Güzel-Akdemir Özlen, Akdemir Atilla
Department of Pharmaceutical Chemistry, Istanbul University, Faculty of Pharmacy, Beyazit/Istanbul, Turkey.
Department of Pharmacology, Faculty of Pharmacy, Istinye University, Sariyer/Istanbul, Turkey.
Expert Opin Ther Pat. 2025 Jan;35(1):17-30. doi: 10.1080/13543776.2024.2423004. Epub 2024 Nov 10.
infects almost half of the World population. Although many infected people are symptom free, the microorganism can still cause a variety of gastrointestinal disorders and gastric adenocarcinoma. It is considered a priority pathogen for the development of new antibiotics by the World Health Organisation (WHO). Many virulence factors of have been described. This paper will on Urease (HPU).
This paper will discuss the (patho)physiology and structure of HPU. In addition, urease inhibitors with known activity against the HPU or inhibitors that show growth inhibition will be discussed.
Increase in selectivity, affinity and potency of HPU inhibitors can be achieved by the design of compounds that interact with distinct regions within the enzyme active site. Especially, covalent interactions seem promising as they clearly effect the dose requirement of the drug candidate.
感染了世界上近一半的人口。尽管许多感染者没有症状，但这种微生物仍可导致多种胃肠道疾病和胃腺癌。它被世界卫生组织（WHO）视为开发新型抗生素的优先病原体。已经描述了许多的毒力因子。本文将聚焦于脲酶（HPU）。
本文将讨论HPU的（病理）生理学和结构。此外，还将讨论对HPU具有已知活性的脲酶抑制剂或显示生长抑制作用的抑制剂。
通过设计与酶活性位点内不同区域相互作用的化合物，可以提高HPU抑制剂的选择性、亲和力和效力。特别是，共价相互作用似乎很有前景，因为它们明显影响候选药物的剂量需求。
