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Recent Prototype Drug Development: Insights in Protein Science and Enzymology...
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Recent Prototype Drug Development: Insights in Protein Science and Enzymology for Precision Medicine

A special issue of Biology (ISSN 2079-7737).

Deadline for manuscript submissions: closed (31 May 2024) | Viewed by 7766

Special Issue Editors

Prof. Dr. Hang Fai (Henry) Kwok

E-Mail Website
Guest Editor
1. Institute of Translational Medicine, Faculty of Health Sciences, University of Macau, Avenida de Universidade, Taipa, Macau SAR 999078, China
2. Department of Biomedical Sciences, Faculty of Health Sciences, University of Macau, Avenida de Universidade, Taipa, Macau SAR 999078, China
Interests: novel therapeutic antibodies development; venom-based peptide & natural biomolecule prototype drugs development; cancer biomarkers & immunotherapy markers discovery for prognostic and therapeutic validation
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Tianbao Chen

E-Mail Website
Guest Editor
Natural Drug Discovery Group, School of Pharmacy, Queen’s University Belfast, Belfast BT7 1NN, UK
Interests: peptide science; antibiotic resistance; structure–activity relationship; drug design
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The specificity and precise mechanisms of drugs are crucial in reducing the severity of side effects associated with their use. Adverse effects may require that the drug dosages be reduced or the drug regimen be changed such that the drugs tolerable to patients. As we are enter the third decade of the 21st century, the achievements made by biomedical scientists and pharmaceutical institutes/companies have been exceptional in the last decade, leading to significant advancements in the fast-growing field of druggable target identification for drug screening and development via advanced protein science and enzymology research.

We are pleased to invite you to contribute research and/or review articles on the latest developments in molecular pharmacology and enzymology research in the precision medicine era. We aim to bring leading researchers together to exchange and share their recent findings in molecular pharmacology, prototype drug development, and precision medicine for different disease treatments.

In this Special Issue, original research articles and reviews are welcome. Research areas may include (but not limited to) the following:

  • Molecular pharmacology
  • Precision medicine
  • Druggable genes
  • Signal inhibition
  • Immune checkpoint inhibitors
  • Stress tolerance
  • Drug resistance
  • Network pharmacology
  • Predictive biomarkers

We look forward to receiving your contributions.

Prof. Dr. Hang Fai (Henry) Kwok
Prof. Dr. Tianbao Chen
Guest Editors

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. Biology 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

  • immunotherapy
  • targeted therapy
  • therapeutic antibody
  • chemotherapy
  • novel bioactive molecule
  • biomarker
  • drug resistance
  • enzymology
  • molecular pharmacology
  • precision medicine

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Published Papers (2 papers)

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24 pages, 4325 KiB  
Article
The Molecular Mechanisms of Oleanane Aldehyde-β-enone Cytotoxicity against Doxorubicin-Resistant Cancer Cells
by Natalia Moiseeva, Daria Eroshenko, Lidia Laletina, Ekaterina Rybalkina, Olga Susova, Aida Karamysheva, Irina Tolmacheva, Mikhail Nazarov and Victoria Grishko
Biology 2023, 12(3), 415; https://doi.org/10.3390/biology12030415 - 8 Mar 2023
Cited by 3 | Viewed by 2416
Abstract
Oleanane aldehyde-β-enone (OA), being the semi-synthetic derivative of the triterpenoid betulin, effectively inhibits the proliferation of HBL-100 and K562 cancer cells (IC50 0.47–0.53 µM), as well as the proliferation of their resistant subclones with high P-gp expression HBL-100/Dox, K562/i-S9 and [...] Read more.
Oleanane aldehyde-β-enone (OA), being the semi-synthetic derivative of the triterpenoid betulin, effectively inhibits the proliferation of HBL-100 and K562 cancer cells (IC50 0.47–0.53 µM), as well as the proliferation of their resistant subclones with high P-gp expression HBL-100/Dox, K562/i-S9 and K562/i-S9_Dox (IC50 0.45−1.24 µM). A molecular docking study, rhodamine efflux test, synergistic test with Dox, and ABC transporter gene expression were used to investigate the ability of OA to act as a P-gp substrate or inhibitor against Dox-resistant cells. We noted a trend toward a decrease in ABCB1, ABCC1 and ABCG2 expression in HBL-100 cells treated with OA. The in silico and in vitro methods suggested that OA is neither a direct inhibitor nor a competitive substrate of P-gp in overexpressing P-gp cancer cells. Thus, OA is able to overcome cellular resistance and can accumulate in Dox-resistant cells to realize toxic effects. The set of experiments suggested that OA toxic action can be attributed to activating intrinsic/extrinsic or only intrinsic apoptosis pathways in Dox-sensitive and Dox-resistant cancer cells, respectively. The cytotoxicity of OA in resistant cells is likely mediated by a mitochondrial cell death pathway, as demonstrated by positive staining with Annexin V–FITC, an increasing number of cells in the subG0/G1 phase, reactive oxygen species generation, mitochondrial dysfunction, cytochrome c migration and caspases-9,-6 activation. Full article
(This article belongs to the Special Issue Recent Prototype Drug Development: Insights in Protein Science and Enzymology for Precision Medicine)
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16 pages, 2030 KiB  
Article
Evaluation of the Antimicrobial Properties of a Natural Peptide from Vespa mandarinia Venom and Its Synthetic Analogues as a Possible Route to Defeat Drug-Resistant Microbes
by Jin Zhang, Ruize Sun, Zhiwei Chen, Chunyuan Zhou, Chengbang Ma, Mei Zhou, Xiaoling Chen, Tianbao Chen, Chris Shaw and Lei Wang
Biology 2022, 11(9), 1263; https://doi.org/10.3390/biology11091263 - 25 Aug 2022
Viewed by 2328
Abstract
Antimicrobial peptides (AMPs) from wasp venom have a good track record and potential for drug development as tools against development of antimicrobial resistance. Herein, the biological function and activity profile of peptide VM, which was discovered in the venom of the wasp, Vespa [...] Read more.
Antimicrobial peptides (AMPs) from wasp venom have a good track record and potential for drug development as tools against development of antimicrobial resistance. Herein, the biological function and activity profile of peptide VM, which was discovered in the venom of the wasp, Vespamandarinia, and several of its third-position substituted analogues, were investigated. VM had potent antimicrobial activity against Gram-positive bacteria and biofilm, and all modified peptides achieved the significant enhancement of these capacities. The various physicochemical properties of amino acids substituted in analogues, generated the different mechanisms of action of bacterial membrane disruption. VM-3K showed a maximum 8-fold enhancement of antibacterial activity against Gram-positive bacteria and also presented microbicidal properties against Gram-negative bacteria and fungi. This peptide also exhibited a high killing efficiency at low concentration and had a comparable selectivity index to VM. Furthermore, VM-3K produced a 90% survival of S. aureus-infected waxworms at a concentration of 5.656 mg/kg, at which concentration the natural template peptide only achieved 50% survival. This peptide also lacked short-term resistance generation. Thus, peptide VM-3K could be a promising broad-spectrum antimicrobial candidate for addressing the current antibiotic-resistant infection crisis. It is worth mentioning that this investigation on the relationship between peptide structure and mechanism of action could become an important aspect of drug research on short peptides. Full article
(This article belongs to the Special Issue Recent Prototype Drug Development: Insights in Protein Science and Enzymology for Precision Medicine)
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