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Novel Molecules for Cancer Treatment (2nd Edition)
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Novel Molecules for Cancer Treatment (2nd Edition)

A special issue of Biomolecules (ISSN 2218-273X). This special issue belongs to the section "Molecular Medicine".

Deadline for manuscript submissions: 30 September 2024 | Viewed by 13460

Special Issue Editor

Dr. Javier Martínez Useros

E-Mail Website
Guest Editor
OncoHealth Institute, Health Research Institute—Fundacion Jimenez Diaz University Hospital, Rey Juan Carlos University, 28040 Madrid, Spain
Interests: gastric cancer; pancreatic cancer; colorectal cancer and metastatic melanoma
Special Issues, Collections and Topics in MDPI journals

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 thorough mechanisms that generate tumors from early stages 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 greatly helped the identification of new targets for designing drugs. These drugs could be chemically synthesized or isolated from natural substances. These novel molecules represent a massive step forward in reaching personalized medicine in present clinical practice.

In this Special Issue, entitled "Novel Molecules for Cancer Treatment 2.0", we encourage authors to submit high-quality research articles dealing with novel biomolecules and providing strong evidence of their antitumor potential activity to the scientific and clinical communities. 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 that could provide rationales for further translational oncology research.

I look forward to receiving your manuscripts.

Dr. Javier Martinez 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.

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

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

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Published Papers (6 papers)

