keyword
https://read.qxmd.com/read/38399248/peg-lipid-plga-hybrid-particles-for-targeted-delivery-of-anti-inflammatory-drugs
#21
JOURNAL ARTICLE
Jana Ismail, Lea C Klepsch, Philipp Dahlke, Ekaterina Tsarenko, Antje Vollrath, David Pretzel, Paul M Jordan, Kourosh Rezaei, Justyna A Czaplewska, Steffi Stumpf, Baerbel Beringer-Siemers, Ivo Nischang, Stephanie Hoeppener, Oliver Werz, Ulrich S Schubert
Hybrid nanoparticles (HNPs) were designed by combining a PLGA core with a lipid shell that incorporated PEG-Lipid conjugates with various functionalities (-RGD, -cRGD, -NH2 , and -COOH) to create targeted drug delivery systems. Loaded with a neutral lipid orange dye, the HNPs were extensively characterized using various techniques and investigated for their uptake in human monocyte-derived macrophages (MDMs) using FC and CLSM. Moreover, the best-performing HNPs (i.e., HNP-COOH and HNP-RGD as well as HNP-RGD/COOH mixed) were loaded with the anti-inflammatory drug BRP-201 and prepared in two size ranges (dH ~140 nm and dH ~250 nm)...
January 28, 2024: Pharmaceutics
https://read.qxmd.com/read/38397918/conjecturing-about-small-molecule-agonists-and-antagonists-of-%C3%AE-4%C3%AE-1-integrin-from-mechanistic-insight-to-potential-therapeutic-applications
#22
REVIEW
Tingting He, Daria Giacomini, Alessandra Tolomelli, Monica Baiula, Luca Gentilucci
Integrins are heterodimeric cell-surface receptors that regulate cell-cell adhesion and cellular functions through bidirectional signaling. On the other hand, anomalous trafficking of integrins is also implicated in severe pathologies as cancer, thrombosis, inflammation, allergies, and multiple sclerosis. For this reason, they are attractive candidates as drug targets. However, despite promising preclinical data, several anti-integrin drugs failed in late-stage clinical trials for chronic indications, with paradoxical side effects...
January 30, 2024: Biomedicines
https://read.qxmd.com/read/38397461/enhanced-tumor-targeting-and-antitumor-activity-of-methylated-%C3%AE-cyclodextrin-threaded-polyrotaxanes-by-conjugating-cyclic-rgd-peptides
#23
JOURNAL ARTICLE
Shunyao Zhang, Atsushi Tamura, Nobuhiko Yui
We previously reported that acid-degradable methylated β-cyclodextrins (Me-β-CDs)-threaded polyrotaxanes (Me-PRXs) can induce autophagic cell death through endoplasmic reticulum (ER) stress-related autophagy, even in apoptosis-resistant cells. Hence, Me-PRXs show great potential as anticancer therapeutics. In this study, peptide-supermolecule conjugates were designed to achieve the targeted delivery of Me-PRX to malignant tumors. Arg-Gly-Asp peptides are well-known binding motifs of integrin αv β3 , which is overexpressed on angiogenic sites and many malignant tumors...
February 15, 2024: Biomolecules
https://read.qxmd.com/read/38390528/boosting-cartilage-repair-with-silk-fibroin-dna-hydrogel-based-cartilage-organoid-precursor
#24
JOURNAL ARTICLE
Congyi Shen, Jian Wang, Guangfeng Li, Shuyue Hao, Yan Wu, Peiran Song, Yafei Han, Mengmeng Li, Guangchao Wang, Ke Xu, Hao Zhang, Xiaoxiang Ren, Yingying Jing, Ru Yang, Zhen Geng, Jiacan Su
Osteoarthritis (OA), a common degenerative disease, is characterized by high disability and imposes substantial economic impacts on individuals and society. Current clinical treatments remain inadequate for effectively managing OA. Organoids, miniature 3D tissue structures from directed differentiation of stem or progenitor cells, mimic native organ structures and functions. They are useful for drug testing and serve as active grafts for organ repair. However, organoid construction requires extracellular matrix-like 3D scaffolds for cellular growth...
