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Catalysts
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State-of-the-Art in Enzyme Inhibitors
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State-of-the-Art in Enzyme Inhibitors

A special issue of Catalysts (ISSN 2073-4344). This special issue belongs to the section "Biocatalysis".

Deadline for manuscript submissions: closed (15 May 2023) | Viewed by 8599

Special Issue Editor

Prof. Dr. Longguang Jiang

E-Mail Website
Guest Editor
College of Chemistry, Fuzhou University, Fuzhou 350116, Fujian, China
Interests: structural and functional study on serine protease inhibitors and endothelial cell receptors

Special Issue Information

Dear Colleagues,

Ever since the identification of enzymes as biological catalysts, scientists working with these macromolecules have unwittingly been finding inhibitors. Enzyme inhibitors have been shown to play important roles in various biomedical and clinical areas, from biometrics to the treatment of numerous diseases, including thrombus, diabetes, emphysema, Alzheimer’s disease, cancer, and even COVID-19. Therefore, the development of enzyme inhibitors with a broad spectrum of activity remains a hot topic for future research.

This Special Issue will focus on experimental and theoretical investigations into the development of novel enzyme inhibitors for regulating biocatalysis in vivo or in vitro. Both fundamental and applied studies on their properties, inhibitory mechanisms, and novel applications are of interest. The aim is to provide novel insights that could aid in improving the design of new enzyme inhibitors, better understanding the biological activities of enzymes, and compile a set of manuscripts that inform the field of the state of the art in enzyme inhibitors.

Prof. Dr. Longguang Jiang
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Catalysts is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • Enzyme catalysis
  • Inhibition mechanism
  • Screen enzyme inhibitors
  • Small-molecule inhibitors
  • Peptide inhibitors
  • Antibody
  • Nanozymes
  • Enzyme dynamics
  • Enzyme catalysis

Published Papers (4 papers)

