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胎盘碱性磷酸酶(PLAP)发光高通量筛选检测 - 探针2

Placental Alkaline Phosphatase (PLAP) Luminescent HTS assay - Probe 2

作者信息

Lanier Marion, Cashman John, Sergienko Eduard, Garcia Xochella, Brown Brock, Rascon Justin, Narisawa Sonoko, Simao Ana Maria, Millán José Luis, Stonich Derek, Su Ying, Dahl Russell, Chung Thomas DY

Abstract

Placental alkaline phosphatase (PLAP) is highly expressed in primate placental tissue. Its biological function and relevance are still unknown, but PLAP-like enzymes are detected in serum of patients with primary testicular tumors, in particular seminoma and other cancers. Consequently, the identification of PLAP-specific inhibitors with selectivity over tissue non-specific alkaline phosphatase (TNAP) and intestinal alkaline phosphatase (IAP) may provide the necessary tools to characterize its biological role. Currently, inhibitors of PLAP lack either potency or selectivity. The small molecule probe ML095 (CID-25067483) is a biochemical inhibitor of PLAP, and will be useful to elucidate the key biological functions and natural substrates of human PLAP.

摘要

胎盘碱性磷酸酶(PLAP)在灵长类胎盘组织中高度表达。其生物学功能及相关性仍不清楚,但在原发性睾丸肿瘤患者的血清中,尤其是精原细胞瘤和其他癌症患者的血清中可检测到类似PLAP的酶。因此,鉴定出对组织非特异性碱性磷酸酶(TNAP)和肠道碱性磷酸酶(IAP)具有选择性的PLAP特异性抑制剂,可能会为表征其生物学作用提供必要工具。目前,PLAP抑制剂要么缺乏效力,要么缺乏选择性。小分子探针ML095(CID-25067483)是PLAP的生化抑制剂,将有助于阐明人PLAP的关键生物学功能和天然底物。

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