6,677 results match your criteria rgd peptides

Peptide-based delivery vectors with pre-defined geometrical locks.

RSC Med Chem 2020 Nov 13;11(11):1303-1313. Epub 2020 Aug 13.

Department of Biosciences and Bioengineering, Indian Institute of Technology Guwahati Guwahati-781039 Assam India

Design of peptide-based targeted delivery vectors with attributes of specificity and selective cellular targeting by fixing their topology and resulting electrostatic fingerprint is the objective of this study. We formulated our peptide design platform by utilizing the possibilities of side-chain induced geometric restrictions in a typical peptide molecule. Conceptually, we locked the conformation of the RGD/NGR motif of tumor homing peptides (THPs) by mutating glycine in these motifs with d-proline and tailed the peptides with a syndiotactic amphipathic segment for cellular penetration. Read More

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November 2020

A novel bioengineered fragment peptide of Vasostatin-1 exerts smooth muscle pharmacological activities and anti-angiogenic effects via blocking VEGFR signalling pathway.

Comput Struct Biotechnol J 2021 3;19:2664-2675. Epub 2021 May 3.

Institute of Translational Medicine, Faculty of Health Sciences, University of Macau, Avenida de Universidade, Taipa, Macau SAR, China.

Chromogranin A (CgA) is a hydrophilic glycoprotein released by post-ganglionic sympathetic neurons. CgA consists of a single peptide chain containing numerous paired basic residues, which are typical cleavage sites in prohormones to generate bioactive peptides. It is recognized as a diagnostic and prognostic serum marker for neuroendocrine tumours. Read More

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Molecular magnetic resonance imaging of Alpha-v-Beta-3 integrin expression in tumors with ultrasound microbubbles.

Biomaterials 2021 May 27;275:120896. Epub 2021 May 27.

Institute for Experimental Molecular Imaging, RWTH Aachen University, 52074, Aachen, Germany. Electronic address:

Microbubbles (MB) are used as ultrasound (US) contrast agents and can be efficiently targeted against markers of angiogenesis and inflammation. Due to their gas core, MB locally alter susceptibilities in magnetic resonance imaging (MRI), but unfortunately, the resulting contrast is low and not sufficient to generate powerful molecular MRI probes. Therefore, we investigated whether a potent molecular MR agent can be generated by encapsulating superparamagnetic iron oxide nanoparticles (SPION) in the polymeric shell of poly (n-butylcyanoacrylate) (PBCA) MB and targeted them against αβ integrins on the angiogenic vasculature of 4T1 murine breast carcinomas. Read More

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User-defined, temporal presentation of bioactive molecules on hydrogel substrates using supramolecular coiled coil complexes.

Biomater Sci 2021 Jun 2. Epub 2021 Jun 2.

Department of Chemical Engineering, University of Virginia, VA 22903, USA. and Department of Biomedical Engineering, University of Virginia, VA 22903, USA.

The ability to spatiotemporally control the presentation of relevant biomolecules in synthetic culture systems has gained significant attention as researchers strive to recapitulate the endogenous extracellular matrix (ECM) in vitro. With the biochemical composition of the ECM constantly in flux, the development of platforms that allow for user-defined control of bioactivity is desired. Here, we reversibly conjugate bioactive molecules to hydrogel-based substrates through supramolecular coiled coil complexes that form between complementary peptides. Read More

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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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Bio-Functionalized Chitosan for Bone Tissue Engineering.

Int J Mol Sci 2021 May 31;22(11). Epub 2021 May 31.

Department of Industrial Engineering, University of Padua, Via F. Marzolo 9, 35131 Padua, Italy.

Hybrid biomaterials allow for the improvement of the biological properties of materials and have been successfully used for implantology in medical applications. The covalent and selective functionalization of materials with bioactive peptides provides favorable results in tissue engineering by supporting cell attachment to the biomaterial through biochemical cues and interaction with membrane receptors. Since the functionalization with bioactive peptides may alter the chemical and physical properties of the biomaterials, in this study we characterized the biological responses of differently functionalized chitosan analogs. 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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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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An alginate-based macroporous hydrogel matrix to trap cancer cells.

Carbohydr Polym 2021 Aug 24;266:118115. Epub 2021 Apr 24.

