{"title":"治疗幽门螺杆菌的尿素酶抑制剂。","authors":"Özlen Güzel-Akdemir, Atilla Akdemir","doi":"10.1080/13543776.2024.2423004","DOIUrl":null,"url":null,"abstract":"<p><strong>Introduction: </strong><i>Helicobacter pylori</i> 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 <i>H. pylori</i> have been described. This paper will on <i>H. pylori</i> Urease (HPU).</p><p><strong>Area covered: </strong>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 <i>H. pylori</i> growth inhibition will be discussed.</p><p><strong>Expert opinion: </strong>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.</p>","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1-14"},"PeriodicalIF":5.4000,"publicationDate":"2024-11-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Urease inhibitors for the treatment of <i>H. pylori</i>.\",\"authors\":\"Özlen Güzel-Akdemir, Atilla Akdemir\",\"doi\":\"10.1080/13543776.2024.2423004\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Introduction: </strong><i>Helicobacter pylori</i> 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 <i>H. pylori</i> have been described. This paper will on <i>H. pylori</i> Urease (HPU).</p><p><strong>Area covered: </strong>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 <i>H. pylori</i> growth inhibition will be discussed.</p><p><strong>Expert opinion: </strong>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.</p>\",\"PeriodicalId\":12314,\"journal\":{\"name\":\"Expert Opinion on Therapeutic Patents\",\"volume\":\" \",\"pages\":\"1-14\"},\"PeriodicalIF\":5.4000,\"publicationDate\":\"2024-11-10\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Expert Opinion on Therapeutic Patents\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1080/13543776.2024.2423004\",\"RegionNum\":2,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Expert Opinion on Therapeutic Patents","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1080/13543776.2024.2423004","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
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.
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.
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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
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