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Quo Vadis Cancer Research? On Molecular Mechanisms and Drug Discovery 2.0

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A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Oncology".

Deadline for manuscript submissions: closed (31 January 2023) | Viewed by 6348

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Special Issue Editor

Dr. Silvie Rimpelová

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Guest Editor

Department of Biochemistry and Microbiology, University of Chemistry and Technology Prague, Technická 5, Prague 6, Czech Republic
Interests: biocompatible materials; mammalian cells; cell adhesion; antimicrobial activity; anticancer activity; plasma treatment; laser modification; fluorescence microscopy; photodynamic therapy; theranostics
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Special Issue Information

Dear Colleagues,

In cancer research, an immense amount of interdisciplinary information has been gathered over the decades. The remaining gaps in the knowledge on cancer diseases at the cellular and molecular levels are being filled on a daily basis as novel research methods and novel anticancer drugs emerge. In addition, using old and already-approved drugs for different indications, such as cancer, has recently gained increased attention from the scientific community in so-called drug repurposing. Moreover, there is also a very common concept of developing compounds with multiple functionalities—from combining diagnostics with therapy (theranostics) to specific targeting, and photodynamic therapy to immunogenic cell death induction. All of these approaches will hopefully enable the early detection of cancer and help us to combat this disease with minimal side-effects.

The aim of this Special Issue “Quo Vadis Cancer Research? On Molecular Mechanisms and Drug Discovery” is to underline the advances and the most recent discoveries and progress in all fields of science dealing with cancer and its molecular substance; known and also possible synthetic and semisynthetic inhibitors and their structure–activity relationships; in silico modeling; theranostics; cancer biomarkers; and beyond. Original full research articles as well as review articles on this topic from research groups all over the world are welcome in order to disseminate scientific knowledge in these uneasy times of SARS-CoV-2. Researchers working in the fields of cancer research, imaging, drug discovery and related disciplines are encouraged to publish their recent findings in this Special Issue of the International Journal of Molecular Sciences.

Dr. Silvie Rimpelová
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. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. 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

molecular biology of cancer
resistance
in silico modeling
drug discovery
synthesis and semisynthesis
anticancer potential
structure–activity relationship
biological activity
biomarkers
diagnosis and therapy (theranostics)
targeted therapy
antibodies

Related Special Issue

Quo Vadis Cancer Research? On Molecular Mechanisms and Drug Discovery in International Journal of Molecular Sciences (42 articles)

Published Papers (3 papers)

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Research

22 pages, 3686 KiB

Open AccessArticle

Surface-Modified Inhaled Microparticle-Encapsulated Celastrol for Enhanced Efficacy in Malignant Pleural Mesothelioma

by Xuechun Wang, Gautam Chauhan, Alison R. L. Tacderas, Aaron Muth and Vivek Gupta

Int. J. Mol. Sci. 2023, 24(6), 5204; https://doi.org/10.3390/ijms24065204 - 8 Mar 2023

Cited by 1 | Viewed by 2090

Abstract

Malignant pleural mesothelioma (MPM) is a rare and aggressive cancer affecting the pleural lining of the lungs. Celastrol (Cela), a pentacyclic triterpenoid, has demonstrated promising therapeutic potential as an antioxidant, anti-inflammatory, neuroprotective agent, and anti-cancer agent. In this study, we developed inhaled surface-modified Cela-loaded poly(lactic-co-glycolic) acid (PLGA) microparticles (Cela MPs) for the treatment of MPM using a double emulsion solvent evaporation method. The optimized Cela MPs exhibited high entrapment efficiency (72.8 ± 6.1%) and possessed a wrinkled surface with a mean geometric diameter of ~2 µm and an aerodynamic diameter of 4.5 ± 0.1 µm, suggesting them to be suitable for pulmonary delivery. A subsequent release study showed an initial burst release up to 59.9 ± 2.9%, followed by sustained release. The therapeutic efficacy of Cela MPs was evaluated against four mesothelioma cell lines, where Cela MP exhibited significant reduction in IC₅₀ values, and blank MPs produced no toxicity to normal cells. Additionally, a 3D-spheroid study was performed where a single dose of Cela MP at 1.0 µM significantly inhibited spheroid growth. Cela MP was also able to retain the antioxidant activity of Cela only while mechanistic studies revealed triggered autophagy and an induction of apoptosis. Therefore, these studies highlight the anti-mesothelioma activity of Cela and demonstrate that Cela MPs are a promising inhalable medicine for MPM treatment. Full article

(This article belongs to the Special Issue Quo Vadis Cancer Research? On Molecular Mechanisms and Drug Discovery 2.0)

