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10th Anniversary of the Bioorganic Chemistry Section of Molecules
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10th Anniversary of the Bioorganic Chemistry Section of Molecules

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Bioorganic Chemistry".

Deadline for manuscript submissions: 30 November 2025 | Viewed by 2617

Special Issue Editors

Prof. Dr. Mark von Itzstein

E-Mail Website
Guest Editor
Institute for Glycomics, Gold Coast Campus, Griffith University, Gold Coast, QLD 4222, Australia
Interests: drug discovery; glycobiology; chemoenzymatic transformations; chemical virology; infectious diseases; cancer
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Claus Jacob

E-Mail Website
Guest Editor
Division of Bioorganic Chemistry, School of Pharmacy, Saarland University, D-66123 Saarbruecken, Germany
Interests: bioorganic chemistry; catalytic sensor/effector agents; epistemology; intracellular diagnostics; nanotechnology; natural products; reactive sulfur and selenium species; redox regulation via the cellular thiolstat
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Scott Reed

E-Mail Website
Guest Editor
Department of Chemistry, University of Colorado Denver, Campus Box 194, P.O. Box 173364, Denver, CO 80217, USA
Interests: nanoparticle-lipid conjugates as membrane mimics; nanomaterials for phototherapeutic applications; photochemistry; green synthesis; pharmacogenomics
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

In 2025, we will be celebrating the 10th anniversary of the Bioorganic Chemistry Section of Molecules. Molecules has carved out a notable space in the literature on chemistry, with an impact factor of 4.2 (2023) with a 5-year impact factor of 4.6 (2023). We are very grateful to our readers, contributing authors, peer reviewers, editors, and all those who have contributed to our Section and the journal over its many years. Your efforts have led to the international standing that this Section and Molecules now have.

To mark this important milestone, a Special Issue entitled “10th Anniversary of the Bioorganic Chemistry Section of Molecules” is being launched. This Special Issue will include communications, full papers, and high-quality review papers from the field of bioorganic chemistry.

We would like to invite and encourage all research groups in the various areas of bioorganic chemistry to make a contribution to this important and celebratory Special Issue.

Prof. Dr. Mark von Itzstein
Prof. Dr. Claus Jacob
Prof. Dr. Scott Reed
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. Molecules is an international peer-reviewed open access semimonthly 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

  • chemoenzymatic synthesis and use of enzymes in organic chemistry
  • enzyme inhibitors
  • enzyme immobilization and controlled enzyme immobilization
  • biocatalysis (ribozymes and catalytic antibodies)
  • biosynthesis
  • combinatorial biosynthesis
  • biomimetic synthesis
  • synthetic glycobiology
  • immunochemical techniques
  • membrane chemistry
  • protein and small biomolecules
  • protein–protein interactions
  • protein–molecule interactions
  • functional proteins and peptides
  • peptide chemistry
  • biopolymers and artificial supramolecular assemblies
  • the organic chemistry aspects of genetic engineering
  • neurotoxins and neuronal receptors
  • molecular recognition of nucleic acids
  • bioactive lipids
  • non-natural amino acids
  • mass spectrometry studies on biomolecules
  • bioactive peptides and proteins
  • biological signalling

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Published Papers (5 papers)

