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Pharmaceutics
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Peptide-Drug Conjugates for Targeted Anti-Cancer Therapy: From Design to Application
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Peptide-Drug Conjugates for Targeted Anti-Cancer Therapy: From Design to Application

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

Deadline for manuscript submissions: closed (20 February 2023) | Viewed by 16694

Special Issue Editor

Prof. Dr. Jooho Park

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Guest Editor
1. Department of Applied Life Science and Integrated Bioscience, Graduate School, BK21 Program, Konkuk University, Chungju 27478, Korea
2. Department of Integrated Bioscience & Biotechnology, College of Biomedical and Health Science, Research Institute of Inflammatory Disease (RID), Konkuk University, Chungju 27478, Korea
Interests: nanomedicine; prodrug; targeted drug delivery' molecular dynamics; self-assembly; computer simulation; oral drug delivery

Special Issue Information

Dear Colleagues,

Despite advances in medical technology, cancer is still among the leading causes of death globally. Chemotherapy is currently used as a clinical strategy to treat malignant tumors; however, its therapeutic efficacy is highly limited due to non-specific systemic toxicity and a narrow therapeutic window. Advances in drug design and development have led to the emergence of new tumor-targeted therapy using target-specific antibodies or biomolecules. Therefore, with such a concept, various effective biomolecules and conjugates are being developed and studied. In particular, newly designed peptide and drug conjugates using cytotoxic drugs, polymers or proteins have shown outstanding promise in recent decades, showing improved therapeutic efficacy.

Peptide-based biomolecules are generally well recognized or degraded by the target protein, making it easy to modify or design the targeting function. Combined with prodrugs, antibody–drug conjugates (ADCs) or nanomedicine, various peptide-based therapeutics are being studied for clinical applications. Newly developed peptide–drug conjugates could represent a promising therapeutic treatment for patients.

Topics of interest to this Special Issue include various peptide–drug conjugates for targeted therapy, new drug delivery systems, prodrug design, anti-cancer therapy and related concepts. Original research and review papers are welcome.

I look forward to receiving your contributions.

Prof. Dr. Jooho Park
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

  • bioconjugate
  • peptide
  • prodrug
  • drug delivery systems
  • targeted therapy
  • nanomedicine
  • cancer treatment
  • advanced biomolecules
  • antibody–drug conjugate

Published Papers (5 papers)

