Robinson, T. M. Williams, R. B. Lobell, H. E. Huber and C. A. Buser; Bioorg Med Chem Lett 2002; 12: 1269-73. https://doi.org/10.1016/s0960-894x(02)00154-3
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Interested in histidine derivatives? Iris Biotech provides a selection of deamino- and decarboxy-products. Find out more about benefits and potenti
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