May 2024: Bioactive Materials
https://read.qxmd.com/read/38387712/therapeutic-effect-and-mechanism-of-action-of-pterostilbene-nano-drugs-in-dry-eye-models
#25
JOURNAL ARTICLE
Kexin Li, Meng Lin, Kaiyan Huang, Jiaxin Han, Linzhi Wei, Lijie Miao, Huijuan Chen, Qianwen Gong, Xingyi Li, Liang Hu
Dry eye disease is a multifactorial dysfunction of the tear film and ocular surface, with etiology involving inflammation and oxidative stress on the ocular surface. Pterostilbene (PS) is a secondary metabolite extracted from plants, which possesses remarkable anti-inflammatory and antioxidant effects. However, its application is limited by light instability and very poor water solubility. We modified fat-soluble PS into a biparental pterostilbene-glutaric anhydride-arginine-glycine-aspartic acid (PS-GA-RGD) nanomedicine by prodrug ligation of functional peptides...
February 20, 2024: Experimental Eye Research
https://read.qxmd.com/read/38387123/interactions-between-dna-and-the-acridine-intercalator-a-computational-study
#26
JOURNAL ARTICLE
Thaynara Guimarães Miranda, Nicolas Nascimento Ciribelli, Murielly Fernanda Ribeiro Bihain, Anna Karla Dos Santos Pereira, Grasiele Soares Cavallini, Douglas Henrique Pereira
Cancer is a global public health problem characterized by deviations in the mechanisms that control cell proliferation, resulting in mutations and variations in the structure of DNA. The mechanisms of action of chemotherapeutic drugs are related to their interactions and binding with DNA; consequently, the development of antineoplastic agents that target DNA has extensively focused on use of acridine, a heterocyclic molecule that binds to deoxyribonucleic acid via intercalation, a process that modifies DNA and makes replication impossible...
February 12, 2024: Computational Biology and Chemistry
https://read.qxmd.com/read/38376806/synthesis-preclinical-and-initial-clinical-evaluation-of-integrin-%C3%AE-v-%C3%AE-3-and-gastrin-releasing-peptide-receptor-grpr-dual-targeting-radiotracer-68-ga-ga-rgd-rm26-03
#27
JOURNAL ARTICLE
Xuejun Wen, Rongxi Wang, Pengfei Xu, Mengqi Shi, Qingyao Shang, Xueyuan Zeng, Xinying Zeng, Jia Liu, Xin Wang, Zhaohui Zhu, Zhide Guo, Xiaoyuan Chen, Jingjing Zhang
UNLABELLED: Integrin receptor αv β3 and gastrin-releasing peptide receptor (GRPR) expression of tumors could be detected using PET imaging with radiolabeled Arg-Gly-Asp (RGD) and the antagonistic bombesin analog RM26, respectively. The purpose of this study was to investigate the dual receptor-targeting property of the heterodimer RGD-RM26-03 (denoted as LNC1015), demonstrate the tumor diagnostic value of [68 Ga]Ga-LNC1015 in preclinical experiments, and evaluate its preliminary clinical feasibility...
February 20, 2024: European Journal of Nuclear Medicine and Molecular Imaging
https://read.qxmd.com/read/38374394/a-dual-crosslinking-electroactive-hydrogel-based-on-gelatin-methacrylate-and-dibenzaldehyde-terminated-telechelic-polyethylene-glycol-for-3d-bio-printing
#28
JOURNAL ARTICLE
Yulong Wang, Songsong Yang, Heqing Cai, Hailong Hu, Kun Hu, Zhicheng Sun, Ruping Liu, Yen Wei, Lu Han
Gelatin was widely used as scaffold materials in 3D bio-printing due to its excellent bioactivity and availability and especially that their arginine-glycine-aspartic acid (RGD) sequences could efficiently promote cell adhesion and proliferation. In this study, an electroactive and 3D bio-printable hydrogel was prepared through a two-step chemical cross-linking process. Specifically, residual free amino groups of methacrylated gelatin (GelMA) were cross-linked with the aldehyde groups of dibenzaldehyde-terminated telechelic polyethylene glycol (DF-PEG) via Schiff base bonds, forming a gel at 37 °C...