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17 pages, 3084 KiB

Open AccessArticle

Cytotoxicity of Isoxazole Curcumin Analogs on Chronic Myeloid Leukemia-Derived K562 Cell Lines Sensitive and Resistant to Imatinib

by Giordana Feriotto, Paolo Marchetti, Riccardo Rondanin, Federico Tagliati, Serena Aguzzi, Simone Beninati, Fabio Casciano, Claudio Tabolacci and Carlo Mischiati

Int. J. Mol. Sci. 2023, 24(3), 2356; https://doi.org/10.3390/ijms24032356 - 25 Jan 2023

Cited by 3 | Viewed by 1747

Abstract

Despite curcumin (CUR) inhibiting cell proliferation in vitro by activating apoptotic cell death, its use in pharmacological therapy is hampered by poor solubility, low stability in biological fluids, and rapid removal from the body. Therefore, CUR-derivatives with better biological and chemical–physical characteristics are needed. The bis-ketone moiety of CUR strongly influences its stability in slightly alkaline solutions such as plasma. Here, we considered its replacement with isoxazole, beta-enamine, or oxime groups to obtain more stable derivatives. The evaluation of the chemical–physical characteristics showed that only of the isoxazole derivatives 2 and 22 had better potential than CUR in terms of bioavailability. The UV–visible spectrum analysis showed that derivatives 2 and 22 had better stability than CUR in solutions mimicking the biological fluids. When tested on a panel of cell lines, derivatives 2 and 22 had marked cytotoxicity (IC50 = 0.5 µM) compared with CUR only (IC50 = 17 µM) in the chronic myeloid leukemia (CML)-derived K562 cell line. The derivative 22 was the more selective for CML cells. When administered at the average concentration found for CUR in the blood of patients, derivatives 2 and 22 had potent effects on cell cycle progression and apoptosis initiation, while CUR was ineffective. The apoptotic effect of derivatives 2 and 22 was associated with low necrosis. In addition, derivative 22 was able to reverse drug resistance in K562 cells resistant to imatinib (IM), the reference drug used in CML therapy. The cytotoxicity of derivative 22 on IM-sensitive and resistant cells was associated with upregulation of FOXN3 and CDKN1A expression, G2/M arrest, and triggering of apoptosis. In conclusion, derivative 22 has chemical–physical characteristics and biological effects superior to CUR, which allow us to hypothesize its future use in the therapy of CML and CML forms resistant to IM, either alone or in combination with this drug. Full article

(This article belongs to the Special Issue Quo Vadis Cancer Research? On Molecular Mechanisms and Drug Discovery 2.0)

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22 pages, 6864 KiB

Open AccessArticle

A 3D, Compartmental Tumor-Stromal Microenvironment Model of Patient-Derived Bone Metastasis

by Mansoureh Mohseni Garakani, Megan E. Cooke, Michael H. Weber, Michael R. Wertheimer, Abdellah Ajji and Derek H. Rosenzweig

Int. J. Mol. Sci. 2023, 24(1), 160; https://doi.org/10.3390/ijms24010160 - 21 Dec 2022

Viewed by 2033

Abstract

Bone is a frequent site of tumor metastasis. The bone–tumor microenvironment is heterogeneous and complex in nature. Such complexity is compounded by relations between metastatic and bone cells influencing their sensitivity/resistance to chemotherapeutics. Standard chemotherapeutics may not show efficacy for every patient, and new therapeutics are slow to emerge, owing to the limitations of existing 2D/3D models. We previously developed a 3D interface model for personalized therapeutic screening, consisting of an electrospun poly lactic acid mesh activated with plasma species and seeded with stromal cells. Tumor cells embedded in an alginate-gelatin hydrogel are overlaid to create a physiologic 3D interface. Here, we applied our 3D model as a migration assay tool to verify the migratory behavior of different patient-derived bone metastasized cells. We assessed the impact of two different chemotherapeutics, Doxorubicin and Cisplatin, on migration of patient cells and their immortalized cell line counterparts. We observed different migratory behaviors and cellular metabolic activities blocked with both Doxorubicin and Cisplatin treatment; however, higher efficiency or lower IC50 was observed with Doxorubicin. Gene expression analysis of MDA-MB231 that migrated through our 3D hybrid model verified epithelial–mesenchymal transition through increased expression of mesenchymal markers involved in the metastasis process. Our findings indicate that we can model tumor migration in vivo, in line with different cell characteristics and it may be a suitable drug screening tool for personalized medicine approaches in metastatic cancer treatment. Full article

(This article belongs to the Special Issue Quo Vadis Cancer Research? On Molecular Mechanisms and Drug Discovery 2.0)

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