Search for Articles:
Title / Keyword
Author / Affiliation / Email
Journal
Article Type
 
 
Advanced Search
 
Section
Special Issue
Volume
Issue
Number
Page
 
8.3
5.5
Journals
Biomolecules
Special Issues
Novel Molecules for Cancer Treatment 2.0
share announcement

Novel Molecules for Cancer Treatment 2.0

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 6453

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

Published Papers (3 papers)

Download All Papers
Order results
Result details
Show export options expand_more Show export options expand_less
Select all
Export citation of selected articles as:

Research

Jump to: Review

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 1 | Viewed by 1063
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 2.0)
►▼ Show Figures

Figure 1

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 3 | Viewed by 2058
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 2.0)
►▼ Show Figures

Graphical abstract

Review

Jump to: Research

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 37 | Viewed by 2494
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 2.0)
►▼ Show Figures

Figure 1

Show export options expand_more Show export options expand_less
Select all
Export citation of selected articles as:
 
Displaying articles 1-3
Back to TopTop