HP Proliant SL230s

Company: HP Development Company

Catalog#: SL230s

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A Direct in vitro Fatty Acylation Assay for Hedgehog Acyltransferase

Adina R. Schonbrun and Marilyn D. Resh

Published online: 2022-12-20

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Virtual Screening of Transmembrane Serine Protease Inhibitors

Author:

Antti Poso, Topi Tervonen and Juha Klefström,

Date:

2017-04-20

[Abstract] The human family of type II transmembrane serine proteases includes 17 members. The defining features of these proteases are an N-terminal transmembrane domain and a C-terminal serine protease of the chymotrypsin (S1) fold, separated from each other by a variable stem region. Recently accumulated evidence suggests a critical role for these proteases in development of cancer and metastatic capacity. Both the cancer relevance and the accessibility of the extracellularly oriented catalytic domain for therapeutic and imaging agents have fueled drug discovery interest in the type II class of transmembrane serine proteases. Typically, the initial hit discovery processes aim to identify molecules with verifiable activity at the drug target and with sufficient drug-like characters. We present ... [摘要] II型跨膜丝氨酸蛋白酶的人类家族包括17个成员。这些蛋白酶的定义特征是糜蛋白酶（S1）折叠的N末端跨膜结构域和C末端丝氨酸蛋白酶，通过可变的茎区彼此分离。最近积累的证据表明这些蛋白酶在癌症和转移能力的发展中起关键作用。肿瘤相关性和用于治疗和成像剂的细胞外定向催化结构域的可及性促使药物发现对II型跨膜丝氨酸蛋白酶的兴趣。通常，初始命中发现过程旨在识别在药物靶标上具有可验证活性的分子，并具有足够的药物样特征。我们在这里提出了用于跨膜丝氨酸蛋白酶hepinin的候选配体的基于结构的虚拟筛选方案。该方法描述了使用三磷酸腺嘌呤的催化位点的3D结构与ZINC进行分子对接，ZINC是具有 3000万种可购买化合物的分子数据库。小的候选子集经过实验测试，具有可证实的命中，为进一步的铅开发提供了有用的配体结构线索。

受控的蛋白水解活性在细胞过程和信号传导中发挥重要作用，正如所有生物体中蛋白酶的存在所证明的，包括病毒，原核生物和真核生物。不足为奇的是，异常调节的蛋白酶活性是造成人类病态，如心血管疾病和炎症疾病，骨质疏松症，神经系统疾病和癌症的多种因素（Turk，2006; ...

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HP Proliant SL230s

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