February 19, 2024: Scientific Reports
https://read.qxmd.com/read/38372696/a-dual-targeted-gd-based-contrast-agent-for-magnetic-resonance-imaging-in-tumor-diagnosis
#29
JOURNAL ARTICLE
Lin Yu, Kaiqi Zhang, Yiyao Zhang, Xun Wang, Peng Dong, Yanming Ge, Guangmao Ni, Zan Liu, Yanhui Zhang
Enhanced magnetic resonance imaging (MRI) has important clinical value in the diagnosis of tumors. Much effort has been made to improve the relaxivity and specificity of contrast agents (CAs) in tumor diagnosis over the past few decades. However, there is still a lack of CAs which not only enhance the signal intensity of tumors rather than surrounding tissues in MRI but also maintain a high signal intensity prolonged for a long time. Herein, we synthesized a dual-targeted CA, RGD-(DOTA-Gd)-TPP (RDP), in which RGD is used to target the αv β3 integrin receptor overexpressed in tumor cells and TPP is used to bind to a mitochondrion further...
February 19, 2024: Journal of Materials Chemistry. B, Materials for Biology and Medicine
https://read.qxmd.com/read/38370345/ligand-presentation-inside-protein-crystal-nanopores-tunable-interfacial-adhesion-noncovalently-modulates-cell-attachment
#30
JOURNAL ARTICLE
Dafu Wang, Mohammadhasan Hedayati, Julius D Stuart, Liszt Y C Madruga, Ketul C Popat, Christopher D Snow, Matt J Kipper
Protein crystals with sufficiently large solvent pores can non-covalently adsorb polymers in the pores. In principle, if these polymers contain cell adhesion ligands, the polymer-laden crystals could present ligands to cells with tunable adhesion strength. Moreover, porous protein crystals can store an internal ligand reservoir, so that the surface can be replenished. In this study, we demonstrate that poly(ethylene glycol) terminated with a cyclic cell adhesion ligand peptide (PEG-RGD) can be loaded into porous protein crystals by diffusion...
December 2023: Materials today. Nano
https://read.qxmd.com/read/38361795/a-novel-cartilage-targeting-mof-hmme-rgd-sonosensitizer-combined-with-sonodynamic-therapy-to-enhance-chondrogenesis-and-cartilage-regeneration
#31
JOURNAL ARTICLE
Shanchao Luo, Yifeng Shang, Zainen Qin, Bo Zhou, Chun Lu, Yangyang Qu, Jinmin Zhao, Ruiming Liang, Li Zheng, Shixing Luo
Articular cartilage regeneration is still a difficult task due to the cartilage's weak capacity for self-healing and the effectiveness of the available therapies. The engineering of cartilage tissue has seen widespread use of stem cell-based therapies. However, efficient orientation of line-specific bone marrow mesenchymal stem cells (BMSCs) to chondrogenesis and maintenance of chondrogenic differentiation challenged stem cell-based therapy. Herein, we developed a Fe-based metal-organic framework (MOF) loaded with hematoporphyrin monomethyl ether (HMME) and cartilage-targeting arginine-aspartate-glycine (RGD) peptide to form MOF-HMME-RGD sonosensitizer to regulate BMSCs chondrogenic differentiation for cartilage regeneration via the modulation of reactive oxygen species (ROS)...
2024: Frontiers in Bioengineering and Biotechnology
https://read.qxmd.com/read/38349028/rgd-peptide-in-cancer-targeting-benefits-challenges-solutions-and-possible-integrin-rgd-interactions
#32
REVIEW
Hossein Javid, Mahsa Akbari Oryani, Nastaran Rezagholinejad, Ali Esparham, Mahboubeh Tajaldini, Mehdi Karimi-Shahri
RGD peptide can be found in cell adhesion and signaling proteins, such as fibronectin, vitronectin, and fibrinogen. RGD peptides' principal function is to facilitate cell adhesion by interacting with integrin receptors on the cell surface. They have been intensively researched for use in biotechnology and medicine, including incorporation into biomaterials, conjugation to medicinal molecules or nanoparticles, and labeling with imaging agents. RGD peptides can be utilized to specifically target cancer cells and the tumor vasculature by engaging with these integrins, improving drug delivery efficiency and minimizing adverse effects on healthy tissues...