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Research

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19 pages, 14603 KiB  
Article
A Novel Chalcone Derivative Regulates the Expression and Phosphorylation of ERK1/2 by Inhibiting Fli-1 Promoter Activity for Preventing the Malignant Progression of Erythroleukemia
by Min Mo, Youfen Ma, Jia Yu, Mashaal Ahmad, Xinwei Wan, Zijiang Yu, Bixue Xu and Heng Luo
Catalysts 2023, 13(1), 84; https://0-doi-org.brum.beds.ac.uk/10.3390/catal13010084 - 31 Dec 2022
Viewed by 1206
Abstract
Acute erythroleukemia is a rare form of acute myeloid leukemia recognized by its distinct phenotypic attribute of erythroblasts proliferation. In this study, in vitro experiments showed that a newly synthesized chalcone (ZH-254) inhibited cell proliferation, caused apoptosis, arrested the cell cycle in the [...] Read more.
Acute erythroleukemia is a rare form of acute myeloid leukemia recognized by its distinct phenotypic attribute of erythroblasts proliferation. In this study, in vitro experiments showed that a newly synthesized chalcone (ZH-254) inhibited cell proliferation, caused apoptosis, arrested the cell cycle in the G1 phase, and downregulated Fli-1 expression by inhibiting Fli-1 promoter activity. In vivo experiments showed that ZH-254 could effectively alleviate splenomegaly and prolong the survival of erythroleukemia mice. RT-PCR and Western blot analysis showed that ZH-254 could regulate the expression of Fli-1 target genes and G1-phase-related cell cycle proteins, including Rb, Bcl-2, Bax, ERK1/2, Gata-1, P110, SHIP-1, p-ERK1, CDK4, C-myc, Cyclin D1, Smad-3, GSK-3, and p21. Among them, the compound most significantly regulated the expression and phosphorylation of ERK1, the target gene of Fli-1 involved in regulating cell proliferation and apoptosis. Thus, ZH-254 restricts the malignancy of erythroleukemia by causing the inactivation of Fli-1 expression via suppressing its promoter activity, further regulating the expression and phosphorylation of ERK1- and G1-phase-related genes. These results reveal the critical role of Fli-1 in the growth and survival of various hematological malignancies and point to chalcone derivatives as lead compounds for the development of anti-Fli-1 drugs for the treatment of erythroleukemia with overexpression of Fli-1. Full article
(This article belongs to the Special Issue State-of-the-Art in Enzyme Inhibitors)
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10 pages, 1867 KiB  
Article
Structural Studies of Bypass of Forespore Protein C from Bacillus Subtilis to Reveal Its Inhibitory Molecular Mechanism for SpoIVB
by Xinyun Zhang, Gaohui Sun, Cai Yuan, Longguang Jiang and Mingdong Huang
Catalysts 2022, 12(12), 1530; https://0-doi-org.brum.beds.ac.uk/10.3390/catal12121530 - 28 Nov 2022
Viewed by 1045
Abstract
Activation of pro-σK processing requires a signaling protease SpoIVB that is secreted from the forespore into the space between the two cells during sporulation in Bacillus subtilis. Bypass of forespore protein C (BofC) is an inhibitor preventing the autoproteolysis of SpoIVB, [...] Read more.
Activation of pro-σK processing requires a signaling protease SpoIVB that is secreted from the forespore into the space between the two cells during sporulation in Bacillus subtilis. Bypass of forespore protein C (BofC) is an inhibitor preventing the autoproteolysis of SpoIVB, ensuring the factor σK operates regularly at the correct time during the sporulation. However, the regulatory mechanisms of BofC on pro-σK processing are still unclear, especially in the aspect of the interaction between BofC and SpoIVB. Herein, the recombinant BofC (rBofC) was expressed in the periplasm by the E. coli expression system, and crystal growth conditions were obtained and optimized. Further, the crystal structure of rBofC was determined by X-ray crystallography, which is nearly identical to the structures determined by NMR and predicted by AlphaFold. In addition, the modeled structure of the BofC–SpoIVB complex provides insights into the molecular mechanism by which domain 1 of BofC occupies the active site of the SpoIVB serine protease domain, leading to the inhibition of the catalytical activity of SpoIVB and prevention of the substrate of SpoIVB (SpoIVFA) from binding to the active site. Full article
(This article belongs to the Special Issue State-of-the-Art in Enzyme Inhibitors)
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20 pages, 4185 KiB  
Article
Growth Inhibition of Two Prenylated Chalcones on Prostate Cancer Cells through the Regulation of the Biological Activity and Protein Translation of Bloom Helicase
by Bao-Fei Sun, Xu-Hui Zhu, Jing Hou, Lan-Lan Li, Yuan-Kun Qin, Jia Yu, Sha Cheng, Bi-Xue Xu, Fa-Jun Song and Heng Luo
Catalysts 2022, 12(6), 582; https://0-doi-org.brum.beds.ac.uk/10.3390/catal12060582 - 26 May 2022
Viewed by 1390
Abstract
Bloom (BLM) helicase is an important member of the RecQ family of DNA helicases that plays a vital role in the maintenance of genomic stability. The defect of BLM helicase leads to a human genetic disorder called Bloom syndrome, characterized by genomic instability, [...] Read more.
Bloom (BLM) helicase is an important member of the RecQ family of DNA helicases that plays a vital role in the maintenance of genomic stability. The defect of BLM helicase leads to a human genetic disorder called Bloom syndrome, characterized by genomic instability, specific phenotypic features, and a predisposition to many types of cancer. The predisposition to cancer caused by BLM helicase is due to defects in important DNA metabolic pathways such as replication, recombination, and repair. Therefore, the aim of this work was to investigate the effects of two prenylated chalcones, WZH-10 and WZH-43, on the expression of BLM helicase in prostate cancer cells, as well as the biological activity of the purified BLM helicase from cancer cells. This might lead to a better understanding of the role of BLM helicase in the aforementioned DNA metabolic pathways that directly influence chromosomal integrity leading to cancer. The results indicated that the two prenylated chalcones inhibited the growth of prostate cancer cells PC3 by inducing apoptosis and arresting the cell cycle. However, they only inhibited the protein expression of BLM helicase without regulating its transcriptional expression. In addition, they did not significantly regulate the expression of the homologous family members WRN and RECQL1, although the DNA unwinding and ATPase activity of BLM helicase were inhibited by the two prenylated chalcones. Finally, a negligible effect was found on the DNA-binding activity of this enzyme. These results demonstrated that prenylated chalcones can be an effective intervention on the expression and function of the BLM helicase protein in cancer cells to inhibit their growth. Therefore, they might provide a novel strategy for developing new anti-cancer drugs targeting the genomic stability and DNA helicase. Full article
(This article belongs to the Special Issue State-of-the-Art in Enzyme Inhibitors)
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Review

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13 pages, 312 KiB  
Review
Advances in the Clinical Application of Histamine and Diamine Oxidase (DAO) Activity: A Review
by Zhaowang Tan, Yingwei Ou, Wenwei Cai, Yueliang Zheng, Hengjie Li, Yunyun Mao, Shengang Zhou and Jianfeng Tu
Catalysts 2023, 13(1), 48; https://0-doi-org.brum.beds.ac.uk/10.3390/catal13010048 - 26 Dec 2022
Cited by 5 | Viewed by 4302
Abstract
The serum level of diamine oxidase (DAO) reflects the integrity and maturation of the small intestinal mucosa. This measure is important in diagnosing various diseases, including chronic urticaria tachyphylaxis, multiple organ dysfunction syndrome, preterm abortion, and migraine. This review aimed to summarize the [...] Read more.
The serum level of diamine oxidase (DAO) reflects the integrity and maturation of the small intestinal mucosa. This measure is important in diagnosing various diseases, including chronic urticaria tachyphylaxis, multiple organ dysfunction syndrome, preterm abortion, and migraine. This review aimed to summarize the findings of previous studies on the changes in DAO levels in diverse diseases and the application of this enzyme in the clinical setting, as well as the roles of this enzyme under physiological and pathological conditions. The advances in the mechanism and clinical application of DAO presented in this review will contribute to a better understanding of this enzyme and open up new and broader perspectives for future basic research and clinical applications. Full article
(This article belongs to the Special Issue State-of-the-Art in Enzyme Inhibitors)
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