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Cell penetrating peptide

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https://www.readbyqxmd.com/read/29790795/octa-arginine-modified-poly-amidoamine-dendrimers-for-improved-delivery-and-cytotoxic-effect-of-paclitaxel-in-cancer
#1
Sri Vishnu Kiran Rompicharla, Preeti Kumari, Balaram Ghosh, Swati Biswas
Cell penetrating peptides (CPP) have the ability to penetrate the cell membrane and have been associated with various cargos for their facile intracellular translocation. The current study involves the synthesis of a CPP, octa-arginine (R8)-modified poly(amidoamine) dendrimer of generation 4 (G4), which has additionally been PEGylated and conjugated to the poorly soluble anticancer drug, paclitaxel (PTX). The synthesized dendrimer conjugates were characterized by proton nuclear magnetic resonance (1H-NMR) Spectroscopy and zeta potential measurements and evaluated in vitro in cell monolayers and 3D spheroids...
May 23, 2018: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/29790744/myristic-acid-modified-da7r-peptide-for-whole-process-glioma-targeted-drug-delivery
#2
Man Ying, Songli Wang, Mingfei Zhang, Ruifeng Wang, Hangchang Zhu, Huitong Ruan, Danni Ran, Zhilan Chai, Xiaoyi Wang, Weiyue Lu
Clinical treatment of aggressive glioma has been a great challenge, mainly due to the complexity of glioma microenvironment and the existence of blood-brain tumor barrier (BBTB)/blood-brain barrier (BBB), which severely hamper the effective accumulation of most therapeutic agents in glioma region. Additionally, vasculogenic mimicry (VM), angiogenesis and glioma stem cells (GSC) in malignant glioma also lead to the failure of clinical therapy. To address the aforementioned issues, a whole-process glioma targeted drug delivery strategy was proposed...
May 23, 2018: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/29790738/design-and-development-of-polysaccharide-doxorubicin-peptide-bioconjugates-for-dual-synergistic-effects-of-integrin-targeted-and-cell-penetrating-peptides-for-cancer-chemotherapy
#3
Alexandra A P Mansur, Sandhra Maria Carvalho, Zelia Ines Portela Lobato, Maria de Fátima Leite, Armando da Silva Cunha, Herman S Mansur
Polymer-drug conjugation is an attractive approach for target delivering insoluble and highly toxic drugs to tumor sites to overcome the side-effects caused by cancer chemotherapy. In this study we designed and synthesized novel polymer-drug-peptide conjugates for improved specificity on targeting cancer cells. Chemically modified polysaccharide, carboxymethylcellulose (CMC), was conjugated with doxorubicin (DOX) anticancer drug by amide bonds and dually biofunctionalized with integrin-target receptor tripeptide (RGD) and L-arginine (R) as cell-penetrating amino acid for synergistic targeting and enhancing internalization by cancer cells...
May 23, 2018: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/29790494/channel-current-analysis-estimates-the-pore-formation-and-the-penetration-of-transmembrane-peptides
#4
Yusuke Sekiya, Shungo Sakashita, Keisuke Shimizu, Kenji Usui, Ryuji Kawano
We measured the current signal of the transmembrane model peptides using the barrel-stave, toroidal pore, and penetration models in order to establish a precise assignment of the channel signals. In addition, we analyzed the spike signals to estimate the membrane penetration of model cell-penetration peptides of different lengths.
May 23, 2018: Analyst
https://www.readbyqxmd.com/read/29789580/the-effects-of-anti-lap-monoclonal-antibody-down-regulation-of-cd4-lap-t-cells-on-allogeneic-corneal-transplantation-in-mice
#5
Shang Li, Hongshuang Lu, Ruti Sella, Wei Zhang, Hongwei Dong, Chungang Guo, Natalie A Afshari, Zhiqiang Pan, Ying Jie
CD4+latency-associated peptide (LAP)+ T cells are a newly discovered T cell subset with suppressive function on immune responses. In this study, we investigate the role of CD4+LAP+ T cells on mice corneal allograft survival by down-regulating their expression using anti-LAP mAb. We show that a blockage of LAP leads to a decrease in the percentage of T cells expressing CD4+Foxp3+, CD4+GARP+, CD4+LAP+ and CD4+IL-10+ in the lymph nodes and spleens of mice undergoing orthotopic penetrating transplantation of corneal allograft, without affecting corneal graft survival...
