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Although chemotherapy has been known as a powerful medication for cancer treatment over the years, there is an important necessity for designing a novel targeted drug delivery system to overcome the drawbacks of this conventional method including undesired side effects on normal cells and drug resistance. The structural differences between the surface of cancerous and normal cells allow to design and engineer targeted drug delivery systems for cancer treatment. Integrins as one of the cell surface receptors over-expressed in cancer cells could potentially be suitable candidates for targeting cancer cells. In the present study, the novel nano-carriers based on designed MiRGD peptides and graphene quantum dots (GQDs) have been used for targeted delivery of doxorubicin (Dox) and curcumin (Cur) as hydrophilic and hydrophobic drug models, respectively. The prepared nano-composites were characterized by UV-vis and photoluminescence (PL) spectroscopies, Zeta-Sizer and transmission electron microscopy (TEM). Altogether, the results of cellular uptake and fluorimetric assays performed in HUVEC and HFF cells as models of αv integrin-over-expressed cancer and normal cells, respectively, besides in-vivo study on breast cancer bearing BALB/c mice, demonstrated that the prepared nano-composites can be considered as suitable multifunctional theranostic peptideticles for targeted drug delivery and tracking.
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http://dx.doi.org/10.1016/j.nano.2022.102544 | DOI Listing |
J Environ Pathol Toxicol Oncol
January 2025
Department of Pharmacy, Renmin Hospital, Hubei University of Medicine, Shiyan, Hubei 442000, P.R. China.
Despite advancements in systemic therapy, the mortality rate for patients with metastatic melanoma remains around 70%, underscoring the imperative for alternative treatment strategies. Through the establishment of a chemoresistant melanoma model and a subsequent drug investigation, we have identified pacritinib, a medication designed for treating myelofibrosis and severe thrombocytopenia, as a potential candidate to overcome resistance to melanoma therapy. Our research reveals that pacritinib, administered at clinically achievable concentrations, effectively targets dacarbazine-resistant melanoma cells by suppressing IRAK1 rather than JAK2.
View Article and Find Full Text PDFJ Environ Pathol Toxicol Oncol
January 2025
Pharmacology and Drug Discovery Research Laboratory, Division of Life Sciences; Institute of Advanced Study in Science and Technology (IASST), An Autonomous Institute under - Department of Science & Technology (Govt. of India).
Iron is an essential trace element for the human body, but having too much or too little of it can cause various biological issues. When ferrous ions react with hydrogen peroxide, they create highly reactive and soluble hydroxyl radicals that can damage cells through oxidation. This reaction, known as the Fenton reaction, can cause lipid peroxidation and ferroptosis.
View Article and Find Full Text PDFCrit Rev Ther Drug Carrier Syst
January 2025
Department of Pharmacology, PSG College of Pharmacy, Coimbatore 641004, Tamil Nadu, India.
Treating neurological disorders is challenging due to the blood-brain barrier (BBB), which limits therapeutic agents, including proteins and peptides, from entering the central nervous system. Despite their potential, the BBB's selective permeability is a significant obstacle. This review explores recent advancements in protein therapeutics for BBB-targeted delivery and highlights computational tools.
View Article and Find Full Text PDFCrit Rev Ther Drug Carrier Syst
January 2025
Department of Biotechnology, School of Chemical and Life Sciences, Jamia Hamdard, New Delhi 110062, India.
Cancer stem cells (CSCs) are a category of cancer cells endowed with the ability to renew themselves, undergo unregulated growth, and exhibit a differentiation capacity akin to that of normal stem cells. CSCs have been linked with tumor metastasis and cancer recurrence due to their ability to elude immune monitoring. As a result, targeting CSCs specifically may improve the efficacy of cancer therapy.
View Article and Find Full Text PDFJ Med Chem
September 2025
State Key Laboratory of Bioactive Molecules and Druggability Assessment, Guangdong Basic Research Center of Excellence for Natural Bioactive Molecules and Discovery of Innovative Drugs, International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Discovery o
Aberrant activation of fibroblast growth factor receptors (FGFRs) plays a critical role in tumorigenesis across multiple cancer types, driving the development of various FGFR inhibitors. Despite clinical advances, therapeutic efficacy remains limited by the emergence of drug resistance, primarily mediated by gatekeeper mutations in FGFRs. To overcome this challenge, we designed and synthesized a novel series of 7-(1-methyl-1-indole-3-yl)-5-pyrrolo[2,3-]pyrazine derivatives as covalent pan-FGFR inhibitors targeting both wild-type and gatekeeper mutants.
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