Special Issue "Small Molecules in Targeted Cancer Therapy and Diagnosis"

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmacology".

Deadline for manuscript submissions: 26 January 2024 | Viewed by 686

Special Issue Editor

Department of Pharmacy, University of Genoa, Viale Benedetto XV, 3, 16132 Genoa, Italy
Interests: pyrazolo[3,4-d]pyrimidines; kinase inhibitors; anticancer agents; small molecules
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Cancer remains a significant global health challenge, necessitating innovative approaches to improve patient outcomes. In recent years, targeted cancer therapy and diagnosis has witnessed remarkable advancements driven by small molecules. These compounds offer promising avenues for precise cancer treatment and accurate disease detection, providing personalized and effective interventions. This Special Issue aims to highlight the latest developments in small molecule-based approaches for targeted cancer therapy and diagnosis and addresses the associated challenges. In particular, it will provide insights into the design, synthesis, and characterization of small molecules, including inhibitors, activators, modulators, and imaging agents. Emphasis will be placed on their mechanisms of action, molecular interactions, and potential for targeted cancer therapy and diagnosis.

Topics of interest may include, but are not limited to, the following:

  • Rational design and synthesis of small molecules targeting specific oncogenic targets, such as kinases, receptors, and transcription factors.
  • Small molecules as modulators of immune responses in cancer immunotherapy.
  • Application of small molecules in combination therapies to overcome drug resistance.
  • Strategies for targeted drug delivery utilizing small molecule conjugates or nanocarriers.
  • Computational modeling and virtual screening techniques for the design of small molecules with enhanced selectivity and potency.
  • Pharmacokinetic and pharmacodynamic considerations in small molecule-based cancer therapy and diagnosis.
  • Small molecule-based imaging agents for cancer diagnosis, including optical, radioactive, and magnetic resonance imaging (MRI) probes.
  • Development of theranostic agents in cancers.

This Special Issue aims to bring together researchers from diverse disciplines to present their cutting-edge research, share insights, and foster collaborations. The ultimate goal is to accelerate the translation of small molecule-based approaches into clinical applications, thereby improving the lives of cancer patients. We invite researchers to contribute their research articles or reviews to this Special Issue.

Dr. Francesca Musumeci
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. Pharmaceuticals 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 2900 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.


  • small molecules
  • cancer therapy
  • cancer diagnosis
  • targeted therapy
  • theranostic agents

Published Papers (1 paper)

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12 pages, 1046 KiB  
Entecavir: A Review and Considerations for Its Application in Oncology
Pharmaceuticals 2023, 16(11), 1603; https://doi.org/10.3390/ph16111603 - 14 Nov 2023
Viewed by 528
Entecavir (ETV) is a drug used as a first-line treatment for chronic hepatitis B (CHB) virus infection because it is a guanosine nucleoside analogue with activity against the hepatitis B virus polymerase. The ETV dosage can range from 0.5 mg to 1 mg [...] Read more.
Entecavir (ETV) is a drug used as a first-line treatment for chronic hepatitis B (CHB) virus infection because it is a guanosine nucleoside analogue with activity against the hepatitis B virus polymerase. The ETV dosage can range from 0.5 mg to 1 mg once a day and the most common side effects include headache, insomnia, fatigue, dizziness, somnolence, vomiting, diarrhea, nausea, dyspepsia, and increased liver enzyme levels. In addition to its conventional use, ETV acts as an inhibitor of lysine-specific demethylase 5B (KDM5B), an enzyme that is overexpressed in breast, lung, skin, liver, and prostate tumors and is involved in the hormonal response, stem cell regeneration, genomic stability, cell proliferation, and differentiation. The KDM5B enzyme acts as a transcriptional repressor in tumor suppressor genes, silencing them, and its overexpression leads to drug resistance in certain tumor types. Furthermore, the literature suggests that KDM5B activates the PI3K/AKT signaling pathway, while reducing KDM5B expression decreases AKT signaling, resulting in decreased tumor cell proliferation. In silico studies have demonstrated that ETV can inhibit tumor cell proliferation and induce apoptosis by reducing KDM5B expression. ETV also appears to inhibit PARP-1, has a high genetic barrier, reducing the chance of resistance development, and can also prevent the reactivation of the hepatitis B virus in cancer patients, which have proven to be significant advantages regarding its use as a repurposed drug in oncology. Therefore, ETV holds promise beyond its original therapeutic indication. Full article
(This article belongs to the Special Issue Small Molecules in Targeted Cancer Therapy and Diagnosis)
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