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Research

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18 pages, 3048 KiB  
Article
Colchicine Binding Site Tubulin Inhibitors Impair Vincristine-Resistant Neuroblastoma Cell Function
by Cinthia N. Reed, Kaylee B. Garrison, Joshua Thammathong, Jindrich Cinatl, Jr., Martin Michaelis, Souvik Banerjee and April M. Weissmiller
Molecules 2025, 30(10), 2186; https://doi.org/10.3390/molecules30102186 - 16 May 2025
Viewed by 88
Abstract
High-risk neuroblastoma remains a clinically challenging pediatric cancer, with an approximate five-year survival rate of ~60%. Frontline therapy for this group of patients includes surgery and intensive chemotherapy that involves combinations of the tubulin inhibitor vincristine with several other chemotherapeutics. Unfortunately, unresponsiveness to [...] Read more.
High-risk neuroblastoma remains a clinically challenging pediatric cancer, with an approximate five-year survival rate of ~60%. Frontline therapy for this group of patients includes surgery and intensive chemotherapy that involves combinations of the tubulin inhibitor vincristine with several other chemotherapeutics. Unfortunately, unresponsiveness to therapy and relapse are common, with tumors often displaying resistance to vincristine. Recently, we characterized a novel set of tubulin inhibitors that are distinct from vincristine and bind within the colchicine binding site present on tubulin monomers. Colchicine binding site inhibitors (CBSIs) have gained traction as improved chemotherapeutics due to their potential to overcome tubulin inhibitor-induced resistance. In this study, we investigate the functional impact of CBSI treatment on multiple neuroblastoma cell lines, including those that are vincristine-resistant. We demonstrate that our newly developed compounds are effective at disrupting cell division in non-resistant and resistant cells and have cellular activity against vincristine-resistant cell lines. Interestingly, we find that vincristine-resistant cell lines differ in their ability to undergo apoptotic cell death in response to CBSI treatment. Taken together, these findings provide a solid foundation to further investigate the utility of CBSIs for neuroblastoma treatment, while highlighting the distinct resistance mechanisms that can emerge in these childhood cancers. Full article
(This article belongs to the Special Issue 10th Anniversary of the Bioorganic Chemistry Section of Molecules)
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14 pages, 1702 KiB  
Article
Matrine Restores Colistin Efficacy Against mcr-1-Carrying Escherichia coli
by Zhinan Wang, Xiaowei Li, Liang Zhao, Saiwa Liu, Jingjing Du, Xi Jia, Lirui Ge, Jian Xu, Kexin Cui, Yu Ga, Jinxiu Wang and Xi Xia
Molecules 2025, 30(10), 2122; https://doi.org/10.3390/molecules30102122 - 11 May 2025
Viewed by 203
Abstract
The emergence of mcr-1-mediated colistin resistance has become a critical global health concern, highlighting the urgent need for innovative approaches to restore colistin’s therapeutic potential. In this study, we evaluated the antibacterial activity of four matrine-type alkaloids—namely, matrine, oxymatrine, sophocarpine, and sophoramine—against [...] Read more.
The emergence of mcr-1-mediated colistin resistance has become a critical global health concern, highlighting the urgent need for innovative approaches to restore colistin’s therapeutic potential. In this study, we evaluated the antibacterial activity of four matrine-type alkaloids—namely, matrine, oxymatrine, sophocarpine, and sophoramine—against mcr-1-positive Escherichia coli. While these alkaloids showed limited efficacy when used alone, the combination of matrine with colistin exhibited remarkable synergistic effects, as demonstrated by checkerboard assays and time-kill curve analyses. The matrine–colistin combination caused minimal erythrocyte damage while effectively attenuating resistance development in vitro. This synergy was further corroborated in a murine infection model, where the combination significantly reduced bacterial loads in target tissues. Mechanistic studies revealed that the matrine–colistin combination enhances antimicrobial activity by disrupting bacterial membrane integrity, increasing intracellular colistin accumulation, and triggering reactive oxygen species-mediated oxidative damage. Collectively, these findings highlight the potential of matrine as a promising adjuvant to overcome colistin resistance, providing a novel therapeutic approach to address the challenge of infections cause by multidrug-resistant Gram-negative bacteria. Full article
(This article belongs to the Special Issue 10th Anniversary of the Bioorganic Chemistry Section of Molecules)
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11 pages, 1502 KiB  
Article
Rapid and Efficient Synthesis of Succinated Thiol Compounds via Maleic Anhydride Derivatization
by Hiroshi Yamaguchi, Hikari Sugawa, Himeno Takahashi and Ryoji Nagai
Molecules 2025, 30(3), 571; https://doi.org/10.3390/molecules30030571 - 27 Jan 2025
Viewed by 821
Abstract
Succination is a non-enzymatic post-translational modification of cysteine (Cys) residues, resulting in the formation of S-(2-succino)cysteine (2SC). While hundreds of 2SC-modified proteins have been identified and are associated with the dysfunction of proteins, the underlying molecular mechanisms remain poorly understood. Conventional methods [...] Read more.
Succination is a non-enzymatic post-translational modification of cysteine (Cys) residues, resulting in the formation of S-(2-succino)cysteine (2SC). While hundreds of 2SC-modified proteins have been identified and are associated with the dysfunction of proteins, the underlying molecular mechanisms remain poorly understood. Conventional methods for synthesizing succinated compounds, such as 2SC, often require prolonged reaction times and/or HCl hydrolysis. In this study, we present a rapid and efficient synthesis method for succinated compounds using maleic anhydride, enabling more effective in vivo studies of succination mechanisms. This method was tested on thiol compounds with varying molecular weights, including Cys derivatives, Cys-containing peptides, and reduced bovine serum albumin. By incubating these compounds in an aqueous buffer with maleic anhydride dissolved in an organic solvent like diethyl ether, we achieved significantly improved succination efficiency compared to conventional methods. The succination efficiency using maleic anhydride surpassed that of fumaric acid or maleic acid. Notably, this approach facilitated the succination of amino acids, peptides, and proteins within minutes at 25 °C, without requiring acid hydrolysis. Our findings provide a straightforward, time-efficient strategy for synthesizing succinated thiol compounds, offering a valuable tool to enhance the understanding of succination’s molecular mechanisms and its role in protein function and dysfunction. Full article
(This article belongs to the Special Issue 10th Anniversary of the Bioorganic Chemistry Section of Molecules)
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14 pages, 1855 KiB  
Article
Synthesis of 2-Deoxyglycosides with Exclusive β-Configuration Using 2-SAc Glycosyl Bromide Donors
by Yang-Fan Guo, Tian-Tian Xu, Guo-Hui Zhang and Hai Dong
Molecules 2025, 30(1), 185; https://doi.org/10.3390/molecules30010185 - 5 Jan 2025
Viewed by 889
Abstract
In this study, we developed an indirect method for the synthesis of 2-deoxyglycosides with an exclusive β-configuration using glucosyl and galactosyl bromide donors with 2-thioacetyl (SAc) groups. The 2-SAc glucosyl and galactosyl bromide donors were easily obtained through the treatment of 1-OAc, 2-SAc [...] Read more.
In this study, we developed an indirect method for the synthesis of 2-deoxyglycosides with an exclusive β-configuration using glucosyl and galactosyl bromide donors with 2-thioacetyl (SAc) groups. The 2-SAc glucosyl and galactosyl bromide donors were easily obtained through the treatment of 1-OAc, 2-SAc glucose and galactose with HBr-CH3COOH solution, respectively. The glycosylation of such donors with acceptors under an improved Koenigs–Knorr condition resulted in glycosylation products with an exclusive β-configuration in excellent yields. The synthetic approach of 2-SAc glycosyl donors using glycals as the starting materials was also investigated. Based on these studies, the synthetic method of using 2-deoxyglycosides with an exclusive β-configuration through desulfurization will have more practical applications. Full article
(This article belongs to the Special Issue 10th Anniversary of the Bioorganic Chemistry Section of Molecules)
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Review