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Research

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13 pages, 3037 KiB  
Article
Development of a Peptide-Based Nano-Sized Cathepsin B Inhibitor for Anticancer Therapy
by So-Hyeon Park, Jun-Hyuck Lee, Seong-Bin Yang, Dong-Nyeong Lee, Tae-Bong Kang and Jooho Park
Pharmaceutics 2023, 15(4), 1131; https://doi.org/10.3390/pharmaceutics15041131 - 3 Apr 2023
Cited by 3 | Viewed by 2331
Abstract
Numerous cathepsin B inhibitors have been developed and are under investigation as potential cancer treatments. They have been evaluated for their ability to inhibit cathepsin B activity and reduce tumor growth. However, they have shown critical limitations, including low anticancer efficacy and high [...] Read more.
Numerous cathepsin B inhibitors have been developed and are under investigation as potential cancer treatments. They have been evaluated for their ability to inhibit cathepsin B activity and reduce tumor growth. However, they have shown critical limitations, including low anticancer efficacy and high toxicity, due to their low selectivity and delivery problems. In this study, we developed a novel peptide and drug conjugate (PDC)-based cathepsin B inhibitor using cathepsin-B-specific peptide (RR) and bile acid (BA). Interestingly, this RR and BA conjugate (RR–BA) was able to self-assemble in an aqueous solution, and as a result, it formed stable nanoparticles. The nano-sized RR–BA conjugate showed significant cathepsin B inhibitory effects and anticancer effects against mouse colorectal cancer (CT26) cells. Its therapeutic effect and low toxicity were also confirmed in CT26 tumor-bearing mice after intravenous injection. Therefore, based on these results, the RR–BA conjugate could be developed as an effective anticancer drug candidate for inhibiting cathepsin B in anticancer therapy. Full article
(This article belongs to the Special Issue Peptide-Drug Conjugates for Targeted Anti-Cancer Therapy: From Design to Application)
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15 pages, 1603 KiB  
Article
Prognostic and Predictive Value of LIV1 Expression in Early Breast Cancer and by Molecular Subtype
by Alexandre de Nonneville, Pascal Finetti, Laurys Boudin, Emilie Denicolaï, Daniel Birnbaum, Emilie Mamessier and François Bertucci
Pharmaceutics 2023, 15(3), 938; https://doi.org/10.3390/pharmaceutics15030938 - 14 Mar 2023
Cited by 2 | Viewed by 2295
Abstract
Background: LIV1 is a transmembrane protein that may become a new therapeutic target through the development of antibody–drug conjugates (ADCs). Few studies are available regarding the assessment of LIV1 expression in clinical breast cancer (BC) samples. Methods: We analyzed LIV1 mRNA expression in [...] Read more.
Background: LIV1 is a transmembrane protein that may become a new therapeutic target through the development of antibody–drug conjugates (ADCs). Few studies are available regarding the assessment of LIV1 expression in clinical breast cancer (BC) samples. Methods: We analyzed LIV1 mRNA expression in 8982 primary BC. We searched for correlations between LIV1 expression and clinicopathological data, including disease-free survival (DFS), overall survival (OS), pathological complete response to chemotherapy (pCR), and potential vulnerability and actionability to anti-cancer drugs used or under development in BC. Analyses were performed in the whole population and each molecular subtype separately. Results: LIV1 expression was associated with good-prognosis features and with longer DFS and OS in multivariate analysis. However, patients with high LIV1 expression displayed a lower pCR rate than patients with low expression after anthracycline-based neoadjuvant chemotherapy, including in multivariate analysis adjusted on grade and molecular subtypes. LIV1-high tumors were associated with higher probabilities of sensitivity to hormone therapy and CDK4/6 inhibitors and lower probabilities of sensitivity to immune-checkpoint inhibitors and PARP inhibitors. These observations were different according to the molecular subtypes when analyzed separately. Conclusions: These results may provide novel insights into the clinical development and use of LIV1-targeted ADCs by identifying prognostic and predictive value of LIV1 expression in each molecular subtype and associated vulnerability to other systemic therapies. Full article
(This article belongs to the Special Issue Peptide-Drug Conjugates for Targeted Anti-Cancer Therapy: From Design to Application)
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15 pages, 3259 KiB  
Article
Experimental HER2-Targeted Therapy Using ADAPT6-ABD-mcDM1 in Mice Bearing SKOV3 Ovarian Cancer Xenografts: Efficacy and Selection of Companion Imaging Counterpart
by Javad Garousi, Tianqi Xu, Yongsheng Liu, Olga Vorontsova, Sophia Hober, Anna Orlova, Vladimir Tolmachev, Torbjörn Gräslund and Anzhelika Vorobyeva
Pharmaceutics 2022, 14(8), 1612; https://doi.org/10.3390/pharmaceutics14081612 - 2 Aug 2022
Cited by 1 | Viewed by 2621
Abstract
Overexpression of the human epidermal growth factor receptor 2 (HER2) in breast and gastric cancer is exploited for targeted therapy using monoclonal antibodies and antibody-drug conjugates. Small engineered scaffold proteins, such as the albumin binding domain (ABD) derived affinity proteins (ADAPTs), are a [...] Read more.
Overexpression of the human epidermal growth factor receptor 2 (HER2) in breast and gastric cancer is exploited for targeted therapy using monoclonal antibodies and antibody-drug conjugates. Small engineered scaffold proteins, such as the albumin binding domain (ABD) derived affinity proteins (ADAPTs), are a promising new format of targeting probes for development of drug conjugates with well-defined structure and tunable pharmacokinetics. Radiolabeled ADAPT6 has shown excellent tumor-targeting properties in clinical trials. Recently, we developed a drug conjugate based on the HER2-targeting ADAPT6 fused to an albumin binding domain (ABD) for increased bioavailability and conjugated to DM1 for cytotoxic action, designated as ADAPT6-ABD-mcDM1. In this study, we investigated the therapeutic efficacy of this conjugate in mice bearing HER2-expressing SKOV3 ovarian cancer xenografts. A secondary aim was to evaluate several formats of imaging probes for visualization of HER2 expression in tumors. Administration of ADAPT6-ABD-mcDM1 provided a significant delay of tumor growth and increased the median survival of the mice, in comparison with both a non-targeting homologous construct (ADAPTNeg-ABD-mcDM1) and the vehicle-treated groups, without inducing toxicity to liver or kidneys. Moreover, the evaluation of imaging probes showed that small scaffold proteins, such as 99mTc(CO)3-ADAPT6 or the affibody molecule 99mTc-ZHER2:41071, are well suited as diagnostic companions for potential stratification of patients for ADAPT6-ABD-mcDM1–based therapy. Full article
(This article belongs to the Special Issue Peptide-Drug Conjugates for Targeted Anti-Cancer Therapy: From Design to Application)
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Review

