Antipain (hydrochloride) is a reversible protease inhibitor [1]. Antipain forms a hemiacetal adduct with the active serine in the active site of protease through its terminal aldehyde group, thereby inhibiting the activity of various proteases including serine proteases and cysteine proteases [2-3]. Antipain is commonly used in the study of tumors [4].
In hamster embryo cells, Antipain (6μg/mL; 24h) affects the fixation and expression of X-ray-induced neoplastic transformation by regulating DNA repair processes [5]. In BALB/c 3T3 cells, Antipain (10μM; 48h) treatment reduces the cell transformation rate induced by 3-MCA and 1,2-DBE [6].
References:
[1]. Suda H, AOYAGI T, HAMADA M, et al. Antipain, a new protease inhibitor isolated from agtinomycetes[J]. The Journal of antibiotics, 1972, 25(4): 263-265.
[2]. Otto H H, Schirmeister T. Cysteine proteases and their inhibitors[J]. Chemical reviews, 1997, 97(1): 133-172.
[3]. Nguyen Q V, Knapp W, Humphreys R E. Inhibition by leupeptin and antipain of the intracellular proteolysis of Ii[J]. Human immunology, 1989, 24(3): 153-163.
[4]. Nomura T, Enomoto T, Shibata K, et al. Antiteratogenic effects of tumor inhibitors, caffeine, antipain, and retinoic acid in mice[J]. Cancer research, 1983, 43(11): 5156-5162.
[5]. Borek C, Miller R, Pain C, et al. Conditions for inhibiting and enhancing effects of the protease inhibitor antipain on x-ray-induced neoplastic transformation in hamster and mouse cells[J]. Proceedings of the National Academy of Sciences, 1979, 76(4): 1800-1803.
[6]. Vaccari M, Argnani A, Horn W, et al. Effects of the protease inhibitor antipain on cell malignant transformation[J]. Anticancer research, 1999, 19(1A): 589-596.
Antipain (hydrochloride)是一种可逆性蛋白酶抑制剂 [1]。Antipain通过其末端醛基与蛋白酶活性位点的活性丝氨酸形成半缩醛加合物，从而抑制包括丝氨酸蛋白酶和半胱氨酸蛋白酶在内的多种蛋白酶的活性 [2-3]。Antipain常用于肿瘤研究 [4]。
在仓鼠胚胎细胞中，Antipain（6μg/mL；24h）通过调节DNA修复过程影响X射线诱导的肿瘤转化的固定和表达 [5]。在BALB/c 3T3细胞中，Antipain（10μM；48h）处理可降低3-MCA和1,2-DBE诱导的细胞转化率 [6]。