5,392 results match your criteria rgd peptide


Synthesis of Novel, Dual-Targeting Ga-NODAGA-LacN-E[c(RGDfK)] Glycopeptide as a PET Imaging Agent for Cancer Diagnosis.

Pharmaceutics 2021 May 26;13(6). Epub 2021 May 26.

Division of Nuclear Medicine and Translational Imaging, Department of Medical Imaging, Faculty of Medicine, University of Debrecen, Nagyerdei krt. 98, H-4032 Debrecen, Hungary.

Radiolabeled peptides possessing an Arg-Gly-Asp (RGD) motif are widely used radiopharmaceuticals for PET imaging of tumor angiogenesis due to their high affinity and selectivity to αβ integrin. This receptor is overexpressed in tumor and tumor endothelial cells in the case of numerous cancer cell lines, therefore, it is an excellent biomarker for cancer diagnosis. The galectin-3 protein is also highly expressed in tumor cells and N-acetyllactosamine is a well-established ligand of this receptor. Read More

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Molecular Imaging and Preclinical Studies of Radiolabeled Long-Term RGD Peptides in U-87 MG Tumor-Bearing Mice.

Int J Mol Sci 2021 May 21;22(11). Epub 2021 May 21.

Division of Isotope Application, Institute of Nuclear Energy Research, Taoyuan 32546, Taiwan.

The Arg-Gly-Asp (RGD) peptide shows a high affinity for αβ integrin, which is overexpressed in new tumor blood vessels and many types of tumor cells. The radiolabeled RGD peptide has been studied for cancer imaging and radionuclide therapy. We have developed a long-term tumor-targeting peptide DOTA-EB-cRGDfK, which combines a DOTA chelator, a truncated Evans blue dye (EB), a modified linker, and cRGDfK peptide. Read More

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GP96 Drives Exacerbation of Secondary Bacterial Pneumonia following Influenza A Virus Infection.

mBio 2021 Jun 1:e0326920. Epub 2021 Jun 1.

Department of Oral and Molecular Microbiology, Osaka University Graduate School of Dentistry, Osaka, Japan.

Influenza A virus (IAV) infection predisposes the host to secondary bacterial pneumonia, known as a major cause of morbidity and mortality during influenza virus epidemics. Analysis of interactions between IAV-infected human epithelial cells and Streptococcus pneumoniae revealed that infected cells ectopically exhibited the endoplasmic reticulum chaperone glycoprotein 96 (GP96) on the surface. Importantly, efficient pneumococcal adherence to epithelial cells was imparted by interactions with extracellular GP96 and integrin α, with the surface expression mediated by GP96 chaperone activity. Read More

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The investigation into the effect of the length of RGD peptides and temperature on the interaction with the αIIbβ3 integrin: a molecular dynamic study.

J Biomol Struct Dyn 2021 Jun 1:1-12. Epub 2021 Jun 1.

Physiology Research Center, Faculty of Medicine, Iran University of Medical Sciences, Tehran, Iran.

The tripeptide Arg-Gly-Asp acid (RGD) is a protein sequence in the binding of proteins to cell surfaces, and is involved in various biological processes such as cell adhesion to the extracellular matrix, platelet activation, hemostasis, etc. The C2 domain of the Von Willebrand Factor (VWF), containing the RGD motif, plays an important role in the initial homeostasis process. It binds to the αIIbβ3 integrin and stimulates platelet aggregation. Read More

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Oxidation and RGD Modification Affect the Early Neural Differentiation of Murine Embryonic Stem Cells Cultured in Core-Shell Alginate Hydrogel Microcapsules.

Cells Tissues Organs 2021 May 26:1-10. Epub 2021 May 26.

Department of Biomedical Engineering, The Ohio State University, Columbus, Ohio, USA.

Directed neural differentiation of embryonic stem cells (ESCs) has been studied extensively to improve the treatment of neurodegenerative disorders. This can be done through stromal-cell derived inducing activity (SDIA), by culturing ESCs directly on top of a layer of feeder stromal cells. However, the stem cells usually become mixed with the feeder cells during the differentiation process, making it difficult to obtain a pure population of the differentiated cells for further use. Read More

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Engineered Matrices Enable the Culture of Human Patient-Derived Intestinal Organoids.

