Review
Infectious Diseases
Gabriela Silva Cruz, Ariane Teixeira dos Santos, Erika Helena Salles de Brito, Gandhi Radis-Baptista
Summary: This review presents the antibacterial, antiparasitic, and antiviral effects of cell-penetrating antimicrobial peptides and highlights their potential for treating intracellular infections.
Article
Pharmacology & Pharmacy
Tamara Lutzenburg, Nele Burdina, Matthias S. Scholz, Ines Neundorf
Summary: Cell-penetrating peptides (CPPs) are used to increase the intracellular accumulation of cargoes by forming stable secondary structures at the outer surface of the plasma membrane. Incorporation of hydrophobic moieties like carboranes (CBs) can alter the lipophilicity of peptides and enhance secondary structure formation, leading to potential applications in nucleic acid delivery.
Article
Chemistry, Multidisciplinary
So Hee Nam, Joomyung Jang, Dae Hee Cheon, Seung-Eun Chong, Joon Hyung Ahn, Soonsil Hyun, Jaehoon Yu, Yan Lee
Summary: The designed pH-activatable cell-penetrating peptide dimer LH2 with histidine residues is able to penetrate cells specifically in weak acidic conditions, delivering paclitaxel effectively into triple-negative breast cancer cells. Both non-covalent complexes (PTX-LH2(M)) and covalent conjugates (PTX-LH2(C)) of LH2 show strong antitumor effects in a triple-negative breast cancer grafted mouse model at extremely low dosages, indicating potential for targeted drug delivery and therapy.
JOURNAL OF CONTROLLED RELEASE
(2021)
Article
Pharmacology & Pharmacy
Quim Pena, Sergi Rodriguez-Calado, A. Jalila Simaan, Merce Capdevila, Pau Bayon, Oscar Palacios, Julia Lorenzo, Olga Iranzo
Summary: The study investigates the application of copper-based metal compounds in cancer treatment, enhancing their anticancer activity by modifying their solubility and cellular uptake through functionalization. Results show that copper complexes conjugated with cell-penetrating peptides exhibit improved anticancer activity.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Keisuke Tsuchiya, Kanako Horikoshi, Minami Fujita, Motoharu Hirano, Maho Miyamoto, Hidetomo Yokoo, Yosuke Demizu
Summary: Researchers have developed hydrophobic CPPs based on the hydrophobic CPP TP10 by introducing an aliphatic carbon side chain. These stapled peptides maintained the hydrophobicity of TP10, enhanced helicity, and improved cell-penetrating efficiency. The stapled peptide F-3 with CF showed stable α-helical structure and highest cell-membrane permeability, while peptide F-4 exhibited remarkable stability in complex formation with pDNA for efficient intracellular delivery.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Multidisciplinary
Anselm F. L. Schneider, Marina Kithil, M. Cristina Cardoso, Martin Lehmann, Christian P. R. Hackenberger
Summary: The challenge of delivering proteins into cells has been addressed by conjugating arginine-rich cell-penetrating peptides to the cell surface, enabling efficient delivery of protein-CPP conjugates. The use of thiol-reactive cell-penetrating peptides allows for simple co-incubation to deliver thiol-containing proteins, greatly simplifying protein and antibody delivery with minimal genetic or chemical engineering.
Article
Medicine, Research & Experimental
Haruya Yagi, Takumi Tomono, Yuma Handa, Natsuki Saito, Masami Ukawa, Kohei Miyata, Koichi Shigeno, Shinji Sakuma
Summary: This study investigates the use of cell-penetrating peptides anchored to polymeric platforms as an absorption enhancer for delivering biologics via mucosal routes. Results show that hyaluronic acid modified with L-octaarginine significantly enhances the mucosal absorption of protein drugs in the nasal cavities. The lung mucosa and oral mucosa were found to be suitable routes for mucosal absorption of biologics.
MOLECULAR PHARMACEUTICS
(2023)
Article
Biochemistry & Molecular Biology
Yi-Fei Zhang, Yun-Feng Wu, Tai-Jin Lan, Yao Chen, Shi-Hong Su
Summary: This study investigated the effects of HPPH/EPI/CPP-pGO on tumor growth in osteosarcoma, showing superior inhibition both in vitro and in vivo. The combination of CPP modified and PEG-grafted GO loaded with photosensitive agent and Epirubicin exhibited strong antitumor effects, significantly inhibiting cell viability, colony formation, and inducing apoptosis compared to control groups. Additionally, the group treated with HPPH/EPI/CPP-pGO showed the most effective tumor growth inhibition among all tested groups.