Center for Research in Radiotherapy, Department of Nuclear Medicine and Radiobiology, Faculty of Medicine and Health Sciences, Université de Sherbrooke, Sherbrooke, Québec, Canada. Electronic address:

To overcome the radioresistance of glioblastoma (GBM) cells infiltrated in the brain, we propose to attract these cancer cells into a trap to which a lethal radiation dose can be delivered safely. Herein, we have prepared and characterized a sodium alginate-based macroporous hydrogel as a potential cancer cell trap. Microcomputed X-ray tomography shows that the hydrogel matrices comprise interconnected pores with an average diameter of 300 μm. Read More

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Nanoengineered Peptide-Based Antimicrobial Conductive Supramolecular Biomaterial for Cardiac Tissue Engineering.

Adv Mater 2021 May 25:e2008715. Epub 2021 May 25.

Shmunis School of Biomedicine and Cancer Research, George S. Wise Faculty of Life Sciences, Tel Aviv University, Tel Aviv, 6997801, Israel.

Owing to their dynamic nature and ordered architecture, supramolecular materials strikingly resemble organic components of living systems. Although short-peptide self-assembled nanostructured hydrogels are regarded as intriguing supramolecular materials for biotechnology, their application is often limited due to their low stability and considerable challenge of combining other desirable properties. Herein, a di-Fmoc-based hydrogelator containing the cell-adhesive Arg-Gly-Asp (RGD) fragment that forms a mechanically stable, self-healing hydrogel is designed. Read More

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New trends in the development of multifunctional peptides to functionalize biomaterials.

J Pept Sci 2021 May 24:e3335. Epub 2021 May 24.

Biomaterials, Biomechanics and Tissue Engineering Group, Department of Materials Science and Engineering, Universitat Politècnica de Catalunya (UPC), Barcelona, Spain.

Improving cell-material interactions is a major goal in tissue engineering. In this regard, functionalization of biomaterials with cell instructive molecules from the extracellular matrix stands out as a powerful strategy to enhance their bioactivity and achieve optimal tissue integration. However, current functionalization strategies, like the use of native full-length proteins, are associated with drawbacks, thus urging the need of developing new methodologies. Read More

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Peptidic biofunctionalization of laser patterned dental zirconia: A biochemical-topographical approach.

Mater Sci Eng C Mater Biol Appl 2021 Jun 20;125:112096. Epub 2021 Apr 20.

Biomaterials, Biomechanics and Tissue Engineering Group (BBT), Department of Materials Science and Engineering, Universitat Politècnica de Catalunya-BarcelonaTECH, 08019 Barcelona, Spain; Barcelona Research Center in Multiscale Science and Engineering, Universitat Politècnica de Catalunya-BarcelonaTECH, 08019 Barcelona, Spain. Electronic address:

A dual approach employing peptidic biofunctionalization and laser micro-patterns on dental zirconia was explored, with the aim of providing a flexible tool to improve tissue integration of restorations. Direct laser interference patterning with a femtosecond Ti:Sapphire laser was employed, and two periodic grooved patterns were produced with a periodicity of 3 and 10 μm. A platform containing the cell-adhesive RGD and the osteogenic DWIVA peptides was used to functionalize the grooved surfaces. Read More

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Expression and purification of a recombinant ELRL-MAP30 with dual-targeting anti-tumor bioactivity.

Protein Expr Purif 2021 Sep 30;185:105893. Epub 2021 Apr 30.

College of Life Science, Zhejiang Chinese Medical University, Hangzhou, 310053, China. Electronic address:

MAP30 (Momordica antiviral protein 30kD) is a single-chain Ⅰ-type ribosome inactivating protein with a variety of biological activities, including anti-tumor ability. It was reported that MAP30 would serve as a novel and relatively safe agent for prophylaxis and treatment of liver cancer. To determine whether adding two tumor targeting peptides could improve the antitumor activities of MAP30, we genetically modified MAP30 with an RGD motif and a EGFRi motif, which is a ligand with high affinity for αvβ3 integrins and with high affinity for EGFR. Read More

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September 2021

Multifunctional pathology-mapping theranostic nanoplatforms for US/MR imaging and ultrasound therapy of atherosclerosis.

Nanoscale 2021 May 30;13(18):8623-8638. Epub 2021 Apr 30.

Department of Ultrasound, Laboratory of Ultrasound Imaging and Drug, West China Hospital, Sichuan University, Chengdu, Sichuan 610041, China.

Atherosclerotic thrombosis is the leading cause of most life-threatening cardiovascular diseases (CVDs), particularly as a result of rupture or erosion of vulnerable plaques. Rupture or erosion-prone plaques are quite different in cellular composition and immunopathology, requiring different treatment strategies. The current imaging technology cannot distinguish the types of vulnerable plaques, and thus empirical treatment is still applied to all without a tailored and precise treatment. 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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High-throughput hyaluronic acid hydrogel arrays for cell selective adhesion screening.