Adv Sci (Weinh) 2021 05 12;8(10):2004705. Epub 2021 Mar 12.

Department of Materials Science & Engineering Stanford University Stanford CA 94305 USA.

Human intestinal organoids from primary human tissues have the potential to revolutionize personalized medicine and preclinical gastrointestinal disease models. A tunable, fully defined, designer matrix, termed hyaluronan elastin-like protein (HELP) is reported, which enables the formation, differentiation, and passaging of adult primary tissue-derived, epithelial-only intestinal organoids. HELP enables the encapsulation of dissociated patient-derived cells, which then undergo proliferation and formation of enteroids, spherical structures with polarized internal lumens. Read More

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The effect of RGD-targeted and non-targeted liposomal Galbanic acid on the therapeutic efficacy of pegylated liposomal doxorubicin: From liposomal preparation to in-vivo studies.

Int J Pharm 2021 May 19;604:120710. Epub 2021 May 19.

Nanotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran. Electronic address:

The anti-cancer therapeutic application of Galbanic acid (Gba) as a strong antiangiogenic sesquiterpene coumarin has been limited due to its low water solubility. This issue necessitates developing new liposomal formulations for the efficient delivery of Gba in vivo. In this study, various liposomal formulations were prepared by a thin-film hydration method, and Gba was incorporated into the liposomal bilayers, which consequently increased its release profile compared to formulations in our previous study prepared by remote loading methods. Read More

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Multifunctional nanoplatforms as cascade-responsive drug-delivery carriers for effective synergistic chemo-photodynamic cancer treatment.

J Nanobiotechnology 2021 May 17;19(1):140. Epub 2021 May 17.

Department of Oral and Maxillofacial Head & Neck Oncology, Shanghai Ninth People's Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, 200011, China.

Synergistic chemo-photodynamic therapy has garnered attention in the field of cancer treatment. Here, a pH cascade-responsive micellar nanoplatform with nucleus-targeted ability, for effective synergistic chemo-photodynamic cancer treatment, was fabricated. In this micellar nanoplatform, 5-(4-carboxyphenyl)-10,15,20-triphenylporphyrin (Por), a photodynamic therapy (PDT) agent was utilized for carrying the novel anticancer drug GNA002 to construct a hydrophobic core, and cyclic RGD peptide (cRGD)-modified polyethylene glycol (PEG) (cRGD-PEG) connected the cell-penetrating peptide hexaarginine (R) through a pH-responsive hydrazone bond (cRGD-PEG-N = CH-R) to serve as a hydrophilic shell for increasing blood circulation time. Read More

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Label-free tracking of whole-cell response on RGD functionalized surfaces to varied flow velocities generated by fluidic rotation.

J Colloid Interface Sci 2021 Oct 20;599:620-630. Epub 2021 Apr 20.

Nanobiosensorics Laboratory, ELKH EK MFA, Budapest, Hungary. Electronic address:

Fluidic flow plays important roles in colloid and interface sciences. Measuring adsorption, aggregation processes and living cell behavior under a fluidic environment with varied flow velocities in a parallel and high-throughput manner remains to be a challenging task. Here a method is introduced to monitor cell response to well-defined flow with varied velocities over an array of label-free resonant waveguide grating (RWG) based optical biosensors. Read More

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October 2021

Enhancing osteogenesis of adipose-derived mesenchymal stem cells using gold nanostructure/peptide-nanopatterned graphene oxide.

Colloids Surf B Biointerfaces 2021 Apr 29;204:111807. Epub 2021 Apr 29.

School of Integrative Engineering, Chung-Ang University, Seoul, Republic of Korea; Integrative Research Center for Two-Dimensional Functional Materials, Institute of Interdisciplinary Convergence Research, Chung-Ang University, Seoul, Republic of Korea. Electronic address:

Graphene derivatives are highly promising materials for use in stem-cell-based regenerative therapies, particularly for bone regeneration. Herein, we report a graphene oxide (GO)-based hybrid platform (GOHP) that is highly effective for guiding the osteogenesis of human adipose-derived mesenchymal stem cells (hAMSCs). A GO-coated indium tin oxide (ITO) substrate was electrochemically modified with Au nanostructures (GNSs), following which a cysteine-modified quadruple-branched arginine-glycine-aspartic acid was self-assembled on the ITO-GO-GNS hybrid via Au-S bonds. Read More

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RGD-Peptide Functionalization Affects the Diffusion of a Responsive Trimeric MRI Contrast Agent through Interactions with Integrins.