FRONTIERS IN MOLECULAR BIOSCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Kamila Rzad, Ewa Paluszkiewicz, Damian Neubauer, Mateusz Olszewski, Katarzyna Kozlowska-Tylingo, Wojciech Kamysz, Iwona Gabriel
Summary: The synthesized compound showed high antifungal activity and only the conjugate was effective by entering the fungal cells and accumulating inside, possibly through altering the permeability of the fungal cell membrane to achieve killing activity. The conjugate exhibited promising results in antifungal activity with low cytotoxicity against human cell lines, indicating potential clinical applications.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Materials Science, Multidisciplinary
Yu-Fon Chen, Yao-Tsung Yeh, Yu-Chu Su, Chorng-An Liao, Cheng-Hsieh Huang, Ying-Jung Cheng, Jeng-Shiung Jan
Summary: This study investigated the anticancer activity of a cell adhesion inhibiting peptide comprised of L-lysine (Lys) and Benzyl-L-cysteine (BnCys) and its impact on intestinal microbiota. The peptide inhibits cell migration and adhesion by interfering with E-cadherin packaging and disrupting cell membrane integrity, leading to apoptotic pathways activation. Furthermore, the peptide when combined with low-dose cisplatin effectively inhibits tumor growth and metastasis without causing weight loss, and it increases the relative proportion of intestinal Akkermansia muciniphila (Akk). These findings suggest promising potential for designing cell migration/adhesion inhibiting peptides that target membrane E-cadherin for anticancer therapy.
MATERIALS & DESIGN
(2022)
Article
Biochemistry & Molecular Biology
Rajavenkatesh Krishnamoorthy, Meenakshi Singh, Parthiban Anaikutti, L. Edwin Paul, Sivasankaran Dhanasekaran, Thennarsu Sathiah
Summary: Two novel short peptides, P1 and P2, were designed and synthesized, which showed strong binding ability to receptors and proteins related to tumor. The peptides demonstrated good anticancer activities against cancer cells and low cytotoxicity to normal cells. In silico studies were conducted to predict the binding sites and orientation of the peptides for potential anticancer targets.
BIOORGANIC CHEMISTRY
(2023)
Article
Biology
Ghulam Abbas, Alfredo E. Cardenas, Ron Elber
Summary: We conducted molecular dynamics simulations to study model heterogeneous membranes and their interactions with an anticancer peptide, NAF-1(44-67). The organization of the peptide in the membrane depends on nearby phospholipid types and is influenced by the charge and size of the head groups.
Article
Chemistry, Multidisciplinary
Jianan Zhou, Yuting Cai, Tingting Li, Haixiang Zhou, Huilei Dong, Xia Wu, Zenghui Li, Wenjie Wang, Dan Yuan, Yun Li, Junfeng Shi
Summary: A novel topical delivery system, Gel 2_1 & Eylea, is developed using an aflibercept-loaded eye-drop hydrogel facilitated by cell-penetrating peptide 1. Gel 2_1 & Eylea demonstrates superior membrane permeability, increased stability, and prolonged drug retention time on the ocular surface, and significantly reduces the density of neovascularization with no adverse effects on normal corneoscleral limbal vessels in a rabbit CoNV model, showing high efficacy and biocompatibility. This research identifies a promising treatment for corneal neovascularization and potentially benefits other ocular neovascular diseases.
Article
Pharmacology & Pharmacy
Zhe Ma, Jiaxin Pi, Ying Zhang, Huan Qin, Bing Zhang, Nan Li, Zheng Li, Zhidong Liu
Summary: The tumor-targeted nanostructured lipid carrier encapsulating gambogic acid and paclitaxel, co-modified with acid-cleavable folic acid and a human-derived cell-penetrating peptide, demonstrated enhanced targeting and penetrability to tumor tissues, leading to improved anticancer activity and therapeutic efficacy.
Article
Pharmacology & Pharmacy
Csaba Bato, Ildiko Szabo, Zoltan Banoczi
Summary: In this study, the preparation and investigation of efficient cyclic CPPs are described. Different oligoarginines were designed to conjugate with rigid aromatic scaffolds or form disulfide bonds. The constructs displayed efficient internalization on cancerous cell lines. By utilizing more than one endocytic pathway, short peptides that can compete with well-known CPPs may be synthesized through cyclization.
