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Pharmaceutics
Special Issues
Inhibitors in the Treatment of Cancer and Neurodegenerative Disorders
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Special Issue "Inhibitors in the Treatment of Cancer and Neurodegenerative Disorders"

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Targeting and Design".

Deadline for manuscript submissions: 30 June 2023 | Viewed by 590

Special Issue Editors

Prof. Dr. Katarina Nikolic

E-Mail Website
Guest Editor
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, Belgrade, Serbia
Interests: drug design; medicinal chemistry; epigenetic inhibitors; multitarget ligands
Prof. Dr. Biljana Bufan
E-Mail Website
Guest Editor
Department of Microbiology and Immunology, Faculty of Pharmacy, University of Belgrade, Belgrade, Serbia
Interests: immunomodulation; pathogenic mechanisms of autoimmune diseases
Dr. Dusan Ruzic

E-Mail Website
Guest Editor
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, Belgrade, Serbia
Interests: medicinal chemistry; drug design; epigenetic inhibitors

Special Issue Information

Dear Colleagues,

Molecular mechanisms that underpin the onset and progression of malignant and neurodegenerative diseases seem to have little in common. Some epidemiological studies add weight to the inverse association between certain types of cancer and neurodegenerative diseases. However, there is no clear consensus on this connotation. Cancer cells escape cell death signals whereas aberrant activation of neuronal cell death is a common hallmark in neurodegenerative diseases. Numerous studies suggest common genetic and epigenetic factors that are implicated in cancer and neurodegeneration. Some of these include p53, ATM gene, Cyclin-dependent kinase 5 (CDK5), glycogen synthase kinase-3 (GSK3), histone deacetylase 2 (HDAC2), Brain-derived Neurotrophic Factor (BDNF), changes in microRNA (miRNA) expression and many more.

To improve our understanding of the crosstalk between cancer and neurodegeneration, this Special Issue aims to discuss the novel therapeutic agents able to target aberrant molecular mechanisms common in cancer and neurodegenerative diseases.

In this Special Issue, original research articles and reviews are welcome. Research areas may include (but are not limited to) the following:

  • Identification of prognostic markers for cancer and neurodegeneration
  • Identification of novel drug targets and signaling molecules
  • Repurposing of drug treatments for cancer and neurodegeneration
  • Drug design of novel compounds targeting cancer and neurodegeneration

We look forward to receiving your contributions.

Prof. Dr. Katarina Nikolic
Prof. Dr. Biljana Bufan
Dr. Dusan Ruzic
Guest Editors

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. Pharmaceutics 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 2600 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

  • drug design
  • cancer
  • neurodegeneration
  • repurposing
  • parkinson disease
  • multiple sclerosis
  • novel small-molecule inhibitors
  • kinases
  • epigenetics
  • aging

Published Papers (1 paper)

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Article
A Novel and Highly Selective Epidermal Growth Factor Receptor Inhibitor, SMUZ106, for the Treatment of Glioblastoma
by
Ying Jiang
,
Chunhui Huang
,
Yaqi Huang
,
Lifan Long
,
Guowu Wu
,
Fengqiu Guo
,
Chuan Huang
,
Siming Liu
,
Zhengguang Zhu
,
Shaoyu Wu
,
Zhonghuang Li
,
Jiajie Zhang
and
Shanhe Wan
Pharmaceutics 2023, 15(5), 1501; https://doi.org/10.3390/pharmaceutics15051501 - 15 May 2023
Viewed by 404
Abstract
Targeting the epidermal growth factor receptor (EGFR) is one of the potential ways to treat glioblastoma (GBM). In this study, we investigate the anti-GBM tumor effects of the EGFR inhibitor SMUZ106 in both in vitro and in vivo conditions. The effects of SMUZ106 [...] Read more.
Targeting the epidermal growth factor receptor (EGFR) is one of the potential ways to treat glioblastoma (GBM). In this study, we investigate the anti-GBM tumor effects of the EGFR inhibitor SMUZ106 in both in vitro and in vivo conditions. The effects of SMUZ106 on the growth and proliferation of GBM cells were explored through MTT and clone formation experiments. Additionally, flow cytometry experiments were conducted to study the effects of SMUZ106 on the cell cycle and apoptosis of GBM cells. The inhibitory activity and selectivity of SMUZ106 to the EGFR protein were proved by Western blotting, molecular docking, and kinase spectrum screening methods. We also conducted a pharmacokinetic analysis of SMUZ106 hydrochloride following i.v. or p.o. administration to mice and assessed the acute toxicity level of SMUZ106 hydrochloride following p.o. administration to mice. Subcutaneous and orthotopic xenograft models of U87MG-EGFRvIII cells were established to assess the antitumor activity of SMUZ106 hydrochloride in vivo. SMUZ106 could inhibit the growth and proliferation of GBM cells, especially for the U87MG-EGFRvIII cells with a mean IC50 value of 4.36 μM. Western blotting analyses showed that compound SMUZ106 inhibits the level of EGFR phosphorylation in GBM cells. It was also shown that SMUZ106 targets EGFR and presents high selectivity. In vivo, the absolute bioavailability of SMUZ106 hydrochloride was 51.97%, and its LD50 exceeded 5000 mg/kg. SMUZ106 hydrochloride significantly inhibited GBM growth in vivo. Furthermore, SMUZ106 inhibited the activity of U87MG-resistant cells induced by temozolomide (TMZ) (IC50: 7.86 μM). These results suggest that SMUZ106 hydrochloride has the potential to be used as a treatment method for GBM as an EGFR inhibitor. Full article
(This article belongs to the Special Issue Inhibitors in the Treatment of Cancer and Neurodegenerative Disorders)
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