January 2024: Cancer Medicine
https://read.qxmd.com/read/38343773/photonic-control-of-ligand-nanospacing-in-self-assembly-regulates-stem-cell-fate
#33
JOURNAL ARTICLE
Sungkyu Lee, Jounghyun Yoo, Gunhyu Bae, Ramar Thangam, Jeongyun Heo, Jung Yeon Park, Honghwan Choi, Chowon Kim, Jusung An, Jungryun Kim, Kwang Rok Mun, Seungyong Shin, Kunyu Zhang, Pengchao Zhao, Yuri Kim, Nayeon Kang, Seong-Beom Han, Dahee Kim, Jiwon Yoon, Misun Kang, Jihwan Kim, Letao Yang, Solmaz Karamikamkar, Jinjoo Kim, Yangzhi Zhu, Alireza Hassani Najafabadi, Guosheng Song, Dong-Hwee Kim, Ki-Bum Lee, Soong Ju Oh, Hyun-Do Jung, Hyun-Cheol Song, Woo Young Jang, Liming Bian, Zhiqin Chu, Juyoung Yoon, Jong Seung Kim, Yu Shrike Zhang, Yongju Kim, Ho Seong Jang, Sehoon Kim, Heemin Kang
Extracellular matrix (ECM) undergoes dynamic inflation that dynamically changes ligand nanospacing but has not been explored. Here we utilize ECM-mimicking photocontrolled supramolecular ligand-tunable Azo+ self-assembly composed of azobenzene derivatives (Azo+ ) stacked via cation-π interactions and stabilized with RGD ligand-bearing poly(acrylic acid). Near-infrared-upconverted-ultraviolet light induces cis -Azo+ -mediated inflation that suppresses cation-π interactions, thereby inflating liganded self-assembly...
April 2024: Bioactive Materials
https://read.qxmd.com/read/38341468/synthesis-molecular-docking-and-dft-analysis-of-novel-bis-schiff-base-derivatives-with-thiobarbituric-acid-for-%C3%AE-glucosidase-inhibition-assessment
#34
JOURNAL ARTICLE
Saba Gul, Faheem Jan, Aftab Alam, Abdul Shakoor, Ajmal Khan, Abdullah F AlAsmari, Fawaz Alasmari, Momin Khan, Li Bo
A library of novel bis-Schiff base derivatives based on thiobarbituric acid has been effectively synthesized by multi-step reactions as part of our ongoing pursuit of novel anti-diabetic agents. All these derivatives were subjected to in vitro α-glucosidase inhibitory potential testing after structural confirmation by modern spectroscopic techniques. Among them, compound 8 (IC50  = 0.10 ± 0.05 µM), and 9 (IC50  = 0.13 ± 0.03 µM) exhibited promising inhibitory activity better than the standard drug acarbose (IC50  = 0...
February 10, 2024: Scientific Reports
https://read.qxmd.com/read/38335948/selective-induction-of-molecular-assembly-to-tissue-level-anisotropy-on-peptide-based-optoelectronic-cardiac-biointerfaces
#35
JOURNAL ARTICLE
Ze-Fan Yao, Yuyao Kuang, Hao-Tian Wu, Emil Lundqvist, Xin Fu, Natalie Celt, Jian Pei, Albert Yee, Herdeline Ann M Ardoña
The conduction efficiency of ions in excitable tissues and of charged species in organic conjugated materials both benefit from having ordered domains and anisotropic pathways. In this study, we present a photocurrent-generating cardiac biointerface that investigates the sensitivity of cardiomyocytes to geometrically comply to biomacromolecular cues differentially assembled on a conductive nanogrooved substrate. Through a polymeric surface-templated approach, photoconductive substrates with symmetric peptide-quaterthiophene (4T)-peptide units assembled as 1D nanostructures on nanoimprinted polyalkylthiophene (P3HT) surface are developed...
February 9, 2024: Advanced Materials
https://read.qxmd.com/read/38334981/mechanism-of-rgd-conjugated-nanodevice-binding-to-its-target-protein-integrin-%C3%AE-v-%C3%AE-3-by-atomistic-molecular-dynamics-and-machine-learning
#36
JOURNAL ARTICLE
Giulia Frigerio, Edoardo Donadoni, Paulo Siani, Jacopo Vertemara, Stefano Motta, Laura Bonati, Luca De Gioia, Cristiana Di Valentin
Active targeting strategies have been proposed to enhance the selective uptake of nanoparticles (NPs) by diseased cells, and recent experimental findings have proven the effectiveness of this approach. However, no mechanistic studies have yet revealed the atomistic details of the interactions between ligand-activated NPs and integrins. As a case study, here we investigate, by means of advanced molecular dynamics simulations (MD) and machine learning methods (namely equilibrium MD, binding free energy calculations and training of self-organized maps), the interaction of a cyclic-RGD-conjugated PEGylated TiO2 NP (the nanodevice) with the extracellular segment of integrin αV β3 (the target), the latter experimentally well-known to be over-expressed in several solid tumors...
