p-Aminophenylmercuric acetate, an organomercurial MMP activator capable of attacking protein sulfhydryl groups or inducing cysteine switch reactions involved in both the activation and inhibition of MMP-8 [1]. p-Aminophenylmercuric acetate can convert the latent form of MMP-9 (94kDa) purified from the human cell line HL-60 into an intermediary active form (84kDa)[2]. p-Aminophenylmercuric acetate can be used as a building block to synthesize novel types of photochromic dyes[3].
In vitro, p-Aminophenylmercuric acetate (30µM; 20min) reduced the number of dihydromorphane binding sites in rat brain homogenate and increased the sensitivity of the agonist to the inhibitory effect on sodium binding[4]. p-Aminophenylmercuric acetate treatment (100µM) for 1h activated the betacellulin precursor (pro-BTC) shedding in Wild-type dermal fibroblasts transfected with BTC-hemagglutinin (HA)[5]. Treatment with p-Aminophenylmercuric acetate (>0.3μg/ml) for 24 hours significantly induced the death of murine lymphocytes[6].
References:
[1] Gendron R, Grenier D, Sorsa T, et al. Inhibition of the activities of matrix metalloproteinases 2, 8, and 9 by chlorhexidine[J]. Clinical Diagnostic Laboratory Immunology, 1999, 6(3): 437-439.
[2] Backstrom J R, Tökés Z A. The 84‐kDa form of human matrix metalloproteinase‐9 degrades substance P and gelatin[J]. Journal of neurochemistry, 1995, 64(3): 1312-1318.
[3] Kanakkanatt S V, Patel V S, Patel R G, et al. Novel Methods of Synthesis of Dithizonate Type Photochromic Dyes & Polymers[J]. Molecular Crystals and Liquid Crystals Science and Technology. Section A. Molecular Crystals and Liquid Crystals, 1994, 246(1): 159-168.
[4] PASTERNAK G W, WILSON H A, SNYDER S H. Differential effects of protein-modifying reagents on receptor binding of opiate agonists and antagonists[J]. Molecular Pharmacology, 1975, 11(3): 340-351.
[5] Sanderson M P, Erickson S N, Gough P J, et al. ADAM10 mediates ectodomain shedding of the betacellulin precursor activated by p-aminophenylmercuric acetate and extracellular calcium influx[J]. Journal of Biological Chemistry, 2005, 280(3): 1826-1837.
[6] Kim H M, Hong D H, Lee C W, et al. Studies on cell-specific cytotoxicities induced by p-aminophenyl-mercuric acetate (APMA)[J]. The Journal of Toxicological Sciences, 1998, 23(SupplementIV): 653-656.
p-Aminophenylmercuric acetate是一种有机汞化合物，可作为MMP激活剂，能够作用于蛋白质巯基或诱导与MMP-8激活和抑制均相关的半胱氨酸转换反应[1]。p-Aminophenylmercuric acetate能将从人源细胞系HL-60中纯化的无活性前体形式MMP-9（94kDa）转化为中间活性形式（84kDa）[2]。p-Aminophenylmercuric acetate可作为结构单元用于合成新型光致变色染料[3]。
在体外，p-Aminophenylmercuric acetate处理（30µM；20分钟）减少了大鼠脑匀浆中二氢吗啡结合位点的数量，并提高了激动剂对钠结合抑制效应的敏感性[4]。p-Aminophenylmercuric acetate处理（100µM）1小时激活了转染BTC-hemagglutinin (HA)的野生型皮肤成纤维细胞中betacellulin前体（pro-BTC）的脱落过程[5]。使用浓度高于0.3µg/ml的p-Aminophenylmercuric acetate处理24小时，可显著诱导小鼠淋巴细胞死亡[6]。