Urease inhibitors for the treatment of H. pylori.

IF 5.4 2区 医学 Q1 CHEMISTRY, MEDICINAL Expert Opinion on Therapeutic Patents Pub Date : 2024-11-10 DOI:10.1080/13543776.2024.2423004
Özlen Güzel-Akdemir, Atilla Akdemir
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Abstract

Introduction: Helicobacter pylori 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 H. pylori have been described. This paper will on H. pylori Urease (HPU).

Area covered: 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 H. pylori growth inhibition will be discussed.

Expert opinion: 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.

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治疗幽门螺杆菌的尿素酶抑制剂。
幽门螺杆菌是一种革兰氏阴性细菌,感染了世界上几乎一半的人口。虽然许多感染者没有症状,但这种微生物仍可导致各种胃肠道疾病,甚至胃腺癌。世界卫生组织(WHO)将其视为开发新抗生素的优先病原体。幽门螺杆菌的许多毒力因子已被描述。这里的重点是尿素酶。这种酶将尿素转化为二氧化碳和氨。氨能中和幽门螺杆菌周围微环境中的胃酸,从而保护幽门螺杆菌。本文将讨论幽门螺杆菌尿素酶(HPU)的(病理)生理学和结构。此外,还将讨论对幽门螺杆菌尿素酶具有已知活性的尿素酶抑制剂或可抑制幽门螺杆菌生长的抑制剂。
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来源期刊
CiteScore
12.10
自引率
1.50%
发文量
50
审稿时长
6-12 weeks
期刊介绍: Expert Opinion on Therapeutic Patents (ISSN 1354-3776 [print], 1744-7674 [electronic]) is a MEDLINE-indexed, peer-reviewed, international journal publishing review articles on recent pharmaceutical patent claims, providing expert opinion the scope for future development, in the context of the scientific literature. The Editors welcome: Reviews covering recent patent claims on compounds or applications with therapeutic potential, including biotherapeutics and small-molecule agents with specific molecular targets; and patenting trends in a particular therapeutic area Patent Evaluations examining the aims and chemical and biological claims of individual patents Perspectives on issues relating to intellectual property The audience consists of scientists, managers and decision-makers in the pharmaceutical industry and others closely involved in R&D Sample our Bioscience journals, sign in here to start your access, Latest two full volumes FREE to you for 14 days.
期刊最新文献
Mycobacterium tuberculosis inhibitors: an updated patent review (2021-present). Urease inhibitors for the treatment of H. pylori. A patent review of UNC-51-like kinase 1/2 inhibitors (2019-present). Menin-MLL protein-protein interaction inhibitors: a patent review (2021-present). Therapeutic compounds targeting interleukin-1 receptor-associated kinase 4 (IRAK4): an updated patent review (2019 to present).
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