February 9, 2024: Nanoscale
https://read.qxmd.com/read/38334590/imaging-of-endometriotic-lesions-using-crgd-mn-probe-in-a-mouse-model-of-endometriosis
#37
JOURNAL ARTICLE
Nazanin Talebloo, M Ariadna Ochoa Bernal, Elizabeth Kenyon, Christiane L Mallett, Sujan Kumar Mondal, Asgerally Fazleabas, Anna Moore
Approximately 10% of women suffer from endometriosis during their reproductive years. This disease is a chronic debilitating condition whose etiology for lesion implantation and survival heavily relies on adhesion and angiogenic factors. Currently, there are no clinically approved agents for its detection. In this study, we evaluated cRGD-peptide-conjugated nanoparticles (RGD-Cy5.5-MN) to detect lesions using magnetic resonance imaging (MRI) in a mouse model of endometriosis. We utilized a luciferase-expressing murine suture model of endometriosis...
February 5, 2024: Nanomaterials
https://read.qxmd.com/read/38332815/photosensitizer-singlet-oxygen-sensor-conjugated-silica-nanoparticles-for-photodynamic-therapy-and-bioimaging
#38
JOURNAL ARTICLE
Jeladhara Sobhanan, Kenji Ono, Takuya Okamoto, Makoto Sawada, Paul S Weiss, Vasudevanpillai Biju
Intracellular singlet oxygen (1 O2 ) generation and detection help optimize the outcome of photodynamic therapy (PDT). Theranostics programmed for on-demand phototriggered 1 O2 release and bioimaging have great potential to transform PDT. We demonstrate an ultrasensitive fluorescence turn-on sensor-sensitizer-RGD peptide-silica nanoarchitecture and its 1 O2 generation-releasing-storing-sensing properties at the single-particle level or in living cells. The sensor and sensitizer in the nanoarchitecture are an aminomethyl anthracene (AMA)-coumarin dyad and a porphyrin or CdSe/ZnS quantum dots (QDs), respectively...
February 7, 2024: Chemical Science
https://read.qxmd.com/read/38330994/preparation-in-vitro-anti-tumor-activity-and-in-vivo-pharmacokinetics-of-rgd-decorated-liposomes-loaded-with-shikonin
#39
JOURNAL ARTICLE
Xianchun Wen, Jiping Li, Hao Zhang, Xinliang Mao, Huilin Deng, Li Fan, Liling Yue, Chengchong Li, Siwen Pan
Shikonin (SHK) has been evidenced to possess effects against various cancer cells. However, poor aqueous solubility and high toxicity restrict its application. In the study, RGD-decorated liposomes loaded with SHK (RGD-Lipo-SHK) were prepared via thin-film hydration method. Characterization and cellular uptake of liposomes was evaluated. Cytotoxicity of blank liposomes and different SHK formulations was measured against breast cancer cells (MDA-MB-231, MCF-7, and MCF-10A). Anti-tumor effects and pharmacokinetic parameters of different SHK formulations were appraised in tumor spheroids and in rat model, respectively...
February 8, 2024: Pharmaceutical Development and Technology
https://read.qxmd.com/read/38330637/evaluation-of-targeting-%C3%AE-v-%C3%AE-3-in-breast-cancers-using-rgd-peptide-based-agents
#40
JOURNAL ARTICLE
Anders Josefsson, Angel G Cortez, Jing Yu, Sunipa Majumdar, Abhinav Bhise, Robert F Hobbs, Jessie R Nedrow
Patients with HER2-positive and triple negative breast cancer (TNBC) are associated with increased risk to develop metastatic disease including reoccurring disease that is resistant to standard and targeted therapies. The αV β3 has been implicated in BC including metastatic disease. The aims of this study were to investigate the potential of αV β3 -targeted peptides to deliver radioactive payloads to BC tumors expressing αV β3 on the tumor cells or limited to the tumors' neovascular...
February 6, 2024: Nuclear Medicine and Biology
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