May 22, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29787950/macroporous-silica-nanoparticles-for-delivering-bcl2-function-converting-peptide-to-treat-multidrug-resistant-cancer-cells
#6
Weixia Xu, Pengjin Ge, Boning Niu, Xiaokun Zhang, Jie Liu, Jingjing Xie
The abundance of B cell lymphoma gene 2 (Bcl-2) is closely correlated with the resistance of cancer cells to chemotherapeutic agents, and a peptide derived from orphan nuclear receptor Nur77 can convert Bcl-2 from a protector to a killer of cancer cells. However, successful application of the Bcl-2-converting peptide to treat drug-resistant cancer cells depends on an efficient delivery carrier. Mesoporous silica nanoparticles (MSNs) have been extensively studied as promising candidates for small molecule drug delivery...
May 15, 2018: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/29787814/lipid-modified-cell-penetrating-peptide-based-self-assembly-micelles-for-co-delivery-of-narciclasine-and-siulk1-in-hepatocellular-carcinoma-therapy
#7
Xiaoyun Wang, Fengbo Wu, Guoyou Li, Nan Zhang, Xiangrong Song, Yu Zheng, Changyang Gong, Bo Han, Gu He
Hepatocellular carcinoma (HCC) is the most frequent type of primary liver cancer, and one therapeutic approach is to target both the AMPK and autophagy pathways in order to synergistically promote programmed cell death. Here, a series of amphiphilic, lipid-modified cell-penetrating peptides were synthesized and allowed to self-assemble into micelles loaded with the AMPK activator narciclasine (Narc) and short interfering RNA targeting the unc-51-like kinase 1 (siULK1). The size of these micelles, their efficiency of transfection into cells, and their ability to release drug or siRNA cargo in vitro were pH-sensitive, such that drug release was facilitated in the acidic microenvironment of the tumor...
May 19, 2018: Acta Biomaterialia
https://www.readbyqxmd.com/read/29780514/construction-of-histidine-containing-hydrocarbon-stapled-cell-penetrating-peptides-for-in-vitro-and-in-vivo-delivery-of-sirnas
#8
Soonsil Hyun, Yoonhwa Choi, Ha Neul Lee, Changki Lee, Donghoon Oh, Dong-Ki Lee, Changjin Lee, Yan Lee, Jaehoon Yu
A hydrocarbon stapled peptide based strategy was used to develop an optimized cell penetrating peptide for siRNA delivery. Various stapled peptides, having amphipathic Leu- and Lys-rich regions, were prepared and their cell penetrating potentials were evaluated. One peptide, stEK, was found to have high cell penetration and siRNA delivery abilities at low nanomolar concentrations. In order to improve its ability to promote gene silencing, stEK was modified by replacing several Lys residues with His moieties...
April 21, 2018: Chemical Science
https://www.readbyqxmd.com/read/29780163/heteromerization-of-%C3%AE-opioid-receptor-and-cholecystokinin-b-receptor-through-the-third-transmembrane-domain-of-the-%C3%AE-opioid-receptor-contributes-to-the-anti-opioid-effects-of-cholecystokinin-octapeptide
#9
Yin Yang, Qian Li, Qi-Hua He, Ji-Sheng Han, Li Su, You Wan
Activation of the cholecystokinin type B receptor (CCKBR) by cholecystokinin octapeptide (CCK-8) inhibits opioid analgesia. Chronic opiate treatment leads to an increase in the CCK-8 concentration and thus enhances the antagonism of CCK-8 against opioid analgesia; the underlying molecular mechanisms remain of great interest. In the present study, we validated the colocalization of the μ-opioid receptor (MOR) and CCKBR in pain signal transmission-related spinal cord dorsal horn and dorsal root ganglion neurons of rats...
May 21, 2018: Experimental & Molecular Medicine
https://www.readbyqxmd.com/read/29777875/switching-cell-penetrating-and-cxcr4-binding-activities-of-nanoscale-organized-arginine-rich-peptides
#10
Marianna Teixeira de Pinho Favaro, Naroa Serna, Laura Sánchez-García, Rafael Cubarsi, Mónica Roldán, Alejandro Sánchez-Chardi, Ugutz Unzueta, Ramón Mangues, Neus Ferrer-Miralles, Adriano Rodrigues Azzoni, Esther Vázquez, Antonio Villaverde
Arginine-rich protein motifs have been described as potent cell-penetrating peptides (CPPs) but also as rather specific ligands of the cell surface chemokine receptor CXCR4, involved in the infection by the human immunodeficiency virus (HIV). Polyarginines are commonly used to functionalize nanoscale vehicles for gene therapy and drug delivery, aimed to enhance cell penetrability of the therapeutic cargo. However, under which conditions these peptides do act as either unspecific or specific ligands is unknown...
