abstract：:Glutamic acid is a commonly used linker to form dimeric peptides with enhanced binding affinity than their corresponding monomeric counterparts. We have previously labeled NOTA-Bn-NCS-PEG3-E[c(RGDyK)]2 (NOTA-PRGD2) [1] with [(18)F]AlF and (68)Ga for imaging tumor angiogenesis. The p-SCN-Bn-NOTA was attached to E[c(RGD...

journal_title：Molecular pharmaceutics

authors： Lang L,Ma Y,Kiesewetter DO,Chen X

更新日期：2014-11-03 00:00:00

abstract：:Doxorubicin (DOX) is one of the most commonly used antineoplastic agents, but its clinical application is oftentimes coupled with severe side effects. Selective delivery of DOX to tumors via nanosized drug carrier represents an attractive approach to this problem. Previously, we developed a dual functional nanomicella...

journal_title：Molecular pharmaceutics

authors： Lu J,Zhao W,Huang Y,Liu H,Marquez R,Gibbs RB,Li J,Venkataramanan R,Xu L,Li S,Li S

更新日期：2014-11-03 00:00:00

abstract：:Tumor endothelial marker 8 (TEM8) is a cell surface receptor that is highly expressed in a variety of human tumors and promotes tumor angiogenesis and cell growth. Antibodies targeting TEM8 block tumor angiogenesis in a manner distinct from the VEGF receptor pathway. Development of a TEM8 imaging agent could aid in pa...

journal_title：Molecular pharmaceutics

authors： Kuo F,Histed S,Xu B,Bhadrasetty V,Szajek LP,Williams MR,Wong K,Wu H,Lane K,Coble V,Vasalatiy O,Griffiths GL,Paik CH,Elbuluk O,Szot C,Chaudhary A,St Croix B,Choyke P,Jagoda EM

更新日期：2014-11-03 00:00:00

abstract：:Generation 5 poly(amidoamine) (G5 PAMAM) methotrexate (MTX) conjugates employing two small molecular linkers, G5-(COG-MTX)n, G5-(MFCO-MTX)n were prepared along with the conjugates of the G5-G5 (D) dimer, D-(COG-MTX)n, D-(MFCO-MTX)n. The monomer G5-(COG-MTX)n conjugates exhibited only a weak, rapidly reversible binding...

journal_title：Molecular pharmaceutics

authors： van Dongen MA,Rattan R,Silpe J,Dougherty C,Michmerhuizen NL,Van Winkle M,Huang B,Choi SK,Sinniah K,Orr BG,Banaszak Holl MM

更新日期：2014-11-03 00:00:00

abstract：:Lipophilic cations such as phosphonium salts can accumulate in mitochondria of heart in response to the negative inner-transmembrane potentials. Two phosphonium salts [(18)F]FMBTP and [(18)F]mFMBTP were prepared and evaluated as potential myocardial perfusion imaging (MPI) agents in this study. The cations were radiol...

journal_title：Molecular pharmaceutics

authors： Zhao Z,Yu Q,Mou T,Liu C,Yang W,Fang W,Peng C,Lu J,Liu Y,Zhang X

更新日期：2014-11-03 00:00:00

abstract：:The objective of this work was to investigate the feasibility of using a novel granulation technique, namely, fluidized hot melt granulation (FHMG), to prepare gastroretentive extended-release floating granules. In this study we have utilized FHMG, a solvent free process in which granulation is achieved with the aid o...

journal_title：Molecular pharmaceutics

authors： Zhai H,Jones DS,McCoy CP,Madi AM,Tian Y,Andrews GP

更新日期：2014-10-06 00:00:00

abstract：:The objective of this study is to synthesize and evaluate acute toxicity of the bacterial cellulose (BC)/acrylamide (Am) hydrogels as noncytotoxic and biocompatible oral drug delivery vehicles. A novel series of solubilized BC/Am hydrogels were synthesized using a microwave irradiation method. The hydrogels were chara...

