Novel Molecules for Cancer Treatment (3rd Edition)

A special issue of Biomolecules (ISSN 2218-273X). This special issue belongs to the section "Natural and Bio-derived Molecules".

Deadline for manuscript submissions: 30 June 2025 | Viewed by 1497

Special Issue Editor

Special Issue Information

Dear Colleagues,

Cancer can appear anywhere in the body due to the accumulation of mutations and other genomic aberrations that lead to uncontrolled cell proliferation, the inhibition of apoptosis, and increased cell migration. Tumor cells are able to activate via mechanisms that generate tumors and develop metastases through the induction of the epithelial-to-mesenchymal transition, angiogenesis, and an immunosuppressive microenvironment. Other crucial events in tumorigenesis are the emergence of the undifferentiated phenotype, in addition to the generation and maintenance of cancer stem cells. In carcinogenesis, the coactivation of several genes and pathways is common, and the study of these factors and signaling pathways has enabled the identification of novel targets for the design of drugs. These drugs could be chemically synthesized or isolated from natural substances and represent a signficant advancement in realizing personalized medicine in present clinical practice.

In this Special Issue, entitled "Novel Molecules for Cancer Treatment (3rd Edition)", we encourage authors to submit high-quality research articles that address novel biomolecules and provide the scientific and clinical communities with strong evidence of their antitumor activity. This activity could be observed in both solid tumors and in hematological malignancies, and could be evaluated with in vitro and/or in vivo models. On the other hand, we are open to receiving updated reviews concerning novel molecules or treatment strategies based on synthetic or natural compounds and that provide a basis for further translational oncological research.

I look forward to receiving your manuscripts.

Dr. Javier Martínez Useros
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. Biomolecules is an international peer-reviewed open access monthly journal published by MDPI.

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Keywords

  • cancer
  • small molecules
  • antibody-drug-conjugated
  • tyrosine kinase inhibitors
  • target therapy
  • monoclonal antibodies
  • immunotherapy
  • natural compounds

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Published Papers (1 paper)

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Research

21 pages, 8334 KiB  
Article
A Phosphatidyl Conjugated Telomerase-Dependent Telomere-Targeting Nucleoside Demonstrates Colorectal Cancer Direct Killing and Immune Signaling
by Merve Yilmaz, Sibel Goksen, Ilgen Mender, Gunes Esendagli, Sefik Evren Erdener, Alessandra Ahmed, Ates Kutay Tenekeci, Larisa L. Birichevskaya, Sergei M. Gryaznov, Jerry W. Shay and Z. Gunnur Dikmen
Biomolecules 2024, 14(12), 1616; https://doi.org/10.3390/biom14121616 - 18 Dec 2024
Viewed by 1276
Abstract
Telomerase and telomeres are crucial in cancer cell immortalization, making them key targets for anticancer therapies. Currently, 6-thio-dG (THIO) combined with the anti-PD-1 inhibitor Cemiplimab is under phase II clinical investigation (NCT05208944) in NSCLC patients resistant to prior immunotherapies. This study presents the [...] Read more.
Telomerase and telomeres are crucial in cancer cell immortalization, making them key targets for anticancer therapies. Currently, 6-thio-dG (THIO) combined with the anti-PD-1 inhibitor Cemiplimab is under phase II clinical investigation (NCT05208944) in NSCLC patients resistant to prior immunotherapies. This study presents the design, synthesis, and evaluation of novel bimodular conjugate molecules combining telomere-targeting nucleoside analogs and phosphatidyl diglyceride groups. Among them, dihexanoyl-phosphatidyl-THIO (diC6-THIO) showed high anticancer activity with sub-µM EC50 values in vitro across various cancer cell lines. In mouse colorectal cancer models, diC6-THIO demonstrated strong anticancer effects alone and in combination with PD1/PD-L1 inhibitors. Administration of this compound resulted in the efficient formation of Telomere dysfunction Induced Foci (TIFs) in vitro, indicating an on-target, telomerase-mediated telomere-modifying mechanism of action for the molecule. Systemic treatment also activated CD4+ and CD8+ T cells while reducing regulatory T cells, indicating immune system enhancement. Notably, diC6-THIO exhibits an improved solubility profile while maintaining comparable anticancer properties, further supporting its potential as a promising therapeutic candidate. These findings highlight diC6-THIO as a promising telomere-targeting prodrug with dual effects on telomere modification and immune activation. Full article
(This article belongs to the Special Issue Novel Molecules for Cancer Treatment (3rd Edition))
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