May 16, 2018: Nanomedicine: Nanotechnology, Biology, and Medicine
https://www.readbyqxmd.com/read/29774608/virion-like-membrane-breaking-nanoparticles-with-tumor-activated-cell-and-tissue-dual-penetration-conquer-impermeable-cancer
#11
Xiao Zhang, Xianghui Xu, Yachao Li, Cheng Hu, Zhijun Zhang, Zhongwei Gu
Poor drug penetration into tumor cells and tissues is a worldwide difficulty in cancer therapy. A strategy is developed for virion-like membrane-breaking nanoparticles (MBNs) to smoothly accomplish tumor-activated cell-and-tissue dual-penetration for surmounting impermeable drug-resistant cancer. Tailor-made dendritic arginine-rich peptide prodrugs are designed to mimic viral protein transduction domains and globular protein architectures. Attractively, these protein mimics self-assemble into virion-like nanoparticles in aqueous solution, having highly ordered secondary structure...
May 17, 2018: Advanced Materials
https://www.readbyqxmd.com/read/29770868/effect-of-dimerized-melittin-on-gastric-cancer-cells-and-antibacterial-activity
#12
Elaheh Jamasbi, Sasidharan S Lucky, Wenyi Li, Mohammed Akhter Hossain, Ponnampalam Gopalakrishnakone, Frances Separovic
Melittin is the peptide toxin found in bee venom and is effective against cancer cells. To enhance its activity, a branched dimeric form of melittin was designed. The monomeric form of the peptide was more cytotoxic against gastric cancer cells at low concentrations (1-5 μM) than the dimer form, while the cytotoxic effect was comparable at higher concentrations (10 μM). Confocal microscopy showed that both the monomer and dimer forms of melittin with fluorescent label at the C terminus penetrated the cytoplasm and localized at the cell nucleus and disrupted the cell membrane...
May 16, 2018: Amino Acids
https://www.readbyqxmd.com/read/29769639/a-novel-cell-penetrating-peptide-protects-against-neuron-apoptosis-after-cerebral-ischemia-by-inhibiting-the-nuclear-translocation-of-annexin-a1
#13
Xing Li, Lu Zheng, Qian Xia, Lu Liu, Meng Mao, Huijuan Zhou, Yin Zhao, Jing Shi
Nuclear translocation of annexin A1 (ANXA1) has recently been reported to participate in neuronal apoptosis after cerebral ischemia. Prevention of the nuclear translocation of ANXA1 should therefore inhibit neuronal apoptosis and protect against cerebral stroke. Here, we found that, in the repeat III domain of ANXA1, the amino-acid residues from R228 to F237 function as a unique nuclear translocation signal (NTS) and are required for nuclear translocation of ANXA1. Intriguingly, we synthesized a cell-penetrating peptide derived by conjugating the trans-activator of transcription (Tat) domain to the NTS sequence...
May 16, 2018: Cell Death and Differentiation
https://www.readbyqxmd.com/read/29767957/magnetic-manipulation-of-reversible-nanocaging-controls-in-vivo-adhesion-and-polarization-of-macrophages
#14
Heemin Kang, Hee Joon Jung, Sung Kyu Kim, Dexter Siu Hong Wong, Sien Lin, Gang Li, Vinayak P Dravid, Liming Bian
Macrophages are key immune cells that perform various physiological functions, such as the maintenance of homeostasis, host defense, disease progression, and tissue regeneration. Macrophages adopt distinctly polarized phenotypes, such as pro-inflammatory M1 phenotype or anti-inflammatory (pro-healing) M2 phenotype, to execute disparate functions. The remotely controlled reversible uncaging of bioactive ligands, such as Arg-Gly-Asp (RGD) peptide, is an appealing approach for temporally regulating the adhesion and resultant polarization of macrophages on the implants in vivo...
May 16, 2018: ACS Nano
https://www.readbyqxmd.com/read/29764120/multi-arm-nanoconjugates-for-cancer-cell-targeted-delivery-of-photosensitizers
#15
Yan Zhao, Fang Li, Chengqiong Mao, Xin Ming
Photodynamic therapy, a procedure that uses a photosensitizer to enable light therapy selectively at diseased sites, remains underutilized in oncological clinic. To further improve its cancer selectivity, we developed a polymeric nanosystem by conjugating a photosensitizer IRDye 700DX (IR700) and cancer targeting RGD peptide to 8-arm polyethylene glycol (PEG). The resulting nanoconjugates (RGD-8PEG-IR700) exhibited a hydrodynamic size of 6.6 nm with narrow distribution of size. The targeted nanoconjugates showed significantly higher intracellular uptake of IR700 in integrin αvβ3-expressing A375 and SKOV3 cells when compared with non-targeted control 8PEG-IR700, and excess amount of RGD peptides could abolish this enhancement, indicating a receptor-medicated uptake mechanism for the targeted polymer conjugates...