J Med Chem 2021 06 7;64(11):7565-7574. Epub 2021 May 7.

Max Planck Institute for Biological Cybernetics, Department for Physiology of Cognitive Processes, Max-Planck-Ring 11, 72072 Tübingen, Germany.

The relevance of MRI as a diagnostic methodology has been expanding significantly with the development of molecular imaging. Partially, the credit for this advancement is due to the increasing potential and performance of targeted MRI contrast agents, which are able to specifically bind distinct receptors or biomarkers. Consequently, these allow for the identification of tissues undergoing a disease, resulting in the over- or underexpression of the particular molecular targets. Read More

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The Spike Glycoprotein of SARS-CoV-2 Binds to β1 Integrins Expressed on the Surface of Lung Epithelial Cells.

Viruses 2021 04 9;13(4). Epub 2021 Apr 9.

Department of Molecular Pathobiology and Cell Adhesion Biology, Mie University Graduate School of Medicine, 2-174 Edobashi, Tsu-City 514-8507, Mie, Japan.

The spike glycoprotein attached to the envelope of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) binds to and exploits angiotensin-converting enzyme 2 (ACE2) as an entry receptor to infect pulmonary epithelial cells. A subset of integrins that recognize the arginyl-glycyl-aspartic acid (RGD) sequence in the cognate ligands has been predicted in silico to bind the spike glycoprotein and, thereby, to be exploited for viral infection. Here, we show experimental evidence that the β1 integrins predominantly expressed on human pulmonary epithelial cell lines and primary mouse alveolar epithelial cells bind to this spike protein. Read More

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A Smart Multifunctional Nanoparticle for Enhanced Near-Infrared Image-Guided Photothermal Therapy Against Gastric Cancer.

Int J Nanomedicine 2021 19;16:2897-2915. Epub 2021 Apr 19.

Department of Gastrointestinal Surgery, The Third Affiliated Hospital of Sun Yat-sen University, Guangzhou, 510630, People's Republic of China.

Background: Surgery is considered to be a potentially curative approach for gastric cancer. However, most cases are diagnosed at a very advanced stage for the lack of typical symptoms in the initial stage, which makes it difficult to completely surgical resect of tumors. Early diagnosis and precise personalized intervention are urgent issues to be solved for improving the prognosis of gastric cancer. Read More

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Antineoplastic Effects and Mechanisms of a New RGD Chimeric Peptide from Bullfrog Skin on the Proliferation and Apoptosis of B16F10 Cells.

Protein J 2021 Apr 20. Epub 2021 Apr 20.

Tianjin Key Laboratory of Agricultural Animal Breeding and Healthy Husbandry, College of Animal Science and Veterinary Medicine, Tianjin Agricultural University, Tianjin, 300384, China.

Malignant melanoma, an increasingly common form of skin cancer, poses a significant threat to public health, especially when the disease progresses past skin lesions to the stage of advanced metastasis. In this work, a new anti-tumor peptide, temporin La (T-La), was selected from a cDNA library generated from bullfrog skin. Two new derivative antitumor peptides, T-La (S) and T-La (FS), were designed by bioinformatics analysis and coupled with the RGD small molecule peptide to create chimeric RGD peptides, (RGD-T-La [S] and RGD-T-La [FS]). Read More

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Synthesis and biological studies of c(RGDyK) conjugates of cucurbitacins.

Future Med Chem 2021 May 16;13(10):877-895. Epub 2021 Apr 16.

Department of Chemistry, Aristotle University of Thessaloniki, University Campus, Thessaloniki, 54124, Greece.

Cucurbitacins (CUCUs) are triterpenoids known to display potent cytotoxic effects; however, their clinical application is limited due to poor pharmacokinetics and systemic toxicity. This work focuses on the development of c(RGDyK)-CUCU conjugates for the selective delivery of CUCUs to integrin-overexpressing cancer cells. The activity of the conjugates against various cancer cells was studied. Read More

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Inhibited effect of an RGD peptide hydrogel on the expression of β1-integrin, FAK, and Akt in Tenon's capsule fibroblasts.