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Research

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15 pages, 4181 KiB  
Article
PPARγ Antagonists Exhibit Antitumor Effects by Regulating Ferroptosis and Disulfidptosis
by Shiyu Zhang, Ying Wang, Junjie Gu, Yang Yang, Jing Liang, Yimei Wang, Ning Ji, Ming Liu, Yingxin Zhang, Silu Sun, Qianming Chen and Jing Li
Biomolecules 2024, 14(5), 596; https://doi.org/10.3390/biom14050596 - 18 May 2024
Viewed by 3774
Abstract
Oral squamous cell carcinoma (OSCC) stands as a prevalent subtype of head and neck squamous cell carcinoma, leading to disease recurrence and low survival rates. PPARγ, a ligand-dependent nuclear transcription factor, holds significance in tumor development. However, the role of PPARγ in the [...] Read more.
Oral squamous cell carcinoma (OSCC) stands as a prevalent subtype of head and neck squamous cell carcinoma, leading to disease recurrence and low survival rates. PPARγ, a ligand-dependent nuclear transcription factor, holds significance in tumor development. However, the role of PPARγ in the development of OSCC has not been fully elucidated. Through transcriptome sequencing analysis, we discovered a notable enrichment of ferroptosis-related molecules upon treatment with PPARγ antagonist. We subsequently confirmed the occurrence of ferroptosis through transmission electron microscopy, iron detection, etc. Notably, ferroptosis inhibitors could not completely rescue the cell death caused by PPARγ inhibitors, and the rescue effect was the greatest when disulfidptosis and ferroptosis inhibitors coexisted. We confirmed that the disulfidptosis phenotype indeed existed. Mechanistically, through qPCR and Western blotting, we observed that the inhibition of PPARγ resulted in the upregulation of heme oxygenase 1 (HMOX1), thereby promoting ferroptosis, while solute carrier family 7 member 11 (SLC7A11) was also upregulated to promote disulfidptosis in OSCC. Finally, a flow cytometry analysis of flight and multiplex immunohistochemical staining was used to characterize the immune status of PPARγ antagonist-treated OSCC tissues in a mouse tongue orthotopic transplantation tumor model, and the results showed that the inhibition of PPARγ led to ferroptosis and disulfidptosis, promoted the aggregation of cDCs and CD8+ T cells, and inhibited the progression of OSCC. Overall, our findings reveal that PPARγ plays a key role in regulating cell death in OSCC and that targeting PPARγ may be a potential therapeutic approach for OSCC. Full article
(This article belongs to the Special Issue Novel Molecules for Cancer Treatment (2nd Edition))
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31 pages, 7428 KiB  
Article
Discovery of A Novel Series of Quinazoline–Thiazole Hybrids as Potential Antiproliferative and Anti-Angiogenic Agents
by Alexandru Șandor, Ionel Fizeșan, Ioana Ionuț, Gabriel Marc, Cristina Moldovan, Ilioara Oniga, Adrian Pîrnău, Laurian Vlase, Andreea-Elena Petru, Ioana Macasoi and Ovidiu Oniga
Biomolecules 2024, 14(2), 218; https://doi.org/10.3390/biom14020218 - 12 Feb 2024
Cited by 2 | Viewed by 1636
Abstract
Considering the pivotal role of angiogenesis in solid tumor progression, we developed a novel series of quinazoline–thiazole hybrids (SA01–SA07) as antiproliferative and anti-angiogenic agents. Four out of the seven compounds displayed superior antiproliferative activity (IC50 =1.83-4.24 µM) on HepG2 cells [...] Read more.
Considering the pivotal role of angiogenesis in solid tumor progression, we developed a novel series of quinazoline–thiazole hybrids (SA01–SA07) as antiproliferative and anti-angiogenic agents. Four out of the seven compounds displayed superior antiproliferative activity (IC50 =1.83-4.24 µM) on HepG2 cells compared to sorafenib (IC50 = 6.28 µM). The affinity towards the VEGFR2 kinase domain was assessed through in silico prediction by molecular docking, molecular dynamics studies, and MM-PBSA. The series displayed a high degree of similarity to sorafenib regarding the binding pose within the active site of VEGFR2, with a different orientation of the 4-substituted-thiazole moieties in the allosteric pocket. Molecular dynamics and MM-PBSA evaluations identified SA05 as the hybrid forming the most stable complex with VEGFR2 compared to sorafenib. The impact of the compounds on vascular cell proliferation was assessed on EA.hy926 cells. Six compounds (SA01–SA05, SA07) displayed superior anti-proliferative activity (IC50 = 0.79–5.85 µM) compared to sorafenib (IC50 = 6.62 µM). The toxicity was evaluated on BJ cells. Further studies of the anti-angiogenic effect of the most promising compounds, SA04 and SA05, through the assessment of impact on EA.hy296 motility using a wound healing assay and in ovo potential in a CAM assay compared to sorafenib, led to the confirmation of the anti-angiogenic potential. Full article
(This article belongs to the Special Issue Novel Molecules for Cancer Treatment (2nd Edition))
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17 pages, 3043 KiB  
Article
Nanobody-Based EGFR-Targeting Immunotoxins for Colorectal Cancer Treatment
by Javier Narbona, Luisa Hernández-Baraza, Rubén G. Gordo, Laura Sanz and Javier Lacadena
Biomolecules 2023, 13(7), 1042; https://doi.org/10.3390/biom13071042 - 26 Jun 2023
Cited by 8 | Viewed by 2664
Abstract
Immunotoxins (ITXs) are chimeric molecules that combine the specificity of a targeting domain, usually derived from an antibody, and the cytotoxic potency of a toxin, leading to the selective death of tumor cells. However, several issues must be addressed and optimized in order [...] Read more.
Immunotoxins (ITXs) are chimeric molecules that combine the specificity of a targeting domain, usually derived from an antibody, and the cytotoxic potency of a toxin, leading to the selective death of tumor cells. However, several issues must be addressed and optimized in order to use ITXs as therapeutic tools, such as the selection of a suitable tumor-associated antigen (TAA), high tumor penetration and retention, low kidney elimination, or low immunogenicity of foreign proteins. To this end, we produced and characterized several ITX designs, using a nanobody against EGFR (VHH 7D12) as the targeting domain. First, we generated a nanoITX, combining VHH 7D12 and the fungal ribotoxin α-sarcin (αS) as the toxic moiety (VHHEGFRαS). Then, we incorporated a trimerization domain (TIEXVIII) into the construct, obtaining a trimeric nanoITX (TriVHHEGFRαS). Finally, we designed and characterized a bispecific ITX, combining the VHH 7D12 and the scFv against GPA33 as targeting domains, and a deimmunized (DI) variant of α-sarcin (BsITXαSDI). The results confirm the therapeutic potential of α-sarcin-based nanoITXs. The incorporation of nanobodies as target domains improves their therapeutic use due to their lower molecular size and binding features. The enhanced avidity and toxic load in the trimeric nanoITX and the combination of two different target domains in the bispecific nanoITX allow for increased antitumor effectiveness. Full article
(This article belongs to the Special Issue Novel Molecules for Cancer Treatment (2nd Edition))
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Review