May 16, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29763715/near-infrared-light-activated-red-emitting-upconverting-nanoplatform-for-t-1-weighted-magnetic-resonance-imaging-and-photodynamic-therapy
#16
Xiang-Long Tang, Jun Wu, Ben-Lan Lin, Sheng Cui, Hong-Mei Liu, Ru-Tong Yu, Xiao-Dong Shen, Ting-Wei Wang, Wei Xia
Photodynamic therapy (PDT) has increasingly become an efficient and attractive cancer treatment modality based on reactive oxygen species (ROS) that can induce tumor death after irradiation with ultraviolet or visible light. Herein, to overcome the limited tissue penetration in traditional PDT, a novel near-infrared (NIR) light-activated NaScF4 : 40% Yb, 2% Er@CaF2 upconversion nanoparticle (rUCNP) is successfully designed and synthesized. Chlorin e6, a photosensitizer and a chelating agent for Mn2+ , is loaded into human serum albumin (HSA) that further conjugates onto rUCNPs...
May 12, 2018: Acta Biomaterialia
https://www.readbyqxmd.com/read/29762718/cell-penetrating-thiazole-peptides-inhibit-c-myc-expression-via-site-specific-targeting-of-c-myc-g-quadruplex
#17
Debasish Dutta, Manish Debnath, Diana Müller, Rakesh Paul, Tania Das, Irene Bessi, Harald Schwalbe, Jyotirmayee Dash
The structural differences among different G-quadruplexes provide an opportunity for site-specific targeting of a particular G-quadruplex structure. However, majority of G-quadruplex ligands described thus far show little selectivity among different G-quadruplexes. In this work, we delineate the design and synthesis of a crescent-shaped thiazole peptide that preferentially stabilizes c-MYC quadruplex over other promoter G-quadruplexes and inhibits c-MYC oncogene expression. Biophysical analysis such as Förster resonance energy transfer (FRET) melting and fluorescence spectroscopy show that the thiazole peptide TH3 can selectively interact with the c-MYC G-quadruplex over other investigated G-quadruplexes and duplex DNA...
May 14, 2018: Nucleic Acids Research
https://www.readbyqxmd.com/read/29757394/a-barley-powdery-mildew-fungus-non-autonomous-retrotransposon-encodes-a-peptide-that-supports-penetration-success-on-barley
#18
Mathias Nottensteiner, Bernd Zechmann, Christopher McCollum, Ralph Hückelhoven
Pathogens overcome plant immunity by the means of secreted effectors. Host effector targets often act in pathogen defense but might also support fungal accommodation or nutrition. The barley ROP GTPase HvRACB is involved in accommodation of fungal haustoria of the powdery mildew fungus Blumeria graminis f.sp. hordei (Bgh) in barley epidermal cells. We found that HvRACB interacts with the ROP-interactive peptide 1 (ROPIP1) that is encoded on the active non-long terminal repeat retroelement Eg-R1 of Bgh. Over-expression of ROPIP1 in barley epidermal cells and host-induced post-transcriptional gene silencing (HIGS) of ROPIP1 suggested that ROPIP1 is involved in virulence of Bgh...
May 11, 2018: Journal of Experimental Botany
https://www.readbyqxmd.com/read/29757340/polyethylene-glycol-and-octa-arginine-dual-functionalized-nanographene-oxide-an-optimization-for-efficient-nucleic-acid-delivery
#19
Rana Imani, Satya Prakash, Hojatollah Vali, Shahab Faghihi
The successful application of nucleic acid-based therapy for the treatment of various cancers is largely dependent on a safe and efficient delivery system. A dual-functionalized graphene oxide (GO)-based nanocarrier with the conjugation of aminated-polyethylene glycol (PEG-diamine) and octa-arginine (R8) for the intracellular delivery of nucleic acids is proposed. The functionalized sites are covalently co-conjugated and the PEG : R8 molar ratio is optimized at 10 : 1 to achieve a hydrocolloidally stable size of 252 ± 2...
May 14, 2018: Biomaterials Science
https://www.readbyqxmd.com/read/29747160/targeting-liver-cancer-and-associated-pathologies-in-mice-with-a-mitochondrial-vdac1-based-peptide
#20
Srinivas Pittala, Yakov Krelin, Varda Shoshan-Barmatz
Hepatocellular carcinoma (HCC) is the third most lethal cancer worldwide. Despite progress in identifying risk factors, the incidence of HCC is increasing. Moreover, therapeutic options are limited and survival is poor. Therefore, alternative and innovative therapeutic strategies are urgently required. R-Tf-D-LP4, a cell-penetrating peptide derived from the mitochondrial multifunctional protein the voltage-dependent anion channel (VDAC1), is identified here as a highly effective liver cancer treatment. Recently, we demonstrated that R-Tf-D-LP4 induced apoptosis and inhibited tumor growth in mouse models...
May 7, 2018: Neoplasia: An International Journal for Oncology Research
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