journal_title：Molecular pharmaceutics

authors： Pandey M,Mohamad N,Amin MC

更新日期：2014-10-06 00:00:00

abstract：:Solvation of drugs in the core (C) and headgroup (H) strata of phospholipid bilayers affects their physiological transport rates and accumulation. These characteristics, especially a complete drug distribution profile across the bilayer strata, are tedious to obtain experimentally, to the point that even simplified pr...

journal_title：Molecular pharmaceutics

authors： Natesan S,Lukacova V,Peng M,Subramaniam R,Lynch S,Wang Z,Tandlich R,Balaz S

更新日期：2014-10-06 00:00:00

abstract：:The blood-brain barrier (BBB) prevents most drugs from reaching the site of central nervous system (CNS) diseases, intensively confining the therapeutic efficiency. Angiopep-2 (here termed (L)Angiopep), which is a 19-mer peptide derived from human Kunitz domain, can trigger transcytosis and traverse the BBB by recogni...

journal_title：Molecular pharmaceutics

authors： Wei X,Zhan C,Chen X,Hou J,Xie C,Lu W

更新日期：2014-10-06 00:00:00

abstract：:Achieving effective gene therapy for glioma depends on gene delivery systems. The gene delivery system should be able to cross the blood-brain barrier (BBB) and further target glioma at its early stage. Active brain tumor targeted delivery can be achieved using the "Trojan horse" technology, which involves either endo...

journal_title：Molecular pharmaceutics

authors： Liu Y,He X,Kuang Y,An S,Wang C,Guo Y,Ma H,Lou J,Jiang C

更新日期：2014-10-06 00:00:00

abstract：:Renal ischemia/reperfusion (I/R) injury causes high mortality and morbidity during renal procedures, yet current drugs should be used at high doses or for long periods due to lack of tissue specificity. In previous work we described a novel mycophenolic acid-glucosamine conjugate (MGC) that targets the proximal tubule...

journal_title：Molecular pharmaceutics

authors： Wang X,Xiong M,Zeng Y,Sun X,Gong T,Zhang Z

更新日期：2014-10-06 00:00:00

abstract：:Curcumin (CUR) is a unique natural compound with promising anticancer and anti-inflammatory activities. However, the therapeutic efficacy of curcumin was challenged in clinical trials, mostly due to its low bioavailability, rapid metabolism, and elimination. We designed a nanodrug form of curcumin, which makes it stab...

journal_title：Molecular pharmaceutics

authors： Wei X,Senanayake TH,Bohling A,Vinogradov SV

更新日期：2014-09-02 00:00:00

abstract：:The presented molecular dynamics simulations are the first simulations to reveal dynamic dissolution of a pharmaceutical crystal in its experimentally determined shape. Continuous dissolution at constant undersaturation of the surrounding medium is ensured by introducing a plane of sticky dummy atoms into the water sl...

journal_title：Molecular pharmaceutics

authors： Greiner M,Elts E,Briesen H

更新日期：2014-09-02 00:00:00

abstract：:The molecular mechanisms of autophagy in polyethylenimine (PEI)-treated cells are not well understood because of the use of nonspecific autophagy inhibitors. Here, we applied autophagy-related gene expression analysis to pinpoint the molecular mechanisms of autophagy in PEI-treated wild-type and atg5 gene knockout (at...

journal_title：Molecular pharmaceutics

authors： Lin CW,Jan MS,Kuo JH

更新日期：2014-09-02 00:00:00

abstract：:DiI and DiD, two fluorophores able to interact by FRET (Förster resonance energy transfer), were coencapsulated in the core of lipid nanocapsules (LNCs) and nanoemulsions (LNEs), lipophilic reservoirs for the delivery of drugs. The ability of FRET imaging to provide information on the kinetics of dissociation of the n...

journal_title：Molecular pharmaceutics

authors： Gravier J,Sancey L,Hirsjärvi S,Rustique E,Passirani C,Benoît JP,Coll JL,Texier I

更新日期：2014-09-02 00:00:00

abstract：:It is well-known that renal cell carcinomas (RCCs) are resistant to classical cytotoxic anticancer drugs. Therefore, facilitating the impact of anticancer drugs by altering the cell phenotype should be a useful strategy for circumventing this. We developed a multifunctional envelope-type nanodevice (MEND) as an in viv...