J Mater Chem B 2021 05 26;9(19):4024-4030. Epub 2021 Apr 26.

MOE Key Laboratory of Macromolecule Synthesis and Functionalization, Department of Polymer Science and Engineering, Zhejiang University, Hangzhou 310027, P. R. China.

As a component of extracellular matrix (ECM), hyaluronic acid (HA) has plenty of applications in the biomedical field such as tissue engineering. Due to its non-adhesive nature, HA requires further grafting of functional molecules for cell related study. RGD and YIGSR are two kinds of cell adhesion peptides. Read More

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Self-Assembly Iron Oxide Nanoclusters for Photothermal-Mediated Synergistic Chemo/Chemodynamic Therapy.

J Immunol Res 2021 7;2021:9958239. Epub 2021 Apr 7.

Department of Neurosurgery & Brain and Nerve Research Laboratory, The First Affiliated Hospital of Soochow University, Suzhou, Jiangsu Province, China.

Methods: Superparamagnetic iron oxide nanoclusters (SPIOCs) were located within the core, which resulted in high photothermal conversion and outstanding generation of reactive oxygen species (ROS). The shell consisted of a human serum albumin- (HSA-) paclitaxel (PTX) layer, which extended the blood circulation time and ensured the effectiveness of the chemotherapy. Arg-Gly-Asp peptides (RGD) were linked to the naked cysteine moieties in HSA to promote the specific targeting of human glioma U87 cells by integrins. 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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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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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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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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Hyaluronic Acid and a Short Peptide Improve the Performance of a PCL Electrospun Fibrous Scaffold Designed for Bone Tissue Engineering Applications.

Int J Mol Sci 2021 Mar 12;22(5). Epub 2021 Mar 12.

The Center for Nanoscience and Nanotechnology, Tel Aviv University, Tel Aviv 6997801, Israel.

Bone tissue engineering is a rapidly developing, minimally invasive technique for regenerating lost bone with the aid of biomaterial scaffolds that mimic the structure and function of the extracellular matrix (ECM). Recently, scaffolds made of electrospun fibers have aroused interest due to their similarity to the ECM, and high porosity. Hyaluronic acid (HA) is an abundant component of the ECM and an attractive material for use in regenerative medicine; however, its processability by electrospinning is poor, and it must be used in combination with another polymer. Read More

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3D Encapsulation and tethering of functionally engineered extracellular vesicles to hydrogels.

Acta Biomater 2021 05 16;126:199-210. Epub 2021 Mar 16.

Department of Oral Biology, College of Dentistry, University of Illinois at Chicago, Chicago, IL 60612, United States. Electronic address:

Mesenchymal stem cell (MSC) derived extracellular vesicles (EVs) in their naïve and engineered forms have emerged as potential alternatives to stem cell therapy. While they have a defined therapeutic potential, the spatial and temporal control of their activity in vivo remains a challenge. The objective of this study was to devise a methodology to encapsulate EVs in 3D hydrogels for prolonged delivery. Read More

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

Biomater Sci 2021 Mar 16. Epub 2021 Mar 16.

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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Geometry encoded functional programming of tumor homing peptides for targeted drug delivery.

J Control Release 2021 May 13;333:16-27. Epub 2021 Mar 13.

Department of Biosciences and Bioengineering, Indian Institute of Technology Guwahati, Guwahati 781039, Assam, India. Electronic address:

Poly-peptide molecules have shown promising applications in drug delivery and tumor targeting. A series of tumor homing peptides were designed by exhaustively sampling low energy geometrical basins of amino acids at specific sites of a peptide molecule to induce a conformational lock. This peptide library was pruned to a limited set of eight molecules, employing electrostatic interactions, docking, and molecular dynamics simulations. 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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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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Substrate stiffness induces neutrophil extracellular trap (NET) formation through focal adhesion kinase activation.

Biomaterials 2021 04 11;271:120715. Epub 2021 Feb 11.

Department of Biomedical Engineering, School of Engineering, Virginia Commonwealth University, Richmond, VA, United States. Electronic address:

Neutrophils predominate the early inflammatory response to tissue injury and implantation of biomaterials. Recent studies have shown that neutrophil activation can be regulated by mechanical cues such as stiffness or surface wettability; however, it is not known how neutrophils sense and respond to physical cues, particularly how they form neutrophil extracellular traps (NET formation). To examine this, we used polydimethylsiloxane (PDMS) substrates of varying physiologically relevant stiffness (0. Read More

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