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Drug Discovery and Development Based on Native/Engineered Microorganisms

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

Deadline for manuscript submissions: closed (31 August 2020) | Viewed by 9816

Special Issue Editors


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Department of Life Science and Biochemical Engineering, Sun Moon University, 70, Sunmoon-ro 221, Tangjeong-myeon, Asan-si, Chungnam 31460, Republic of Korea
Interests: antibiotics; bio-active molecules; nanoparticles; drug development and discovery; chemical biology
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DeFENS, Department of Food, Environmental and Nutritional Sciences, Università degli Studi di Milano, Via Celoria 2, 20133 Milano, Italy
Interests: transition metal catalyzed reactions; synthetic methodologies to obtain bioactive molecules
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Guest Editor
Department of Pharmacy, “G. d’Annunzio” University of Chieti-Pescara, Chieti, Italy
Interests: drug discovery; computational techniques; anticancer agents; aromatase inhibitors
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Guest Editor
Chemistry Lab, Florida International University, Post St Lucie, FL, USA
Interests: natural product chemistry; medicinal and analytical chemistry; computational chemistry; drug discovery and development; neurodegenerative diseases; solid phase peptide synthesis (SPPS)
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Faculty of Pharmacy, University of Ljubljana, Askerceva 7, 1000 Ljubljana, Slovenia
Interests: drug discovery; medicinal chemistry; organic synthesis; enzyme inhibitors; immunomodulators; antimicrobials; anticancer agents; antioxidants; cinnamic acid derivatives
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Special Issue Information

Dear Colleagues,

Most of the molecules utilized as drugs are obtained from microorganisms. These molecules can be natural compounds or their derivatives. In most cases, the useful compounds are obtained at low titers or are cryptic, so various metabolic engineering/genetic engineering approaches are utilized to enhance the production titer. Recent advances in the isolation/culture of previously uncultivable microorganisms and the availability of versatile genetic engineering approaches have taken microbial engineering to the next horizon. However, in cases where the molecules are not accessible from the native host under natural conditions, alternative/heterologous production platforms are utilized. Approaches such as “genome mining” have enabled the connection of secondary metabolites to their respective biosynthetic genetic codes, whereas the application of metabolic engineering, synthetic biology tools, and genome engineering has contributed remarkably to drug development based on engineered microorganisms. Hence, this Special Issue will cover all aspects of drug discovery and development utilizing native/engineered microorganisms.

Potential topics of interest include, but are not limited to:

  • Advances in the isolation/characterization of microorganisms with potential compounds;
  • Isolation/characterization of novel bioactive molecules;
  • Metabolic engineering, synthetic biology, and genome engineering for modulating the production titer from native/heterologous hosts;
  • Chemical/biological approaches for the production of novel compounds;
  • Bioactivities and mechanisms of action of microbe-derived compounds;

Dr. Dipesh Dhakal
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. 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

  • drug discovery
  • natural microbial products
  • microorganisms
  • synthetic biology
  • metabolic engineering
  • bioactivity

Published Papers (2 papers)

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Research

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20 pages, 9542 KiB  
Article
Searching Hit Potential Antimicrobials in Natural Compounds Space against Biofilm Formation
by Roberto Pestana-Nobles, Jorge A. Leyva-Rojas and Juvenal Yosa
Molecules 2020, 25(22), 5334; https://doi.org/10.3390/molecules25225334 - 16 Nov 2020
Cited by 6 | Viewed by 2754
Abstract
Biofilms are communities of microorganisms that can colonize biotic and abiotic surfaces and thus play a significant role in the persistence of bacterial infection and resistance to antimicrobial. About 65% and 80% of microbial and chronic infections are associated with biofilm formation, respectively. [...] Read more.
Biofilms are communities of microorganisms that can colonize biotic and abiotic surfaces and thus play a significant role in the persistence of bacterial infection and resistance to antimicrobial. About 65% and 80% of microbial and chronic infections are associated with biofilm formation, respectively. The increase in infections by multi-resistant bacteria instigates the need for the discovery of novel natural-based drugs that act as inhibitory molecules. The inhibition of diguanylate cyclases (DGCs), the enzyme implicated in the synthesis of the second messenger, cyclic diguanylate (c-di-GMP), involved in the biofilm formation, represents a potential approach for preventing the biofilm development. It has been extensively studied using PleD protein as a model of DGC for in silico studies as virtual screening and as a model for in vitro studies in biofilms formation. This study aimed to search for natural products capable of inhibiting the Caulobacter crescentus enzyme PleD. For this purpose, 224,205 molecules from the natural products ZINC15 database, have been evaluated through molecular docking and molecular dynamic simulation. Our results suggest trans-Aconitic acid (TAA) as a possible starting point for hit-to-lead methodologies to obtain new inhibitors of the PleD protein and hence blocking the biofilm formation. Full article
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Review

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22 pages, 969 KiB  
Review
Exploiting the Biosynthetic Potency of Taxol from Fungal Endophytes of Conifers Plants; Genome Mining and Metabolic Manipulation
by Ashraf S.A. El-Sayed, Manal T. El-Sayed, Amgad M. Rady, Nabila Zein, Gamal Enan, Ahmed Shindia, Sara El-Hefnawy, Mahmoud Sitohy and Basel Sitohy
Molecules 2020, 25(13), 3000; https://doi.org/10.3390/molecules25133000 - 30 Jun 2020
Cited by 30 | Viewed by 6457
Abstract
Endophytic fungi have been considered as a repertoire for bioactive secondary metabolites with potential application in medicine, agriculture and food industry. The biosynthetic pathways by fungal endophytes raise the argument of acquisition of these machineries of such complex metabolites from the plant host. [...] Read more.
Endophytic fungi have been considered as a repertoire for bioactive secondary metabolites with potential application in medicine, agriculture and food industry. The biosynthetic pathways by fungal endophytes raise the argument of acquisition of these machineries of such complex metabolites from the plant host. Diterpenoids “Taxol” is the most effective anticancer drug with highest annual sale, since its discovery in 1970 from the Pacific yew tree, Taxus brevifolia. However, the lower yield of Taxol from this natural source (bark of T. brevifolia), availability and vulnerability of this plant to unpredicted fluctuation with the ecological and environmental conditions are the challenges. Endophytic fungi from Taxus spp. opened a new avenue for industrial Taxol production due to their fast growth, cost effectiveness, independence on climatic changes, feasibility of genetic manipulation. However, the anticipation of endophytic fungi for industrial Taxol production has been challenged by the loss of its productivity, due to the metabolic reprograming of cells, downregulating the expression of its encoding genes with subculturing and storage. Thus, the objectives of this review were to (1) Nominate the endophytic fungal isolates with the Taxol producing potency from Taxaceae and Podocarpaceae; (2) Emphasize the different approaches such as molecular manipulation, cultural optimization, co-cultivation for enhancing the Taxol productivities; (3) Accentuate the genome mining of the rate-limiting enzymes for rapid screening the Taxol biosynthetic machinery; (4) Triggering the silenced rate-limiting genes and transcriptional factors to activates the biosynthetic gene cluster of Taxol. Full article
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