journal_title：Molecular pharmaceutics

authors： Sakurai Y,Hatakeyama H,Akita H,Harashima H

更新日期：2014-08-04 00:00:00

abstract：:Our objective was to design a polymeric micelle-based doxorubicin and lapatinib combination therapy for treating multidrug resistant (MDR) breast cancers. Poly(ethylene glycol)-block-poly(2-methyl-2-benzoxycarbonylpropylene carbonate) (PEG-PBC) polymers were synthesized for preparing doxorubicin and lapatinib loaded m...

journal_title：Molecular pharmaceutics

authors： Wang H,Li F,Du C,Wang H,Mahato RI,Huang Y

更新日期：2014-08-04 00:00:00

abstract：:The bladder is an important tissue in which to evaluate xenobiotic drug interactions and toxicities due to the concentration of parent drug and hepatic/enteric-derived metabolites in the urine as a result of renal excretion. Breaching of the barrier provided by the bladder epithelial lining (the urothelium) can expose...

journal_title：Molecular pharmaceutics

authors： Baker SC,Shabir S,Southgate J

更新日期：2014-07-07 00:00:00

abstract：:Oxidative stress and inflammation are intertwined contributors to numerous acute vascular pathologies. A novel dual bioactive nanoparticle with antioxidant/anti-inflammatory properties was developed based on the interactions of tocopherol phosphate and the manganese porphyrin SOD mimetic, MnTMPyP. The size and drug in...

journal_title：Molecular pharmaceutics

authors： Howard MD,Hood ED,Greineder CF,Alferiev IS,Chorny M,Muzykantov V

更新日期：2014-07-07 00:00:00

abstract：:Combinatorial chemistry has enabled the production of very potent drugs that might otherwise suffer from poor solubility and low oral bioavailability. One approach to increase solubility is to make the drug amorphous, which leads to problems associated with drug stability. To improve stability, one option is to molecu...

journal_title：Molecular pharmaceutics

authors： Pajula K,Wittoek L,Lehto VP,Ketolainen J,Korhonen O

更新日期：2014-07-07 00:00:00

abstract：:"Nano" drug delivery carriers are established technologies for improving the therapeutic index of chemotherapeutic drugs and overcoming formulation challenges of poorly water-soluble compounds. Two important remaining challenges, however, are the need to formulate drugs on a case-by-case basis (due to the specific che...

journal_title：Molecular pharmaceutics

authors： Fuhrmann K,Gauthier MA,Leroux JC

更新日期：2014-06-02 00:00:00

abstract：:Breast cancer is the second most common cause of cancer-related deaths in women. Chemotherapy is an important treatment modality, and paclitaxel (PTX) is often the first-line therapy for its metastatic form. The two most notable limitations related to PTX-based treatment are the poor hydrophilicity of the drug and the...

journal_title：Molecular pharmaceutics

authors： Satsangi A,Roy SS,Satsangi RK,Vadlamudi RK,Ong JL

更新日期：2014-06-02 00:00:00

abstract：:The success of targeted cancer therapy largely relies upon the selection of target and the development of efficient therapeutic agents that specifically bind to the target. In the current study, we chose a cannabinoid CB2 receptor (CB2R) as a new target and used a CB2R-targeted photosensitizer, IR700DX-mbc94, for phot...

journal_title：Molecular pharmaceutics

authors： Jia N,Zhang S,Shao P,Bagia C,Janjic JM,Ding Y,Bai M

更新日期：2014-06-02 00:00:00

abstract：:The αvβ3-integrin addressing cyclic pentapeptide cyclo(RGDfK) was conjugated to NOPO, 1,4,7-triazacyclononane-1,4-bis[methylene(hydroxymethyl)phosphinic acid]-7-[methylene(2-carboxyethyl)phosphinic acid], a bifunctional chelator with exceptional gallium-68 labeling properties. NOPO-c(RGDfK) and its Ga(III) and Cu(II) ...

