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327340

REVIEW OF SERINE PROTEASE INHIBITORS: DEVELOPMENT AND APPLICATIONS

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Last updated: 04 Jan 2025

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Abstract

A class of enzymes known as proteases is responsible for catalyzing the breakdown of covalent peptide bonds. Proteases account for almost 2% of the genes in humans, infectious organisms, and other forms of life.  Serine proteases, so named because they have a nucleophilic serine residue at the active site, make for nearly one-third of all proteases. Although digesting is their primary role in humans, they also play roles in immunological response, apoptosis, inflammation, blood coagulation, and signal transduction. They are therefore very attractive biological targets for the design of pharmacological molecules that can modulate their activity.
This review presents a description of the catalytic activity and structure of serine proteases, and the different strategies to develop inhibitors. Serine protease inhibitors targeting thrombin, FXa, and human neutrophil elastase (HNE), and dipeptidylprotease-4 (DPP4) will be described. It includes therapeutically applied, and those drugs which are still under investigation in clinical trials in the last two decades.

DOI

10.21608/bfsa.2023.327340

Keywords

Serine protease inhibitor, Thrombin, FXa, HNE, DPP4

Authors

First Name

Mai

Last Name

Ramadan

MiddleName

Abed ElRahman

Affiliation

Department of Pharmaceutical Chemistry and Pharmacognosy, Faculty of Pharmacy, Al-Azhar University- Gaza, Gaza, B. O Box: 1277, Palestine

Email

m.ramadan@alazhar.edu.ps

City

Gaza

Orcid

0000-0001-8032-5777

Volume

46

Article Issue

2

Related Issue

44483

Issue Date

2023-12-01

Receive Date

2023-02-16

Publish Date

2023-12-01

Page Start

835

Page End

854

Print ISSN

1110-0052

Online ISSN

3009-7703

Article File

BFSA_Volume 46_Issue 2_Pages 835-854.pdf

PDF . 1.3MB

Link

https://bpsa.journals.ekb.eg/article_327340.html

Detail API

https://bpsa.journals.ekb.eg/service?article_code=327340

Order

327,340

Type

Review Article

Type Code

2,839

Publication Type

Journal

Publication Title

Bulletin of Pharmaceutical Sciences Assiut University

Publication Link

https://bpsa.journals.ekb.eg/

MainTitle

REVIEW OF SERINE PROTEASE INHIBITORS: DEVELOPMENT AND APPLICATIONS

Details

Type

Article

Created At

25 Dec 2024