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Pharmaceuticals, Volume 18, Issue 10

October 2025 - 169 articles

Cover Story: Peptidomimetics incorporating a γ-lactam Gln derivative at the P1 site, originally developed as SARS-CoV-2 Mpro inhibitors, exhibited strong affinity for human cathepsin S (hCatS). In silico studies revealed that despite being solvent-exposed, the γ-lactam at P1 position might be involved in water-mediated hydrogen bonds. Molecular dynamics simulations suggested the presence of two predominant conformations, up and down, which differ in the γ-lactam orientation. Repurposing thousands of peptide-based SARS-CoV-2 Mpro inhibitors containing a γ-lactam at the P1 site, combined with new rational structure–activity relationship studies exploring the S1 pocket, could enable the identification of new potent and selective hCatS ligands. View this paper
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Articles (169)

  • Review
  • Open Access
919 Views
28 Pages

21 October 2025

Predicting RNA–small molecule binding sites is essential for developing RNA-targeted drugs. Identifying these sites experimentally is often costly, making computational methods essential for drug discovery. While traditional approaches rely on...

  • Review
  • Open Access
1,864 Views
29 Pages

Cyclodextrins as Active Therapeutic Agents: Beyond Their Role as Excipients

  • Andreea Silvia Pirvu,
  • Renata-Maria Varut,
  • Diana-Maria Trasca,
  • George Alin Stoica,
  • Kristina Radivojevic,
  • Sirbulet Carmen,
  • Cristian Cosmin Arsenie and
  • Cristina Popescu

21 October 2025

Cyclodextrins (CDs) have traditionally been recognized as excipients that enhance solubility and stability of drugs. However, growing evidence shows that CDs themselves can act as active therapeutic agents. Their unique supramolecular properties enab...

  • Article
  • Open Access
613 Views
41 Pages

Polyprenylated Acylphloroglucinols from Hypericum rochelii and Hypericum olympicum—Cytotoxic Effects on Non-Tumorigenic Cell Lines and Antibacterial Potential

  • Yana Ilieva,
  • Maya M. Zaharieva,
  • Lyudmila Dimitrova,
  • Mila D. Kaleva,
  • Teodor Marinov,
  • Lili I. Dobreva,
  • Tanya Chan Kim,
  • Zlatina Kokanova-Nedialkova,
  • Iliyan Trayanov and
  • Sofia Titorenkova
  • + 4 authors

21 October 2025

Objectives: Research on the antimicrobial effect of Hypericum plant constituents is very rarely accompanied by studies of the cytotoxic effect on cell lines. In the current study, besides microbiological tests, an investigation of the cytotoxicity of...

  • Systematic Review
  • Open Access
1 Citations
3,778 Views
16 Pages

Efficacy of Lamotrigine in the Treatment of Unipolar and Bipolar Depression: Meta-Analysis of Acute and Maintenance Randomised Controlled Trials

  • Danilo Arnone,
  • Linda Östlundh,
  • Meena Mosa,
  • Brianne MacDonald,
  • Jonathan Oldershaw,
  • Tarik Qassem and
  • Allan H. Young

21 October 2025

Background/Objectives: Lamotrigine has been widely investigated in the treatment and prevention of the emergence of symptoms of depression in unipolar and bipolar depression. This work systematically appraises published and unpublished double-blind r...

  • Article
  • Open Access
796 Views
26 Pages

Unraveling the Antihyperglycemic Effects of Dipeptyl Peptidase-4 Inhibitors in Rodents: A Multi-Faceted Approach Combining Effects on Glucose Homeostasis, Molecular Docking, and ADMET Profiling

  • Raquel N. S. Roriz,
  • Claudia J. P. Cardozo,
  • Gabriela A. Freire,
  • Caio B. R. Martins,
  • Raimundo Rigoberto B. X. Filho,
  • Landerson Lopes Pereira,
  • Gisele F. P. Rangel,
  • Tiago L. Sampaio,
  • Lyanna R. Ribeiro and
  • Gisele Silvestre Silva
  • + 16 authors

21 October 2025

Background/Objectives: Dipeptidyl peptidase-4 (DPP-4) inhibitors are antidiabetic agents that regulate blood glucose by preventing the degradation of active incretin hormones. Although clinically effective, this drug class is associated with adverse...

  • Article
  • Open Access
462 Views
18 Pages

Comparative Safety of Empirical Antibiotic Classes in Newly Hospitalized COVID-19 Patients

  • Kalynn Park,
  • Sohyeon Park,
  • Jung Yoon Choi,
  • Chaeyoon Kim,
  • Jeongha Yun,
  • Jiyeon Bae,
  • Ji Yun Bae,
  • Kang-Il Jun,
  • Jeong-Han Kim and
  • Chung-Jong Kim
  • + 2 authors

21 October 2025

Background: Empirical antibiotic use is common in hospitalized patients with COVID-19 despite the low prevalence of bacterial coinfection, raising concerns about antimicrobial resistance and inappropriate prescribing. However, the comparative safety...

  • Article
  • Open Access
785 Views
17 Pages

Anti-Trichomonas vaginalis Activity of Triterpenes from Tagetes nelsonii Greenm

  • Mario Alberto Hernández-Torres,
  • Sara García-Davis,
  • José J. Fernández,
  • Ana R. Diaz-Marrero,
  • Magda Elizabeth Hernández-García,
  • Irma Edith Carranza-Torres and
  • Ezequiel Viveros-Valdez

21 October 2025

Background: Trichomonas vaginalis is the causative agent of human trichomoniasis, the most common non-viral sexually transmitted infection. This disease is associated with an increased susceptibility to HIV and HPV infections. Currently, resistance t...

  • Article
  • Open Access
717 Views
20 Pages

Enhanced Skin Permeation of Diclofenac Sodium Using Mango Seed Kernel Starch Nanoparticles

  • Sesha Rajeswari Talluri,
  • Namrata S. Matharoo,
  • Nirali Dholaria,
  • Nubul Albayati,
  • Shali John and
  • Bozena Michniak-Kohn

20 October 2025

Background: Mango seed kernels, an agro-industrial waste byproduct, constitute approximately 40–50% of the fruit’s weight and serve as a substantial source of starch. There are only a few reported studies on the pharmaceutical application...

  • Article
  • Open Access
653 Views
24 Pages

An Efficacy- and In Vivo Exposure-Oriented Integrated Study to Investigate the Effective Components of Qishen Granule

  • Yueting Li,
  • Tengteng Wang,
  • Chao Cheng,
  • Yingying Huo,
  • Ying Tan,
  • Yifan Xu,
  • Jiale Gao,
  • Jie Liu and
  • Hongbin Xiao

20 October 2025

Background: Qishen granule (QSG) is a widely prescribed herbal formula for the treatment of chronic heart failure. The mechanisms of action of QSG have been clarified; however, the effective substances remain unclear. This lack of clarity hinders qua...

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Pharmaceuticals - ISSN 1424-8247