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26 pages, 1724 KiB  
Review
Therapeutic Uses of Retinol and Retinoid-Related Antioxidants
by Janka Vašková, Marek Stupák, Martina Vidová Ugurbaş, Jozef Židzik and Helena Mičková
Molecules 2025, 30(10), 2191; https://doi.org/10.3390/molecules30102191 - 16 May 2025
Viewed by 37
Abstract
Retinol and retinol-related compounds are essential for human health, particularly in cellular protection, skin health, and the management of medical conditions. Retinol—a vital form of vitamin A—is obtained through the diet as preformed vitamin A or provitamin A carotenoids, retinyl esters. These compounds [...] Read more.
Retinol and retinol-related compounds are essential for human health, particularly in cellular protection, skin health, and the management of medical conditions. Retinol—a vital form of vitamin A—is obtained through the diet as preformed vitamin A or provitamin A carotenoids, retinyl esters. These compounds are indispensable for vision, immune function, and skin health. While retinoic acid has important known biological roles, its presence is limited in the body as it is rapidly metabolized rather than stored, emphasizing the need for sufficient dietary intake. This paper is divided into chapters that highlight important aspects of retinol and retinoid-related compounds, such as their sufficient intake through food sources. The nutritional value of carotenoids is influenced by the balance between trans- and cis-isomers in food, with food processing affecting their bioactivity. Next, it is metabolism in the digestive tract. The bioavailability and efficacy of retinoids are further influenced by gut microbiota, which can modulate immune function and the expression of the genes involved in retinoid metabolism. A third important property greatly influencing their biological function is their structure, predisposing them to certain biological activities. Both retinoids and carotenoids exert key antioxidant functions by protecting cells from oxidative damage, quenching singlet oxygen, and stabilizing free radicals. However, the oxidation of carotenoids can result in various metabolites, such as epoxides and hydroxyketones, that further create a higher demand for antioxidant defenses. Additionally, carotenoids interact with lipoxygenases (LOXs), thus influencing oxidative stress, although this interaction may reduce their antioxidant efficacy. First- and second-generation retinoids regulate gene expression related to skin cell function and oncological diseases. Despite their therapeutic benefits, long-term use carries risks, such as teratogenicity. Ongoing research should aim to enhance the safety, precision, and effectiveness of retinoid therapies, expanding their therapeutic potential. Full article
(This article belongs to the Special Issue 10th Anniversary of the Bioorganic Chemistry Section of Molecules)
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