J Biomed Mater Res B Appl Biomater 2021 Apr 13. Epub 2021 Apr 13.

Institute of Biology and Medicine, College of Life Sciences and Health, Wuhan University of Science and Technology, Wuhan, China.

Tenon's capsule fibroblasts are the main cellular components of filtration tract scar that limit the success rate of glaucoma filtration surgery. Scar formation results from infiltration and proliferation of fibroblasts into damaged areas, meanwhile synthesis of extracellular matrix glycoproteins. Integrins are cell surface receptors for extracellular molecules that mediate cell adhesion, spreading, migration, and invasion. Read More

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Targeted apoptosis of macrophages and osteoclasts in arthritic joints is effective against advanced inflammatory arthritis.

Nat Commun 2021 04 12;12(1):2174. Epub 2021 Apr 12.

Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry, Sichuan Engineering Laboratory for Plant-Sourced Drug and Sichuan Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, Chengdu, 610064, China.

Insufficient apoptosis of inflammatory macrophages and osteoclasts (OCs) in rheumatoid arthritis (RA) joints contributes toward the persistent progression of joint inflammation and destruction. Here, we deliver celastrol (CEL) to selectively induce apoptosis of OCs and macrophages in arthritic joints, with enzyme-responsive nanoparticles (termed PRNPs) composed of RGD modified nanoparticles (termed RNPs) covered with cleavable PEG chains. CEL-loaded PRNPs (CEL-PRNPs) dually target OCs and inflammatory macrophages derived from patients with RA via an RGD-αvβ3 integrin interaction after PEG cleavage by matrix metalloprotease 9, leading to increased apoptosis of these cells. Read More

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Dextran-based scaffolds for in-situ hydrogelation: Use for next generation of bioartificial cardiac tissues.

Carbohydr Polym 2021 Jun 17;262:117924. Epub 2021 Mar 17.

Institute for Organic Chemistry, Leibniz University Hannover, Schneiderberg 1B, 30167 Hannover, Germany. Electronic address:

In pursuit of a chemically-defined matrix for in vitro cardiac tissue generation, we present dextran (Dex)-derived hydrogels as matrices suitable for bioartificial cardiac tissues (BCT). The dextran hydrogels were generated in situ by using hydrazone formation as the crosslinking reaction. Material properties were flexibly adjusted, by varying the degrees of derivatization and the molecular weight of dextran used. Read More

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Shear-Resistant, Biological Tethering of Nanostimulators for Enhanced Therapeutic Cell Paracrine Factor Secretion.

ACS Appl Mater Interfaces 2021 Apr 8;13(15):17276-17288. Epub 2021 Apr 8.

Department of Chemical and Biomolecular Engineering, University of Illinois at Urbana-Champaign, Urbana, Illinois 61801, United States.

Mesenchymal stromal cells (MSCs) secreting multiple growth factors and immunomodulatory cytokines are promising for regenerative medicine. To further enhance their secretory activity, efforts have emerged to tether nanosized carriers of secretory stimuli, named nanostimulators, to the MSC surface by forming nonchemical bonds. Despite some successes, there is a great need to improve the retention of nanostimulators during transport through a syringe needle, where high shear stress exerted on the cell surface separates them. Read More

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Bioengineering a cryogel-derived bioartificial liver using particle image velocimetry defined fluid dynamics.

Mater Sci Eng C Mater Biol Appl 2021 Apr 23;123:111983. Epub 2021 Feb 23.

School of Pharmacy and Biomolecular Sciences, University of Brighton, Brighton, United Kingdom. Electronic address:

Bioartificial Liver (BAL) devices are extracorporeal systems designed to support or recover hepatic function in patients with liver failure. The design of an effective BAL remains an open challenge since it requires a complex co-optimisation of cell colonisation, biomaterial scaffold and BAL fluid dynamics. Building on previous evidence of suitability as a blood perfusion device for detoxification, the current study investigated the use of RGD-containing p(HEMA)-alginate cryogels as BAL scaffolds. Read More

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PET Diagnostic Molecules Utilizing Multimeric Cyclic RGD Peptide Analogs for Imaging Integrin αβ Receptors.