Article
Chemistry, Medicinal
Jovana M. Muskinja, Adrijana Z. Burmudzija, Dejan D. Baskic, Suzana L. Popovic, Danijela V. Todorovic, Milan M. Zaric, Zoran R. Ratkovic
MEDICINAL CHEMISTRY RESEARCH
(2019)
Article
Chemistry, Inorganic & Nuclear
Ana Popovic, Milos Nikolic, Marina Mijajlovic, Zoran Ratkovic, Verica Jevtic, Srecko R. Trifunovic, Gordana Radic, Milan Zaric, Petar Canovic, Marija Milovanovic, Snezana Radisavljevic, Milica Mededovic, Biljana Petrovic, Ivan Jovanovic
TRANSITION METAL CHEMISTRY
(2019)
Article
Chemistry, Medicinal
Nenad Joksimovic, Nenad Jankovic, Jelena Petronijevic, Dejan Baskic, Suzana Popovic, Danijela Todorovic, Milan Zaric, Olivera Klisuric, Milan Vranes, Aleksandar Tot, Zorica Bugarcic
MEDICINAL CHEMISTRY
(2020)
Article
Biochemistry & Molecular Biology
Rogier A. Gaiser, Jaione Ayerra Mangado, Milena Mechkarska, Wendy E. Kaman, Peter van Baarlen, J. Michael Conlon, Jerry M. Wells
CHEMICAL BIOLOGY & DRUG DESIGN
(2020)
Article
Chemistry, Inorganic & Nuclear
Veronika Kucharova, Juraj Kuchar, Milan Zaric, Petar Canovic, Nebojsa Arsenijevic, Vladislav Volarevic, Maja Misirkic, Vladimir Trajkovic, Ivana D. Radojevic, Ljiljana R. Comic, Marek Matik, Ivan Potocnak
INORGANICA CHIMICA ACTA
(2019)
Article
Chemistry, Multidisciplinary
Nenad Markovic, Milan Zaric, Marija D. Zivkovic, Snezana Rajkovic, Ivan Jovanovic, Nebojsa Arsenijevic, Petar Canovic, Srdan Ninkovic
Article
Cell Biology
Galyna Graham, Andrew McCloskey, Yasser H. Abdel-Wahab, J. Michael Conlon, Peter R. Flatt
MOLECULAR AND CELLULAR ENDOCRINOLOGY
(2020)
Article
Infectious Diseases
Gervonne Barran, Jolanta Kolodziejek, Laurent Coquet, Jerome Leprince, Thierry Jouenne, Norbert Nowotny, J. Michael Conlon, Milena Mechkarska
Article
Biochemistry & Molecular Biology
Galyna Graham, J. Michael Conlon, R. Charlotte Moffett, Yasser H. Abdel-Wahab, Peter R. Flatt
Summary: The study showed that long-acting, dual-agonist anti-diabetic peptides can induce alpha-cell to beta-cell transdifferentiation, leading to increased pancreatic insulin content and plasma insulin concentrations. This suggests therapeutic potential for using proglucagon-derived peptides from phylogenetical ancient fish in diabetes treatment.
JOURNAL OF PEPTIDE SCIENCE
(2021)
Review
Biochemistry & Molecular Biology
J. Michael Conlon, Finbarr P. M. O'Harte, Peter R. Flatt
Summary: Peptides derived from ancient fish, such as lamprey GLP-1 and paddlefish glucagon, act as naturally occurring dual agonists at GLP1R and GCPR receptors, showing potential in improving glucose tolerance, insulin sensitivity, and beta-cell proliferation. Studies suggest that these fish-derived peptides have therapeutic potential for obesity-related T2DM.
Article
Biochemistry & Molecular Biology
J. Michael Conlon, Lauren Hunter, Samir Attoub, Bruno Casciaro, Milena Mechkarska, Yasser H. A. Abdel-Wahab
Summary: Ocellatin-3N is a peptide that inhibits the growth of various bacteria and pathogens, and has potential therapeutic effects. It also regulates insulin release and intracellular calcium ion concentration.
JOURNAL OF PEPTIDE SCIENCE
(2023)
Article
Infectious Diseases
J. Michael Conlon, Laure Guilhaudis, Samir Attoub, Laurent Coquet, Jerome Leprince, Thierry Jouenne, Milena Mechkarska
Summary: Peptidomic analysis of skin secretions from Boana boans frogs led to the isolation and structural characterization of five host-defense peptides with limited structural similarity to figainin 2 and picturin peptides. These peptides showed antimicrobial activity and cytotoxicity against human tumor-derived cells.
Article
Infectious Diseases
Milena Mechkarska, Taylor S. Cunning, Megan G. Taggart, Nigel G. Ternan, Jerome Leprince, Laurent Coquet, Thierry Jouenne, Jordi Tena-Garces, Juan J. Calvete, J. Michael Conlon
Summary: The venom of the Trinidad thick-tailed scorpion contains peptides with antimicrobial activity and potassium channel and sodium channel toxins. Among the peptides, TtAP-1 exhibits strong bactericidal activity against various bacteria and can rapidly kill clinically relevant bacteria. However, its high hemolytic activity limits its potential as an anti-infective agent.
Review
Biochemistry & Molecular Biology
Nasrin Abbasi Gharibkandi, J. Michael Conlon, Seyed Jalal Hosseinimehr