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基于碎片的发现使用直角生物物理技术的新型VE-PTP抑制剂

Wataru Asano¹, Kenji Yamanaka¹, Yasunori Ohara¹

¹Biological/Pharmacological Research Laboratories, Central Pharmaceutical Research Institute, Japan Tobacco Inc., 1-1 Murasaki-cho, Takatsuki, Osaka 569-1125, Japan.

|July 6, 2023

概括

研究人员发现了Cpd-2,一种新的,选择性的血管内皮蛋白氨酸酸酶 (VE-PTP) 抑制剂. 这种弱酸性化合物为开发针对VE-PTP的可生物利用药物提供了新的途径,用于治疗癌症等疾病.

科学领域:

生物化学生物化学
药理学药理学是指药理学的学科.
分子生物学分子生物学

背景情况:

氨酸酸化是一种关键的翻译后修饰,调节生物过程,并与癌症和动脉样硬化等疾病有关.
血管内皮蛋白氨酸酸酶 (VE-PTP) 对血管平衡和血管生成至关重要,使其成为潜在的治疗点.
目前,没有药物有效向蛋白氨酸酸酶 (PTP),包括VE-PTP.

研究的目的:

发现VE-PTP的新型抑制剂.
确定一种用于开发可生物利用VE-PTP抑制剂的化合物.
探索用于PTP向药物开发的新化学支架.

主要方法:

基于碎片的查被用于识别潜在的抑制剂.
用各种生物物理技术来描述化合物相互作用.
为了优化抑制剂的特性,进行了结构-活性关系研究.

主要成果:

一种新的VE-PTP抑制剂被发现,被指定为Cpd-2.
Cpd-2具有弱酸性结构和高选择性,与现有的强酸性抑制剂有很大的区别.
该化合物代表了进一步药物开发的有希望的起点.

结论:

Cpd-2是第一个被发现的VE-PTP抑制剂,具有弱酸性和高选择性.
这一发现为开发可生物利用的VE-PTP抑制剂开辟了新的可能性.
针对VE-PTP使用Cpd-2等新型抑制剂可能为血管相关疾病提供治疗效益.

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