Molecules 2021 Mar 22;26(6). Epub 2021 Mar 22.

Radiochemical Studies Laboratory, Institute of Nuclear & Radiological Sciences & Technology, Energy & Safety, National Centre for Scientific Research "Demokritos", Ag. Paraskevi Attikis, 15310 Athens, Greece.

Multimeric ligands consisting of multiple pharmacophores connected to a single backbone have been widely investigated for diagnostic and therapeutic applications. In this review, we summarize recent developments regarding multimeric radioligands targeting integrin αβ receptors on cancer cells for molecular imaging and diagnostic applications using positron emission tomography (PET). Integrin αβ receptors are glycoproteins expressed on the cell surface, which have a significant role in tumor angiogenesis. Read More

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A novel role for milk fat globule-EGF factor 8 protein (MFGE8) in the mediation of mouse sperm-extracellular vesicle interactions.

Proteomics 2021 Mar 31:e2000079. Epub 2021 Mar 31.

Priority Research Centre for Reproductive Science, The University of Newcastle, Callaghan, New South Wales, Australia.

Spermatozoa transition to functional maturity as they are conveyed through the epididymis, a highly specialized region of the male excurrent duct system. Owing to their transcriptionally and translationally inert state, this transformation into fertilization competent cells is driven by complex mechanisms of intercellular communication with the secretory epithelium that delineates the epididymal tubule. Chief among these mechanisms are the release of extracellular vesicles (EV), which have been implicated in the exchange of varied macromolecular cargo with spermatozoa. Read More

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Targeting RGD-binding integrins as an integrative therapy for diabetic retinopathy and neovascular age-related macular degeneration.

Prog Retin Eye Res 2021 Mar 26:100966. Epub 2021 Mar 26.

Oxurion NV, Gaston Geenslaan 1, 3001, Heverlee, Belgium. Electronic address:

Integrins are a class of transmembrane receptors that are involved in a wide range of biological functions. Dysregulation of integrins has been implicated in many pathological processes and consequently, they are attractive therapeutic targets. In the ophthalmology arena, there is extensive evidence suggesting that integrins play an important role in diabetic retinopathy (DR), age-related macular degeneration (AMD), glaucoma, dry eye disease and retinal vein occlusion. Read More

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Multiple bioanalytical methods reveal a thyroid-disrupting mechanism related to the membrane receptor integrin αβ.

Environ Pollut 2021 Jun 17;279:116933. Epub 2021 Mar 17.

Engineering Research Center of Groundwater Pollution Control and Remediation, Ministry of Education, College of Water Sciences, Beijing Normal University, Beijing, 100875, China.

Di(2-ethylhexyl) phthalate (DEHP), a manufactured chemical, is suitable for large-scale production and has extensive applications. Although restricted for use, DEHP is still ubiquitous in the environment and shows potential to disrupt the structure or function of the thyroid system. However, its toxic mechanism is complex and not clearly understood. Read More

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Micro-positron emission tomography imaging of angiogenesis based on F-RGD for assessing liver metastasis of colorectal cancer.

Hepatobiliary Pancreat Dis Int 2021 Mar 9. Epub 2021 Mar 9.

Department of Radiology, Beijing Friendship Hospital, Capital Medical University, Beijing 100050, China. Electronic address:

Background: Positron emission tomography (PET) imaging is a non-invasive method to visualize and quantify the tumor microenvironment. This study aimed to explore the feasibility of F-AIF-NOTA-E[PEG-c(RGDfk)] (denoted as F-RGD) PET quantitative parameters to distinguish the angiogenesis in colorectal cancer (CRC) mice which has different metastatic potential.

Methods: Twenty LoVo and twenty LS174T of CRC liver metastases animal models were established by implantation of human CRC cell lines via intrasplenic injection. Read More

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Enhancement of anti-inflammatory and immunomodulatory effects of adipose-derived human mesenchymal stem cells by making uniform spheroid on the new nano-patterned plates.

Biochem Biophys Res Commun 2021 05 19;552:164-169. Epub 2021 Mar 19.

