Bioactive Molecules for Targeted Cancer Therapy and Delivery Innovations

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Biologics and Biosimilars".

Deadline for manuscript submissions: 31 December 2025 | Viewed by 795

Special Issue Editors


E-Mail Website
Guest Editor
Departamento de Química Orgánica, Facultad de Química y de Farmacia, Pontificia Universidad Católica de Chile, Santiago 702843, Chile
Interests: targeted therapy; tyrosine kinase inhibitors; anti-cancer drugs; drug design; bioactive heterocycles
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
Departamento de Ciencias y Tecnología Farmacéuticas, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Santiago 8380000, Chile
Interests: nanomedicine; micromedicines; anticancer therapies; drug delivery; nutraceutical formulations

Special Issue Information

Dear Colleagues,

Cancer remains one of the main causes of mortality worldwide, and offering new, more effective, and safer therapeutic alternatives is a major challenge for the scientific community and pharmaceutical industry. Targeted therapy has allowed the development of new drugs for the treatment of some types of cancer based on the blockade of specific molecular targets such as monoclonal antibodies for aberrant growth factor receptors or inhibitors for overexpressed or mutated enzymes related to carcinogenesis and/or tumor growth. However, these treatments also result in a loss of clinical efficacy owing to various resistance mechanisms. Therefore, a permanent search for new bioactive molecules to overcome these limitations is necessary. On the other hand, innovations in drug delivery are crucial due to the suboptimal physicochemical properties of both traditional and novel anticancer drugs. Furthermore, the specific targeting of anticancer drugs to tumor tissues is essential for enhancing both safety and efficacy. This can be further optimized using specialized drug delivery systems. Consequently, the continuous search for new drug delivery systems remains an ongoing necessity.

Pharmaceutics invites both original articles and reviews that shed light on the challenges and opportunities of new bioactive molecules and innovations on drug delivery as part of strategies for targeted cancer therapy. Topics include design, synthesis, in vitro and in vivo studies of drugs and drug delivery systems. The collection of manuscripts will be published as a Special Issue of the journal.

Dr. Cristian O. Salas
Dr. Felipe Andrés Oyarzún-Ampuero
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 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.

Keywords

  • bioactive molecules
  • targeted therapy
  • angiogenesis inhibitors
  • signal transduction inhibitors
  • nano and micromedicines
  • drug delivery
  • spatial and temporal drug release

Benefits of Publishing in a Special Issue

  • Ease of navigation: Grouping papers by topic helps scholars navigate broad scope journals more efficiently.
  • Greater discoverability: Special Issues support the reach and impact of scientific research. Articles in Special Issues are more discoverable and cited more frequently.
  • Expansion of research network: Special Issues facilitate connections among authors, fostering scientific collaborations.
  • External promotion: Articles in Special Issues are often promoted through the journal's social media, increasing their visibility.
  • Reprint: MDPI Books provides the opportunity to republish successful Special Issues in book format, both online and in print.

Further information on MDPI's Special Issue policies can be found here.

Published Papers (1 paper)

Order results
Result details
Select all
Export citation of selected articles as:

Research

31 pages, 5167 KiB  
Article
Targeting Neuronal Nitric Oxide Synthase (nNOS) as a Novel Approach to Enhancing the Anti-Melanoma Activity of Immune Checkpoint Inhibitors
by Anika Patel, Shirley Tong, Kate Lozada, Amardeep Awasthi, Richard B. Silverman, Jennifer Totonchy and Sun Yang
Pharmaceutics 2025, 17(6), 691; https://doi.org/10.3390/pharmaceutics17060691 - 24 May 2025
Viewed by 154
Abstract
Background and Objectives: Neuronal nitric oxide synthase (nNOS) overexpressed in melanoma plays a critical role in disease progression. Our previous studies demonstrated that nNOS inhibitors exhibited potent anti-melanoma activity and regulated PD-L1 expressions in the presence of interferon-gamma (IFN-γ). However, the role [...] Read more.
Background and Objectives: Neuronal nitric oxide synthase (nNOS) overexpressed in melanoma plays a critical role in disease progression. Our previous studies demonstrated that nNOS inhibitors exhibited potent anti-melanoma activity and regulated PD-L1 expressions in the presence of interferon-gamma (IFN-γ). However, the role of nNOS in the melanoma immune response has not been well defined. Methods: Changes in gene expression profiles after nNOS inhibitor treatment were determined by transcriptomic analysis. A melanoma mouse model was used to determine the effects of nNOS inhibition on peripheral T cells and the in vivo anti-tumor activity of combining nNOS inhibitors with immune checkpoint blockade. Changes in human T cell activation through interleukin-2 (IL-2) production were investigated using an ex vivo co-culture system with human melanoma cells. Results: Cellular RNA analysis revealed significant changes in the genes involved in key signaling pathways after nNOS inhibitor HH044 treatment. Immunophenotyping of mouse peripheral blood mononuclear cells (PBMCs) after prolonged HH044 treatment showed marked increases in CD4+ and CD8+PD-1+ T cells. Ex vivo studies demonstrated that co-culturing human PBMCs with melanoma cells inhibited T cell activation, decreasing IL-2-secreting T cells both in the presence and absence of IFN-γ. PBMCs from a significant portion of donors (7/11, 64%), however, were reactivated by nNOS inhibitor pretreatment, displaying a significant increase in IL-2+ T cells. Distinctive T cell characteristics were noted at baseline among the responders with increased CD4+RORγt+ and reduced CD4 naïve T cells. In vivo mouse studies demonstrated that nNOS inhibitors, when combined with PD-1 blockade, significantly reduced tumor growth more effectively than monotherapy. Additionally, the median survival was extended from 43 days in the control mice to 176.5 days in mice co-treated with HH044 and anti-PD-1. Conclusions: Targeting nNOS is a promising approach to enhancing the anti-melanoma activity of immune checkpoint inhibitors, not only interfering with melanoma biological activities but also regulating the tumor microenvironment, which subsequently affects T cell activation and tumor immune response. Full article
Show Figures

Figure 1

Back to TopTop