Boc-Phe-Ser-Arg-AMC is a fluorescent substrate that, upon cleavage by proteases, releases highly fluorescent AMC (Ex/Em: 355 nm/460 nm). Boc-Phe-Ser-Arg-AMC is characterized by its preferential hydrolysis by coagulation factor XIa and is widely used for detecting the activities of enzymes such as trypsin, tryptase, and kallikrein[1,2,3]. Boc-Phe-Ser-Arg-AMC is also highly sensitive to proteases in yeast mitochondrial matrix and trypsin in rat mast cells. After the Arg-AMC peptide bond is cleaved by proteases, AMC is released, and the increase in fluorescence intensity is proportional to the enzyme activity[4,5,6].
References:
[1] KALE S S, BERGERON-BRLEK M, WU Y, et al. Thiol-to-amine cyclization reaction enables screening of large libraries of macrocyclic compounds and the generation of sub-kilodalton ligands[J]. Science Advances, 2019, 5(8): eaaw2851.
[2] GONG Z, DAI S, JIANG X, et al. Variants in KLK11, affecting signal peptide cleavage of kallikrein-related peptidase 11, cause an autosomal-dominant cornification disorder[J]. British Journal of Dermatology, 2023, 188(1): 100-111.
[3] KOMATSU N, SAIJOH K, KUK C, et al. Aberrant human tissue kallikrein levels in the stratum corneum and serum of patients with psoriasis: dependence on phenotype, severity and therapy[J]. British Journal of Dermatology, 2007, 156(5): 875-883.
[4] BRAGANZA V J, SIMMONS W H. Tryptase from rat skin: purification and properties[J]. Biochemistry, 1991, 30(20): 4997-5007.
[5] YASUHARA T, OHASHI A. New chelator-sensitive proteases in matrix of yeast mitochondria[J]. Biochemical and Biophysical Research Communications, 1987, 144(1): 277-283.
[6] ROEDL D, TRAIDL-HOFFMANN C, RING J, et al. Serine protease inhibitor lymphoepithelial Kazal type-related inhibitor tends to be decreased in atopic dermatitis. 2009.
Boc-Phe-Ser-Arg-AMC是一种在被蛋白酶切割后可释放高荧光强度AMC（Ex/Em: 355nm/460nm）的荧光底物，具有被凝血因子XIa优先水解的特点，并被广泛应用于胰蛋白酶、类胰蛋白酶及激肽释放酶等酶活性的检测[1,2,3]。Boc-Phe-Ser-Arg-AMC对酵母线粒体基质中的蛋白酶以及大鼠肥大细胞中的胰蛋白酶也高度敏感，被蛋白酶切割Arg-AMC肽键后释放AMC，其荧光强度的增加与酶活性成正比[4,5,6]。