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Molecular Targets of Anticancer Therapy
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Molecular Targets of Anticancer Therapy

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 (28 February 2023) | Viewed by 8091

Special Issue Editor

Dr. Marian Hajduch

E-Mail Website
Guest Editor
Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry, Palacky University Olomouc, Hnevotinska 1333/5, 77900 Olomouc, Czech Republic
Interests: translational medicine; molecular oncology; cancer biomarkers; targeted drugs

Special Issue Information

Dear Colleagues,

The identification and validation of molecular targets of anticancer therapy play a key role in advancing personalized oncology. Cancer cells are known to bear specific, mostly somatic mutations and gene alterations, providing a growth advantage and driving the carcinogenesis process. However, this makes them potentially vulnerable to targeted therapies. Because the human genome has been sequenced and genetic technology has advanced, there is a growing body of knowledge on cancer’s genetic changes, initiation and proliferation, therapeutic mechanisms, and novel treatment targets. Understanding the pathophysiology of the disease, human gene sequence, the discovery of novel molecular targets, and designing targeted therapies represent the core of modern medicine to conquer cancer. This Special Issue welcomes relevant scientific contributions in the field of the identification and validation of molecular targets, development of targeted therapies, theranostics, drug repurposing, immuno-oncology, and other related areas. 

Dr. Marian Hajduch
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 target
  • small molecules
  • theranostics
  • personalized medicine
  • drug repurposing
  • immuno-oncology
  • cancer

Published Papers (2 papers)

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Research

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24 pages, 3742 KiB  
Article
Carborane-Containing Hydroxamate MMP Ligands for the Treatment of Tumors Using Boron Neutron Capture Therapy (BNCT): Efficacy without Tumor Cell Entry
by Sebastian Flieger, Mao Takagaki, Natsuko Kondo, Marlon R. Lutz, Jr., Yash Gupta, Hiroki Ueda, Yoshinori Sakurai, Graham Moran, Prakasha Kempaiah, Narayan Hosmane, Minoru Suzuki and Daniel P. Becker
Int. J. Mol. Sci. 2023, 24(8), 6973; https://doi.org/10.3390/ijms24086973 - 09 Apr 2023
Cited by 2 | Viewed by 2126
Abstract
New carborane-bearing hydroxamate matrix metalloproteinase (MMP) ligands have been synthesized for boron neutron capture therapy (BNCT) with nanomolar potency against MMP-2, -9 and -13. New analogs are based on MMP inhibitor CGS-23023A, and two previously reported MMP ligands 1 (B1) and [...] Read more.
New carborane-bearing hydroxamate matrix metalloproteinase (MMP) ligands have been synthesized for boron neutron capture therapy (BNCT) with nanomolar potency against MMP-2, -9 and -13. New analogs are based on MMP inhibitor CGS-23023A, and two previously reported MMP ligands 1 (B1) and 2 (B2) were studied in vitro for BNCT activity. The boronated MMP ligands 1 and 2 showed high in vitro tumoricidal effects in an in vitro BNCT assay, exhibiting IC50 values for 1 and 2 of 2.04 × 10−2 mg/mL and 2.67 × 10−2 mg/mL, respectively. The relative killing effect of 1 to L-boronophenylalanine (BPA) is 0.82/0.27 = 3.0, and that of 2 is 0.82/0.32 = 2.6, whereas the relative killing effect of 4 is comparable to boronophenylalanine (BPA). The survival fraction of 1 and 2 in a pre-incubation boron concentration at 0.143 ppm 10B and 0.101 ppm 10B, respectively, were similar, and these results suggest that 1 and 2 are actively accumulated through attachment to the Squamous cell carcinoma (SCC)VII cells. Compounds 1 and 2 very effectively killed glioma U87 delta EGFR cells after BNCT. This study is noteworthy in demonstrating BNCT efficacy through binding to MMP enzymes overexpressed at the surface of the tumor cell without tumor cell penetration. Full article
(This article belongs to the Special Issue Molecular Targets of Anticancer Therapy)
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Review

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19 pages, 789 KiB  
Review
Acquired Resistance to Osimertinib in EGFR-Mutated Non-Small Cell Lung Cancer: How Do We Overcome It?
by Elisa Bertoli, Elisa De Carlo, Alessandro Del Conte, Brigida Stanzione, Alberto Revelant, Kelly Fassetta, Michele Spina and Alessandra Bearz
Int. J. Mol. Sci. 2022, 23(13), 6936; https://doi.org/10.3390/ijms23136936 - 22 Jun 2022
Cited by 8 | Viewed by 5540
Abstract
Osimertinib is currently the preferred first-line therapy in patients with non-small cell lung cancer (NSCLC) with common epidermal growth factor receptor (EGFR) mutation and the standard second-line therapy in T790M-positive patients in progression to previous EGFR tyrosine kinase inhibitor. Osimertinib is [...] Read more.
Osimertinib is currently the preferred first-line therapy in patients with non-small cell lung cancer (NSCLC) with common epidermal growth factor receptor (EGFR) mutation and the standard second-line therapy in T790M-positive patients in progression to previous EGFR tyrosine kinase inhibitor. Osimertinib is a highly effective treatment that shows a high response rate and long-lasting disease control. However, a resistance to the treatment inevitably develops among patients. Understanding the secondary mechanisms of resistance and the possible therapeutic options available is crucial to define the best management of patients in progression to osimertinib. We provide a comprehensive review of the emerging molecular resistance mechanism in EGFR-mutated NSCLC pre-treated with osimertinib and its future treatment applications. Full article
(This article belongs to the Special Issue Molecular Targets of Anticancer Therapy)
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