Target Validation Information
TTD ID	T05387
Target Name	Tissue transglutaminase (TG2)
Type of Target	Clinical trial
Drug Potency against Target	Putrescine	Drug Info	Affinity = 50000 nM	[1]
Action against Disease Model	Putrescine	Drug Info	Kinetic evaluation of both of these subclasses revealed that they display reversible inhibition and are competitive with acyl donor TGase substrates at IC50 values as low as 18 |?M. An analysis of structure?activity relationships within these series of inhibitors permitted the identification of potentially important binding interactions. Further testing of some of the most potent inhibitors demonstrated their selectivity for TG2 and their potential for further development.	[2]
References
REF 1	Topical putrescine (Fibrostat) in treatment of hypertrophic scars: phase II study. Plast Reconstr Surg. 1996 Jan;97(1):117-23; discussion 124-5.
REF 2	Cinnamoyl inhibitors of tissue transglutaminase. J Org Chem. 2008 Aug 1;73(15):5766-75.

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