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Pharmaceutics
Special Issues
Recent Advances in Inhibitors for Targeted Therapies
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Recent Advances in Inhibitors for Targeted Therapies

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

Deadline for manuscript submissions: 31 May 2025 | Viewed by 2389

Special Issue Editor

Dr. Anke Wilhelm

E-Mail Website
Guest Editor
Faculty of Natural and Agricultural Sciences, University of the Free State, Bloemfontein, South Africa
Interests: zebrafish research; phytochemistry; organic synthesis (up-scaling); cosmetic chemistry; nanomaterials

Special Issue Information

Dear Colleagues,

Recent advancements in inhibitors for targeted therapies represent a significant breakthrough in cancer treatment, offering renewed hope for patients with challenging tumors. Targeted therapies aim to disrupt specific molecular pathways that promote cancer cell growth, thereby minimizing harm to healthy cells and resulting in fewer side effects compared to traditional chemotherapy.

Key developments have focused on novel small-molecule inhibitors, monoclonal antibodies, and immune checkpoint inhibitors. Notably, enhancements in kinase inhibitors have improved the precision of targeting specific mutations, particularly in genes like BRAF and EGFR. Clinical trials indicate that these targeted inhibitors lead to better patient outcomes.

To maximize treatment effectiveness, it is essential to refine the characteristics of patient groups, develop personalized treatment plans, and adjust drug formulations and dosages as needed.

Additionally, the rise in combination therapies—utilizing multiple inhibitors simultaneously—has shown promise in overcoming resistance mechanisms that often limit the efficacy of single-agent treatments. This approach not only promotes tumor regression but also prolongs remission periods. Integrating antiviral therapies with other treatment modalities, such as vaccines and immunotherapy, is also crucial for maximizing therapeutic effectiveness.

In conclusion, the rapid progress in inhibitors for targeted therapies is transforming cancer treatment, offering more effective and personalized options while enhancing overall survival rates. This Special Issue invites submissions on a variety of topics, including, but not limited to, drug R&D dynamics, broad-spectrum antiviral strategies, emerging technologies, personalized medicine, synthesis and formulation optimization, and combination treatment strategies.

Dr. Anke Wilhelm
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. 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

  • targeted therapy
  • emerging technologies
  • antiviral strategies
  • inhibitor development
  • molecular targets
  • precision medicine
  • drug R&D dynamics
  • pharmaceutics
  • drug resistance

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Published Papers (4 papers)

