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Bioorganic Chemistry in Europe
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Bioorganic Chemistry in Europe

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

Deadline for manuscript submissions: 31 December 2024 | Viewed by 3382

Special Issue Editors

Dr. Marilisa Leone

E-Mail Website
Guest Editor
Institute of Biostructures and Bioimaging (IBB), National Research Council of Italy (CNR), Via Mezzocannone 16, 80134 Naples, Italy
Interests: structural biology; NMR; drug discovery; conformational analysis of proteins and peptides; protein–protein interactions (PPIs); design and evaluation of PPI inhibitors; structure-based drug design; molecular modeling; docking; cancer
Special Issues, Collections and Topics in MDPI journals
Dr. Marian Vincenzi

E-Mail Website
Guest Editor Assistant
Institute of Biostructures and Bioimaging (IBB), National Research Council of Italy (CNR), Via Pietro Castellino 111, 80131 Naples, Italy
Interests: structural biology; drug discovery; structure-based drug design; NMR; docking

Special Issue Information

Dear Colleagues,

Bioorganic chemistry is an emerging field at the interface between the traditional fields of chemistry and biochemistry. This Special Issue of Molecules aims to collect papers about bioorganic chemistry from European scholars. Potential topics include, but are not limited to, the following:

  • Chemoenzymatic synthesis and use of enzymes in organic chemistry;
  • Enzyme inhibitors;
  • Biocatalysis (ribozymes and catalytic antibodies);
  • Combinatorial biosynthesis and biomimetic synthesis;
  • Membrane chemistry;
  • Peptide chemistry;
  • Biopolymers and artificial supramolecular assemblies;
  • Organic chemistry aspects of genetic engineering;
  • Bioactive peptides and proteins.

Scientists from Europe are cordially invited to contribute original research papers or reviews to this Special Issue, which discusses new knowledge or cutting-edge developments in the bioorganic chemistry research field.

Dr. Marilisa Leone
Guest Editor

Dr. Marian Vincenzi
Guest Editor Assistant

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

  • enzyme inhibitors
  • biocatalysis
  • membrane chemistry
  • peptide chemistry
  • bioactive peptides and proteins

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Published Papers (2 papers)

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Review

32 pages, 3523 KiB  
Review
Agents Targeting the Bacterial Cell Wall as Tools to Combat Gram-Positive Pathogens
by Aliaksandr Zhydzetski, Zuzanna Głowacka-Grzyb, Michal Bukowski, Tomasz Żądło, Emilia Bonar and Benedykt Władyka
Molecules 2024, 29(17), 4065; https://doi.org/10.3390/molecules29174065 - 27 Aug 2024
Viewed by 807
Abstract
The cell wall is an indispensable element of bacterial cells and a long-known target of many antibiotics. Penicillin, the first discovered beta-lactam antibiotic inhibiting the synthesis of cell walls, was successfully used to cure many bacterial infections. Unfortunately, pathogens eventually developed resistance to [...] Read more.
The cell wall is an indispensable element of bacterial cells and a long-known target of many antibiotics. Penicillin, the first discovered beta-lactam antibiotic inhibiting the synthesis of cell walls, was successfully used to cure many bacterial infections. Unfortunately, pathogens eventually developed resistance to it. This started an arms race, and while novel beta-lactams, either natural or (semi)synthetic, were discovered, soon upon their application, bacteria were developing resistance. Currently, we are facing the threat of losing the race since more and more multidrug-resistant (MDR) pathogens are emerging. Therefore, there is an urgent need for developing novel approaches to combat MDR bacteria. The cell wall is a reasonable candidate for a target as it differentiates not only bacterial and human cells but also has a specific composition unique to various groups of bacteria. This ensures the safety and specificity of novel antibacterial agents that target this structure. Due to the shortage of low-molecular-weight candidates for novel antibiotics, attention was focused on peptides and proteins that possess antibacterial activity. Here, we describe proteinaceous agents of various origins that target bacterial cell wall, including bacteriocins and phage and bacterial lysins, as alternatives to classic antibiotic candidates for antimicrobial drugs. Moreover, advancements in protein chemistry and engineering currently allow for the production of stable, specific, and effective drugs. Finally, we introduce the concept of selective targeting of dangerous pathogens, exemplified by staphylococci, by agents specifically disrupting their cell walls. Full article
(This article belongs to the Special Issue Bioorganic Chemistry in Europe)
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22 pages, 1115 KiB  
Review
A Phenotypic Approach to the Discovery of Potent G-Quadruplex Targeted Drugs
by Stephen Neidle
Molecules 2024, 29(15), 3653; https://doi.org/10.3390/molecules29153653 - 1 Aug 2024
Cited by 2 | Viewed by 1969
Abstract
G-quadruplex (G4) sequences, which can fold into higher-order G4 structures, are abundant in the human genome and are over-represented in the promoter regions of many genes involved in human cancer initiation, progression, and metastasis. They are plausible targets for G4-binding small molecules, which [...] Read more.
G-quadruplex (G4) sequences, which can fold into higher-order G4 structures, are abundant in the human genome and are over-represented in the promoter regions of many genes involved in human cancer initiation, progression, and metastasis. They are plausible targets for G4-binding small molecules, which would, in the case of promoter G4s, result in the transcriptional downregulation of these genes. However, structural information is currently available on only a very small number of G4s and their ligand complexes. This limitation, coupled with the currently restricted information on the G4-containing genes involved in most complex human cancers, has led to the development of a phenotypic-led approach to G4 ligand drug discovery. This approach was illustrated by the discovery of several generations of tri- and tetra-substituted naphthalene diimide (ND) ligands that were found to show potent growth inhibition in pancreatic cancer cell lines and are active in in vivo models for this hard-to-treat disease. The cycles of discovery have culminated in a highly potent tetra-substituted ND derivative, QN-302, which is currently being evaluated in a Phase 1 clinical trial. The major genes whose expression has been down-regulated by QN-302 are presented here: all contain G4 propensity and have been found to be up-regulated in human pancreatic cancer. Some of these genes are also upregulated in other human cancers, supporting the hypothesis that QN-302 is a pan-G4 drug of potential utility beyond pancreatic cancer. Full article
(This article belongs to the Special Issue Bioorganic Chemistry in Europe)
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