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27 pages, 6776 KiB  
Review
Advances in Radionuclides and Radiolabelled Peptides for Cancer Therapeutics
by Kushal Chakraborty, Jagannath Mondal, Jeong Man An, Jooho Park and Yong-Kyu Lee
Pharmaceutics 2023, 15(3), 971; https://doi.org/10.3390/pharmaceutics15030971 - 17 Mar 2023
Cited by 6 | Viewed by 3980
Abstract
Radiopharmaceutical therapy, which can detect and treat tumours simultaneously, was introduced more than 80 years ago, and it has changed medical strategies with respect to cancer. Many radioactive radionuclides have been developed, and functional, molecularly modified radiolabelled peptides have been used to produce [...] Read more.
Radiopharmaceutical therapy, which can detect and treat tumours simultaneously, was introduced more than 80 years ago, and it has changed medical strategies with respect to cancer. Many radioactive radionuclides have been developed, and functional, molecularly modified radiolabelled peptides have been used to produce biomolecules and therapeutics that are vastly utilised in the field of radio medicine. Since the 1990s, they have smoothly transitioned into clinical application, and as of today, a wide variety of radiolabelled radionuclide derivatives have been examined and evaluated in various studies. Advanced technologies, such as conjugation of functional peptides or incorporation of radionuclides into chelating ligands, have been developed for advanced radiopharmaceutical cancer therapy. New radiolabelled conjugates for targeted radiotherapy have been designed to deliver radiation directly to cancer cells with improved specificity and minimal damage to the surrounding normal tissue. The development of new theragnostic radionuclides, which can be used for both imaging and therapy purposes, allows for more precise targeting and monitoring of the treatment response. The increased use of peptide receptor radionuclide therapy (PRRT) is also important in the targeting of specific receptors which are overexpressed in cancer cells. In this review, we provide insights into the development of radionuclides and functional radiolabelled peptides, give a brief background, and describe their transition into clinical application. Full article
(This article belongs to the Special Issue Peptide-Drug Conjugates for Targeted Anti-Cancer Therapy: From Design to Application)
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17 pages, 2082 KiB  
Review
Peptide-Based Bioconjugates and Therapeutics for Targeted Anticancer Therapy
by Seong-Bin Yang, Nipa Banik, Bomin Han, Dong-Nyeong Lee and Jooho Park
Pharmaceutics 2022, 14(7), 1378; https://doi.org/10.3390/pharmaceutics14071378 - 29 Jun 2022
Cited by 17 | Viewed by 4658
Abstract
With rapidly growing knowledge in bioinformatics related to peptides and proteins, amino acid-based drug-design strategies have recently gained importance in pharmaceutics. In the past, peptide-based biomedicines were not widely used due to the associated severe physiological problems, such as low selectivity and rapid [...] Read more.
With rapidly growing knowledge in bioinformatics related to peptides and proteins, amino acid-based drug-design strategies have recently gained importance in pharmaceutics. In the past, peptide-based biomedicines were not widely used due to the associated severe physiological problems, such as low selectivity and rapid degradation in biological systems. However, various interesting peptide-based therapeutics combined with drug-delivery systems have recently emerged. Many of these candidates have been developed for anticancer therapy that requires precisely targeted effects and low toxicity. These research trends have become more diverse and complex owing to nanomedicine and antibody–drug conjugates (ADC), showing excellent therapeutic efficacy. Various newly developed peptide–drug conjugates (PDC), peptide-based nanoparticles, and prodrugs could represent a promising therapeutic strategy for patients. In this review, we provide valuable insights into rational drug design and development for future pharmaceutics. Full article
(This article belongs to the Special Issue Peptide-Drug Conjugates for Targeted Anti-Cancer Therapy: From Design to Application)
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