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13 pages, 737 KiB  
Review
Plectin: Dual Participation in Tumor Progression
by Zhihui Wang, Wenbin Wang, Qing Luo and Guanbin Song
Biomolecules 2024, 14(9), 1050; https://doi.org/10.3390/biom14091050 - 24 Aug 2024
Viewed by 465
Abstract
The plectin gene can encode a cytoskeletal linking protein, plectin, known for its interaction with three critical components of the cellular cytoskeleton: intermediate filaments, microtubules, and actin filaments. In recent years, more and more studies have reported that plectin is closely related to [...] Read more.
The plectin gene can encode a cytoskeletal linking protein, plectin, known for its interaction with three critical components of the cellular cytoskeleton: intermediate filaments, microtubules, and actin filaments. In recent years, more and more studies have reported that plectin is closely related to tumorigenesis and development, exhibiting both tumor-suppressive and tumor-promoting functions. Here, we first introduce the molecular structure and function of plectin, and then we summarize the current understanding of the crucial role of plectin in cancer progression. Finally, we also discuss the possible reasons for the different roles of plectin expression in various types of cancer and highlight the double-edged sword role of plectin in tumor progression. The review aims to deepen the comprehensive understanding of plectin’s role in cancer and further help to develop novel therapeutic strategies and drug targets. Full article
(This article belongs to the Special Issue Novel Molecules for Cancer Treatment (2nd Edition))
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21 pages, 962 KiB  
Review
The Next Chapter in Cancer Diagnostics: Advances in HPV-Positive Head and Neck Cancer
by Antea Krsek, Lara Baticic, Tamara Braut and Vlatka Sotosek
Biomolecules 2024, 14(8), 925; https://doi.org/10.3390/biom14080925 - 30 Jul 2024
Viewed by 591
Abstract
Human papillomavirus (HPV)-associated head and neck squamous cell carcinoma (HNSCC), particularly oropharyngeal squamous cell carcinoma (OPSCC), is an increasingly prevalent pathology worldwide, especially in developed countries. For diagnosing HPV in HNSCC, the combination of p16 immunohistochemistry (IHC) and polymerase chain reaction (PCR) offers [...] Read more.
Human papillomavirus (HPV)-associated head and neck squamous cell carcinoma (HNSCC), particularly oropharyngeal squamous cell carcinoma (OPSCC), is an increasingly prevalent pathology worldwide, especially in developed countries. For diagnosing HPV in HNSCC, the combination of p16 immunohistochemistry (IHC) and polymerase chain reaction (PCR) offers high sensitivity and specificity, with p16 IHC being a reliable initial screen and PCR confirming HPV presence. Advanced techniques like next-generation sequencing (NGS) and RNA-based assays provide detailed insights but are primarily used in research settings. Regardless of HPV status, standard oncological treatments currently include surgery, radiation, and/or chemotherapy. This conventional approach does not account for the typically better prognosis of HPV-positive HNSCC patients, leading to increased chemo/radiation-induced secondary morbidities and reduced quality of life. Therefore, it is crucial to identify and detect HPV positivity and other molecular characteristics of HNSCC to personalize treatment strategies. This comprehensive review aims to summarize current knowledge on various HPV detection techniques and evaluate their advantages and disadvantages, with a focus on developing methodologies to identify new biomarkers in HPV-positive HNSCC. The review discusses direct and indirect HPV examination in tumor tissue, DNA- and RNA-based detection techniques, protein-based markers, liquid biopsy potentials, immune-related markers, epigenetic markers, novel biomarkers, and emerging technologies, providing an overall insight into the current state of knowledge. Full article
(This article belongs to the Special Issue Novel Molecules for Cancer Treatment (2nd Edition))
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22 pages, 3194 KiB  
Review
Recent Advances of Tubulin Inhibitors Targeting the Colchicine Binding Site for Cancer Therapy
by Mohammed Hawash
Biomolecules 2022, 12(12), 1843; https://doi.org/10.3390/biom12121843 - 10 Dec 2022
Cited by 52 | Viewed by 3207
Abstract
Cancer accounts for numerous deaths each year, and it is one of the most common causes of death worldwide, despite many breakthroughs in the discovery of novel anticancer candidates. Each new year the FDA approves the use of new drugs for cancer treatments. [...] Read more.
Cancer accounts for numerous deaths each year, and it is one of the most common causes of death worldwide, despite many breakthroughs in the discovery of novel anticancer candidates. Each new year the FDA approves the use of new drugs for cancer treatments. In the last years, the biological targets of anticancer agents have started to be clearer and one of these main targets is tubulin protein; this protein plays an essential role in cell division, as well as in intracellular transportation. The inhibition of microtubule formation by targeting tubulin protein induces cell death by apoptosis. In the last years, numerous novel structures were designed and synthesized to target tubulin, and this can be achieved by inhibiting the polymerization or depolymerization of the microtubules. In this review article, recent novel compounds that have antiproliferation activities against a panel of cancer cell lines that target tubulin are explored in detail. This review article emphasizes the recent developments of tubulin inhibitors, with insights into their antiproliferative and anti-tubulin activities. A full literature review shows that tubulin inhibitors are associated with properties in the inhibition of cancer cell line viability, inducing apoptosis, and good binding interaction with the colchicine binding site of tubulin. Furthermore, some drugs, such as cabazitaxel and fosbretabulin, have been approved by FDA in the last three years as tubulin inhibitors. The design and development of efficient tubulin inhibitors is progressively becoming a credible solution in treating many species of cancers. Full article
(This article belongs to the Special Issue Novel Molecules for Cancer Treatment (2nd Edition))
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