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Small Molecule Compounds for Drug Designs
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Small Molecule Compounds for Drug Designs

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

Deadline for manuscript submissions: 31 August 2024 | Viewed by 683

Special Issue Editor

Dr. Hideki Tatsukawa

E-Mail Website
Guest Editor
Cellular Biochemistry Laboratory, Graduate School of Pharmaceutical Sciences, Nagoya University, Tokai National Higher Education and Research System, Nagoya 464-8601, Japan
Interests: small-molecule drugs; target molecules; drug design; cellular biochemistry; machine learning; molecular model

Special Issue Information

Dear Colleagues,

In the field of drug development, small-molecule compounds still play a central role in the development of effective therapeutics. In this Special Issue, we present the latest trends and prospects for the development of new drugs through advanced and creative research.

We welcome research papers on a wide range of topics, including the identification of new target molecules, synthesis of small-molecule drugs using rational design methods and innovative chemical approaches, the evaluation of their effects in bioassays and animal models, and their clinical application. We also look forward to sharing new insights into improving the efficiency of the drug design process, with a focus on methods utilizing advanced technologies such as computational chemistry and machine learning.

We hope that this Special Issue will provide a forum for a diverse group of pharmaceutical researchers, chemists and life scientists to collaborate and build on the current and comprehensive knowledge of small-molecule drugs. We hope that this Special Issue will help foster innovative progress in the development of new medicines and promote collaborative research in industry and academia.

We look forward to receiving valuable research papers from our contributors.

Dr. Hideki Tatsukawa
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at mdpi.longhoe.net 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

  • small-molecule drugs
  • drug discovery
  • synthetic drugs
  • medicinal chemistry
  • computational chemistry

Published Papers (1 paper)

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Research

17 pages, 16649 KiB  
Article
Efficacy of Trametinib in Alleviating Cisplatin-Induced Acute Kidney Injury: Inhibition of Inflammation, Oxidative Stress, and Tubular Cell Death in a Mouse Model
by Joung Eun Lee, Jung-Yeon Kim and Jaechan Leem
Molecules 2024, 29(12), 2881; https://doi.org/10.3390/molecules29122881 - 17 Jun 2024
Viewed by 478
Abstract
Cisplatin, a platinum-based chemotherapeutic, is effective against various solid tumors, but its use is often limited by its nephrotoxic effects. This study evaluated the protective effects of trametinib, an FDA-approved selective inhibitor of mitogen-activated protein kinase kinase 1/2 (MEK1/2), against cisplatin-induced acute kidney [...] Read more.
Cisplatin, a platinum-based chemotherapeutic, is effective against various solid tumors, but its use is often limited by its nephrotoxic effects. This study evaluated the protective effects of trametinib, an FDA-approved selective inhibitor of mitogen-activated protein kinase kinase 1/2 (MEK1/2), against cisplatin-induced acute kidney injury (AKI) in mice. The experimental design included four groups, control, trametinib, cisplatin, and a combination of cisplatin and trametinib, each consisting of eight mice. Cisplatin was administered intraperitoneally at a dose of 20 mg/kg to induce kidney injury, while trametinib was administered via oral gavage at 3 mg/kg daily for three days. Assessments were conducted 72 h after cisplatin administration. Our results demonstrate that trametinib significantly reduces the phosphorylation of MEK1/2 and extracellular signal-regulated kinase 1/2 (ERK1/2), mitigated renal dysfunction, and ameliorated histopathological abnormalities. Additionally, trametinib significantly decreased macrophage infiltration and the expression of pro-inflammatory cytokines in the kidneys. It also lowered lipid peroxidation by-products, restored the reduced glutathione/oxidized glutathione ratio, and downregulated NADPH oxidase 4. Furthermore, trametinib significantly inhibited both apoptosis and necroptosis in the kidneys. In conclusion, our data underscore the potential of trametinib as a therapeutic agent for cisplatin-induced AKI, highlighting its role in reducing inflammation, oxidative stress, and tubular cell death. Full article
(This article belongs to the Special Issue Small Molecule Compounds for Drug Designs)
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