journal_title：Molecular pharmaceutics

authors： Simeček J,Notni J,Kapp TG,Kessler H,Wester HJ

更新日期：2014-05-05 00:00:00

abstract：:Modifying nanoparticles with targeting peptides which can specifically bind to intestinal epithelium was recently suggested as a strategy to further enhance their ability for the oral delivery of macromolecular drugs. However, few studies were focused on comprehensive understanding of the uptake and transport processe...

journal_title：Molecular pharmaceutics

authors： Zhang J,Zhu X,Jin Y,Shan W,Huang Y

更新日期：2014-05-05 00:00:00

abstract：:Here, we report the antiproliferative/cytotoxic properties of 8-hydroxyquinoline (8-HQ) derivatives on HeLa cells in the presence of transition metal ions (Cu(2+), Fe(3+), Co(2+), Ni(2+)). Two series of ligands were tested, the arylvinylquinolinic L1-L8 and the arylethylenequinolinic L9-L16, which can all interact wit...

journal_title：Molecular pharmaceutics

authors： Barilli A,Atzeri C,Bassanetti I,Ingoglia F,Dall'Asta V,Bussolati O,Maffini M,Mucchino C,Marchiò L

更新日期：2014-04-07 00:00:00

abstract：:We developed a modular multifunctional nonviral gene delivery system by targeting the overexpressed cancer surface receptor α5β1 integrin and the upregulated transcriptional activity of the cancer resistance mediating transcription factor NF-κB, thereby introducing a new form of transcriptional targeting. NF-κB regula...

journal_title：Molecular pharmaceutics

authors： Adil MM,Levine RM,Kokkoli E

更新日期：2014-03-03 00:00:00

abstract：:RNA oligonucleotides capable of inducing controlled immunostimulation combined with specific oncogene silencing via an RNA interference (RNAi) mechanism provide synergistic inhibition of cancer cell growth. With this concept, we previously designed a potent immunostimulatory long double stranded RNA, referred to as li...

journal_title：Molecular pharmaceutics

authors： Sajeesh S,Lee TY,Hong SW,Dua P,Choe JY,Kang A,Yun WS,Song C,Park SH,Kim S,Li C,Lee DK

更新日期：2014-03-03 00:00:00

abstract：:Conjugation with a cell penetrating peptide such as Tat presents an effective approach to improve the intracellular accumulation of molecules with low membrane permeability. This strategy, however, leads to a reduced cellular entry of molecules that can cross cell membrane effectively. We report here that covalent lin...

journal_title：Molecular pharmaceutics

authors： Zhang P,Lock LL,Cheetham AG,Cui H

更新日期：2014-03-03 00:00:00

abstract：:Some specific types of tumor cells and tumor endothelial cells represented CD13 proteins and act as receptors for Asn-Gly-Arg (NGR) motifs containing peptide. These CD13 receptors can be specifically recognized and bind through the specific sequence of cyclic NGR (cNGR) peptide and presented more affinity and specific...

journal_title：Molecular pharmaceutics

authors： Gupta M,Chashoo G,Sharma PR,Saxena AK,Gupta PN,Agrawal GP,Vyas SP

更新日期：2014-03-03 00:00:00

abstract：:Bacterial capsular polysaccharides are components of many modern vaccines, but they are weakly immunogenic. Herein, we describe the delivery of pneumococcal capsular polysaccharide serotype-1 (PCP-1) in polylactide polymeric particles to enhance its immunogenicity. Immunization with PCP-1-entrapped particles elicited ...

journal_title：Molecular pharmaceutics

authors： Anish C,Khan N,Upadhyay AK,Sehgal D,Panda AK

更新日期：2014-03-03 00:00:00

abstract：:This work aims to elucidate the mechanism by which N-methylpyrrolidone (NMP) enhances the skin permeation of a compound by combining experimental data with molecular dynamic (MD) simulations. The addition of 10% NMP significantly increased the propranolol (PR) permeation through the human epidermis (∼ 15 μg/cm(2) vs ∼...

journal_title：Molecular pharmaceutics

authors： Cilurzo F,Vistoli G,Selmin F,Gennari CG,Musazzi UM,Franzé S,Lo Monte M,Minghetti P