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13 pages, 2007 KiB  
Article
Membrane-Mediated Action of Phosphodiesterase 5 Inhibitors
by Anna I. Malykhina, Svetlana S. Efimova and Olga S. Ostroumova
Pharmaceutics 2025, 17(5), 563; https://doi.org/10.3390/pharmaceutics17050563 - 24 Apr 2025
Viewed by 245
Abstract
Background/Objectives: Phosphodiesterase 5 (PDE5) inhibitors, sildenafil, vardenafil, and tadalafil, activate the cyclic guanosine monophosphate pathway resulting in vascular smooth muscle relaxation. They have been tested for a broad variety of conditions from cancer to Alzheimer’s disease with a positive impact. The known [...] Read more.
Background/Objectives: Phosphodiesterase 5 (PDE5) inhibitors, sildenafil, vardenafil, and tadalafil, activate the cyclic guanosine monophosphate pathway resulting in vascular smooth muscle relaxation. They have been tested for a broad variety of conditions from cancer to Alzheimer’s disease with a positive impact. The known mechanism of action of these drugs could not explain such a plethora of effects. We studied the influence of PDE5 inhibitors on lipid bilayers as a possible application point of their action. Methods: To monitor the membrane changes induced by PDE5 inhibitors, the differential scanning microcalorimetry and the molecular dynamics simulation were used. Results: We found that sildenafil, vardenafil, and tadalafil change elastic properties of model membranes: PDE5 inhibitors disorder thin membranes and order thick membranes. Moreover, PDE inhibitors were able to induce lipid interdigitation. To address the biological aspect of the findings, we performed molecular dynamics on smooth muscle cell’s lipid raft treated with PDE5 inhibitors and revealed the increased density of the lipids. Furthermore, we showed that the lipid condensation in the PDE inhibitors presence increases nitric oxide permeability. Conclusions: The obtained results may be of biological relevance as lipid raft thickening might have an impact on membrane protein function. Moreover, improved nitric oxide flow through membrane may partially explain therapeutic action of these drugs. The presented results are useful for finding novel implications for PDE inhibitors. Full article
(This article belongs to the Special Issue Recent Advances in Inhibitors for Targeted Therapies)
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17 pages, 9778 KiB  
Article
A Convenient Strategy for Studying Antibody Aggregation and Inhibition of Aggregation: Characterization and Simulation
by Yibo Guo, Xi Chen, Guchen Fang, Xuejun Cao and Junfen Wan
Pharmaceutics 2025, 17(4), 534; https://doi.org/10.3390/pharmaceutics17040534 - 19 Apr 2025
Viewed by 258
Abstract
Background/Objectives: Protein aggregation, particularly the aggregation of antibody-based drugs, has long been a significant challenge in downstream processes and formulation. While the inhibitory effects of excipients on aggregation have been extensively studied using early experimental characterization methods, complete formulation research requires significant amounts [...] Read more.
Background/Objectives: Protein aggregation, particularly the aggregation of antibody-based drugs, has long been a significant challenge in downstream processes and formulation. While the inhibitory effects of excipients on aggregation have been extensively studied using early experimental characterization methods, complete formulation research requires significant amounts of antibodies and time, resulting in high research costs. Methods: This study proposed a quick and small-scale position-restrained simulation method which elucidated the mechanism of the reversible self-association (RSA) of antibodies and the influence of excipients on RSA under different conditions. We also validated the rationality of rapid and small-scale simulations through long-term (>1 μs) and large-scale (>1,000,000 atoms) simulations. Results: Through combing with simple stability characterization, the effects of different excipients on monomer residual content and the trend shown with concentration changes after thermal incubation were found to be similar to those observed in the simulations. Additionally, the formulation proposed by the simulations was validated using experimental characterization. Conclusions: Simulations and experiments revealed the mechanism and showed consistent trends, providing better understanding for aggregation research. Full article
(This article belongs to the Special Issue Recent Advances in Inhibitors for Targeted Therapies)
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16 pages, 2646 KiB  
Article
AChE Inhibition Capability of Nanogels Derived from Natural Molecules: Tannic Acid and Lysine for Alzheimer’s Disease
by Mehtap Sahiner, Selin S. Suner and Nurettin Sahiner
Pharmaceutics 2025, 17(4), 502; https://doi.org/10.3390/pharmaceutics17040502 - 10 Apr 2025
Viewed by 393
Abstract
Background/Objectives: Tannic acid (TA), a known natural polyphenolic acid with many bioactivities including antioxidants, antibacterial, and antiviral, can be combined with a natural essential amino acid L-lysine (LYS) in nanogel formulations to produce p(TA-co-LYS) (p(TA-co-LYS)) nanogels. Methods: A 1:1 mole ratio of [...] Read more.
Background/Objectives: Tannic acid (TA), a known natural polyphenolic acid with many bioactivities including antioxidants, antibacterial, and antiviral, can be combined with a natural essential amino acid L-lysine (LYS) in nanogel formulations to produce p(TA-co-LYS) (p(TA-co-LYS)) nanogels. Methods: A 1:1 mole ratio of TA:LYS was used to prepare corresponding spherical nanogels employing formaldehyde as a linker via the Mannich reaction. Results: The attained p(TA-co-LYS) particles were in 283 ± 57 nm size ranges (via SEM analysis) and possessed smooth surfaces. The zeta potential measurements of p(TA-co-LYS) nanogels suspension at different solution pHs revealed the isoelectric point (IEP) of pH 4.9, suggesting that the particles are negatively charged at the physiological pH range (e.g., at 7.4). In addition to the antioxidant efficacy of nanogels confirmed by three different tests, p(TA-co-LYS) particles showed significant Fe(II) ion chelating capacity at 350 µg/mL concentrations compared to bare TA, which is 21%, whereas the LYS molecule had a chelating capacity of 100% at the same concentrations. Moreover, it was found that p(TA-co-LYS) nanogels inhibited the Acetylcholinesterase enzyme (AChE) at a concentration-dependent profile, e.g., at 333 µg/mL concentration of p(TA-co-LYS), 57.2% of the enzyme AChE activity was inhibited. Furthermore, the minimum inhibition concentrations of p(TA-co-LYS) nanogels of Gram-negative Escherichia coli (ATCC 8739) and Gram-positive Staphylococcus aureus (ATCC 6538) were determined as 12.5 mg/mL. Conclusions: As cytotoxicity studies of p(TA-co-LYS) nanogels on L929 fibroblast cells also ascertained that these particles can be safely used in many biomedical applications, including antioxidant materials, drug delivery devices, and enzyme inhibitors. Full article
(This article belongs to the Special Issue Recent Advances in Inhibitors for Targeted Therapies)
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19 pages, 4074 KiB  
Article
New and Effective Inhibitor of Class I HDACs, Eimbinostat, Reduces the Growth of Hematologic Cancer Cells and Triggers Apoptosis
by Pavel Spirin, Valeria Vedernikova, Tatsiana Volkava, Alexey Morozov, Alla Kleymenova, Anastasia Zemskaya, Lena Shyrokova, Yuri Porozov, Ksenia Glumakova, Timofey Lebedev, Maxim Kozlov and Vladimir Prassolov
Pharmaceutics 2025, 17(4), 416; https://doi.org/10.3390/pharmaceutics17040416 - 25 Mar 2025
Viewed by 458
Abstract
Background: Histone deacetylases (HDACs) are critical epigenetic modulators involved in regulating various molecular mechanisms essential for cell development and growth. Alterations in HDAC activity have been linked to the progression of numerous cancers, including lymphoma. Over the past decade, the FDA has approved [...] Read more.
Background: Histone deacetylases (HDACs) are critical epigenetic modulators involved in regulating various molecular mechanisms essential for cell development and growth. Alterations in HDAC activity have been linked to the progression of numerous cancers, including lymphoma. Over the past decade, the FDA has approved several HDAC inhibitors for lymphoma treatment, leading to heightened interest in this emerging class of drugs. Methods: In our research, we developed a novel HDAC inhibitor that exhibits high selectivity for class I HDACs. Results: Our in vitro findings indicate that treating lymphoma/leukemia cells with this inhibitor results in a marked suppression of cell growth and promotes apoptosis, while leaving the cell cycle unaffected. Conclusions: We propose that our new inhibitor, named eimbinostat, holds significant promise as a potential therapeutic agent for the treatment of hematologic malignancies such as lymphoma or leukemia. Full article
(This article belongs to the Special Issue Recent Advances in Inhibitors for Targeted Therapies)
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