R&D Center, YidoBio, Inc., 123 Beolmal-ro, Anyang-si, Gyeonggi-do, 14056, South Korea. Electronic address:

Human mesenchymal stem cells (MSCs) are known to have anti-inflammatory and immunomodulatory functions; thus, several MSC products have been applied as cell therapy in clinical trials worldwide. Recent studies have demonstrated that MSC spheroids have superior anti-inflammatory and immunomodulatory functions to a single cell suspension. Current methods to prepare MSC spheroids include hanging drop, concave microwell aggregation, spinner flask, and gravity circulation. Read More

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Bicyclic RGD peptides enhance nerve growth in synthetic PEG-based Anisogels.

Biomater Sci 2021 Jun;9(12):4329-4342

DWI Leibniz Institute for Interactive Materials, Forckenbeckstrasse 50, 52074 Aachen, Germany and Institute for Technical and Macromolecular Chemistry, RWTH Aachen, Worringerweg 1-2, 52074 Aachen, Germany. and Institute of Applied Medical Engineering, RWTH University, Pauwelsstraße 20, 52074 Aachen, Germany.

Nerve regeneration scaffolds often consist of soft hydrogels modified with extracellular matrix (ECM) proteins or fragments, as well as linear and cyclic peptides. One of the commonly used integrin-mediated cell adhesive peptide sequences is Arg-Gly-Asp (RGD). Despite its straightforward coupling mechanisms to artificial extracellular matrix (aECM) constructs, linear RGD peptides suffer from low stability towards degradation and lack integrin selectivity. Read More

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Tumor acidic microenvironment-induced drug release of RGD peptide nanoparticles for cellular uptake and cancer therapy.

Colloids Surf B Biointerfaces 2021 Jun 4;202:111673. Epub 2021 Mar 4.

School of Bioscience and Technology, Weifang Medical University, Weifang, 261053, PR China. Electronic address:

Spatial accuracy is crucial in drug delivery, especially to increase the efficacy and reduce the side effects of antitumor drugs. In this study, we developed a simple and broadly applicable strategy in which a target peptide ligand was introduced to construct a pH-responsive drug-loading system to achieve targeted delivery and drug release in lesions. In addition to reaching the tumor tissue through passive targeting modalities such as the enhanced permeability and retention (EPR) effect, active targeting nanoparticles used RGD motifs coupled to nanocarriers to specifically bind certain integrins, such as ανβ3, which is expressed on the surface of tumor cells, to achieve active tumor cell targeting. Read More

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Enzymatically Cross-linked Hydrogels Based on Synthetic Poly(α-amino acid)s Functionalized with RGD Peptide for 3D Mesenchymal Stem Cell Culture.

Biomacromolecules 2021 Apr 12;22(4):1417-1431. Epub 2021 Mar 12.

Institute of Macromolecular Chemistry, Academy of Sciences of the Czech Republic, Heyrovsky Sq. 2, Prague 6 162 06, Czech Republic.

Injectable hydrogel scaffolds combined with stem cell therapy represent a promising approach for minimally invasive surgical tissue repair. In this study, we developed and characterized a fully synthetic, biodegradable poly(-(2-hydroxyethyl)-l-glutamine)-based injectable hydrogel modified with integrin-binding arginine-glycine-aspartic acid (RGD) peptide (PHEG-Tyr-RGD). The biodegradable hydroxyphenyl polymer precursor derivative of PHEG-Tyr was enzymatically cross-linked to obtain injectable hydrogels with different physicochemical properties. Read More

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Paclitaxel and naringenin-loaded solid lipid nanoparticles surface modified with cyclic peptides with improved tumor targeting ability in glioblastoma multiforme.

Biomed Pharmacother 2021 Jun 9;138:111461. Epub 2021 Mar 9.

Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, Hamdard Nagar, New Delhi 110062, India. Electronic address:

The present work describes the systematic development of paclitaxel and naringenin-loaded solid lipid nanoparticles (SLNs) for the treatment of glioblastoma multiforme (GBM). So far only temozolomide therapy is available for the GBM treatment, which fails by large amount due to poor brain permeability of the drug and recurrent metastasis of the tumor. Thus, we investigated the drug combination containing paclitaxel and naringenin for the treatment of GBM, as these drugs have individually demonstrated significant potential for the management of a wide variety of carcinoma. Read More

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