更新日期：2014-03-03 00:00:00

abstract：:In this study, transferrin (Tf)-modified poly(ethylene glycol)-phosphatidylethanolamine (mPEG-PE) micelles loaded with the poorly water-soluble drug, R547 (a potent and selective ATP-competitive cyclin-dependent kinase (CDK) inhibitor), were prepared and evaluated for their targeting efficiency and cytotoxicity in vit...

journal_title：Molecular pharmaceutics

authors： Sawant RR,Jhaveri AM,Koshkaryev A,Zhu L,Qureshi F,Torchilin VP

更新日期：2014-02-03 00:00:00

abstract：:In developing targeted probes for positron emission tomography (PET) based on (64)Cu, stable complexation of the radiometal is key, and a flexible handle for bioconjugation is highly advantageous. Here, we present the synthesis and characterization of the chelator pycup and four derivatives. Pycup is a cross-bridged c...

journal_title：Molecular pharmaceutics

authors： Boros E,Rybak-Akimova E,Holland JP,Rietz T,Rotile N,Blasi F,Day H,Latifi R,Caravan P

更新日期：2014-02-03 00:00:00

abstract：:Abnormal extracellular deposition of β-amyloid (Aβ) is thought to play a key role in the pathogenesis of Alzheimer's disease (AD). Preventing Aβ-induced neurotoxicity has become a potential therapeutic approach to improve the onset and progression of AD. Here we report the synthesis of 1,1'-(biphenyl-4,4'-diyl)-bis(3-...

journal_title：Molecular pharmaceutics

authors： Zhu Y,Sun X,Gong T,He Q,Zhang Z

更新日期：2014-02-03 00:00:00

abstract：:Therapeutic monoclonal antibodies are currently delivered mainly via the intravenous route, since large volumes are often required to deliver a therapeutic dose. Administration via the subcutaneous route would have several therapeutic advantages; the absorption mechanisms for antibodies dosed subcutaneously are poorly...

journal_title：Molecular pharmaceutics

authors： Dahlberg AM,Kaminskas LM,Smith A,Nicolazzo JA,Porter CJ,Bulitta JB,McIntosh MP

更新日期：2014-02-03 00:00:00

abstract：:Heparin is a widely used anticoagulant due to its ability to inhibit key components in the coagulation cascade such as Factor Xa and thrombin (Factor IIa). Its potential to preferentially bind to antithrombin (ATIII) results in a conformational change and activation that leads to the prevention of fibrin formation fro...

journal_title：Molecular pharmaceutics

authors： Suchyta DJ,Handa H,Meyerhoff ME

更新日期：2014-02-03 00:00:00

abstract：:The study presents the effects of blending a cationic gemini surfactant into cationic lipid bilayers and its impact on the plasmid DNA compaction and delivery process. Using nanoDSC, dynamic light scattering, zeta potential, and electrophoretic mobility measurements, together with transfection (2D- and 3D-) and viabil...

journal_title：Molecular pharmaceutics

authors： Sharma VD,Lees J,Hoffman NE,Brailoiu E,Madesh M,Wunder SL,Ilies MA

更新日期：2014-02-03 00:00:00

abstract：:Cytochrome c (Cyt c) is a small mitochondrial heme protein involved in the intrinsic apoptotic pathway. Once Cyt c is released into the cytosol, the caspase mediated apoptosis cascade is activated resulting in programmed cell death. Herein, we explore the covalent immobilization of Cyt c into mesoporous silica nanopar...

journal_title：Molecular pharmaceutics

authors： Méndez J,Morales Cruz M,Delgado Y,Figueroa CM,Orellano EA,Morales M,Monteagudo A,Griebenow K

更新日期：2014-01-06 00:00:00

abstract：:Chemotherapy is an indispensable auxiliary treatment for glioma but highly limited by the existence of both blood-brain barrier (BBB) and blood-brain tumor barrier (BBTB). The dysfunctional brain tumor blood vessels and high interstitial pressure in glioma also greatly hindered the accumulation and deep penetration of...

journal_title：Molecular pharmaceutics

authors： Miao D,Jiang M,Liu Z,Gu G,Hu Q,Kang T,Song Q,Yao L,Li W,Gao X,Sun M,Chen J

更新日期：2014-01-06 00:00:00