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Biomolecules, Volume 14, Issue 12

December 2024 - 174 articles

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Cover Story: Antimicrobial resistance (AMR) and cancer are pressing global health threats. Advances in medicinal chemistry have led to the development of hybrid compounds targeting both AMR and cancer. A recent study reported that a series of 4-substituted-5-(2-(pyridine-2-ylamino)ethyl)-2,4-dihydro-3H-1,2,4-triazole-3-thiones and their chloro analogs possess antimicrobial and anticancer activities. Two 1,2,4-triazole-3-thiones were identified as exceptionally active (MIC 0.9 µg/mL) against C. tenuis, while several chloropyridine derivatives had high antibacterial potency. The target compounds, especially two pyridine ring-bearing hydrazone, significantly reduced cancer cell viability; in silico modeling indicated that they target the MAP kinase pathway, and 4-methylthiobenzylidene derivative demonstrated the highest affinity. View this paper

Articles (174)

  • Review
  • Open Access
8 Citations
4,256 Views
23 Pages

Gut Microbiota Modulation: A Novel Strategy for Rheumatoid Arthritis Therapy

  • Vitaly Chasov,
  • Elvina Gilyazova,
  • Irina Ganeeva,
  • Ekaterina Zmievskaya,
  • Damir Davletshin,
  • Aygul Valiullina and
  • Emil Bulatov

23 December 2024

Rheumatoid arthritis (RA) is a chronic autoimmune disease that leads to joint inflammation, progressive tissue damage and significant disability, severely impacting patients’ quality of life. While the exact mechanisms underlying RA remain elus...

  • Review
  • Open Access
1,403 Views
13 Pages

23 December 2024

G protein-coupled receptors (GPCRs) regulate multiple cellular functions and represent important drug targets. More than 20 years ago, it was noted that GPCR activation (agonist binding) and signaling (G protein activation) are dependent on the membr...

  • Article
  • Open Access
2 Citations
1,670 Views
18 Pages

PLGA-Nano-Encapsulated Disulfiram Inhibits Cancer Stem Cells and Targets Non-Small Cell Lung Cancer In Vitro and In Vivo

  • Kate Butcher,
  • Zhipeng Wang,
  • Sathishkumar Kurusamy,
  • Zaixing Zhang,
  • Mark R. Morris,
  • Mohammad Najlah,
  • Christopher McConville,
  • Vinodh Kannappan and
  • Weiguang Wang

23 December 2024

Cancer stem cells (CSCs) play a key role in non-small cell lung cancer (NSCLC) chemoresistance and metastasis. In this study, we used two NSCLC cell lines to investigate the regulating effect of hypoxia in the induction and maintenance of CSC traits....

  • Article
  • Open Access
2 Citations
1,330 Views
16 Pages

MicroRNA-150 Deletion from Adult Myofibroblasts Augments Maladaptive Cardiac Remodeling Following Chronic Myocardial Infarction

  • Satoshi Kawaguchi,
  • Marisa N. Sepúlveda,
  • Jian-peng Teoh,
  • Taiki Hayasaka,
  • Bruno Moukette,
  • Tatsuya Aonuma,
  • Hyun Cheol Roh,
  • Meena S. Madhur and
  • Il-man Kim

22 December 2024

MicroRNA (miR: small noncoding RNA)-150 is evolutionarily conserved and is downregulated in patients with diverse forms of heart failure (HF) and in multiple mouse models of HF. Moreover, miR-150 is markedly correlated with the outcome of patients wi...

  • Review
  • Open Access
5 Citations
3,193 Views
15 Pages

22 December 2024

The maintenance of healthy mitochondria is essential for neuronal survival and relies upon mitochondrial quality control pathways involved in mitochondrial biogenesis, mitochondrial dynamics, and mitochondrial autophagy (mitophagy). Mitochondrial dys...

  • Article
  • Open Access
1 Citations
1,430 Views
18 Pages

Serum T2-High Inflammation Mediators in Eosinophilic COPD

  • Andrius Januskevicius,
  • Egle Vasyle,
  • Airidas Rimkunas,
  • Jolita Palacionyte,
  • Virginija Kalinauskaite-Zukauske and
  • Kestutis Malakauskas

21 December 2024

Eosinophils are central inflammatory cells in asthma; however, a portion of patients with chronic obstructive pulmonary disease (COPD) have blood or sputum eosinophilia, a condition termed eosinophilic COPD (eCOPD), which may contribute to the progre...

  • Review
  • Open Access
1 Citations
2,006 Views
20 Pages

Binding Molecules in Tick Saliva for Targeting Host Cytokines, Chemokines, and Beyond

  • Chamberttan Souza Desidério,
  • Victor Hugo Palhares Flávio-Reis,
  • Yago Marcos Pessoa-Gonçalves,
  • Rafael Destro Rosa Tiveron,
  • Helioswilton Sales-Campos,
  • Andrei Giacchetto Felice,
  • Siomar de Castro Soares,
  • Rhainer Guillermo-Ferreira,
  • Wellington Francisco Rodrigues and
  • Carlo José Freire Oliveira

21 December 2024

Ticks have coevolved with their hosts over millions of years, developing the ability to evade hemostatic, inflammatory, and immunological responses. Salivary molecules from these vectors bind to cytokines, chemokines, antibodies, complement system pr...

  • Review
  • Open Access
18 Citations
6,147 Views
23 Pages

Lactate and Lactylation: Dual Regulators of T-Cell-Mediated Tumor Immunity and Immunotherapy

  • Zhi-Nan Hao,
  • Xiao-Ping Tan,
  • Qing Zhang,
  • Jie Li,
  • Ruohan Xia and
  • Zhaowu Ma

21 December 2024

Lactate and its derivative, lactylation, play pivotal roles in modulating immune responses within the tumor microenvironment (TME), particularly in T-cell-mediated cancer immunotherapy. Elevated lactate levels, a hallmark of the Warburg effect, contr...

  • Article
  • Open Access
2 Citations
1,360 Views
28 Pages

Suppression of MT5-MMP Reveals Early Modulation of Alzheimer’s Pathogenic Events in Primary Neuronal Cultures of 5xFAD Mice

  • Dominika Pilat,
  • Jean-Michel Paumier,
  • Laurence Louis,
  • Christine Manrique,
  • Laura García-González,
  • Delphine Stephan,
  • Anne Bernard,
  • Raphaëlle Pardossi-Piquard,
  • Frédéric Checler and
  • Michel Khrestchatisky
  • + 3 authors

21 December 2024

We previously reported that membrane-type 5-matrix metalloproteinase (MT5-MMP) deficiency not only reduces pathological hallmarks of Alzheimer’s disease (AD) in 5xFAD (Tg) mice in vivo but also impairs interleukin-1 beta (IL-1β)-media...

  • Article
  • Open Access
1 Citations
1,157 Views
12 Pages

Characterization of the Interaction of Human γS Crystallin with Metal Ions and Its Effect on Protein Aggregation

  • Reinier Cardenas,
  • Arline Fernandez-Silva,
  • Vanesa Ramirez-Bello and
  • Carlos Amero

21 December 2024

Cataracts are diseases characterized by the opacity of the ocular lens and the subsequent deterioration of vision. Metal ions are one of the factors that have been reported to induce crystallin aggregation. For HγS crystallin, several equivalen...

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