Metallo-Cubosomes: Zinc-Functionalized Cubic Nanoparticles for Therapeutic Nucleotide Delivery.

abstract：:The most promising F508del-CFTR corrector, VX-809, has been unsuccessful as an effective, stand-alone treatment for CF patients, but the rescue effect in combination with other drugs may confer an acceptable level of therapeutic benefit. Targeting cellular factors that modify trafficking may act to enhance the cell su...

journal_title：Molecular pharmaceutics

authors： Perkins LA,Fisher GW,Naganbabu M,Schmidt BF,Mun F,Bruchez MP

更新日期：2018-03-05 00:00:00

abstract：:Particle size distribution and stability are key attributes for the evaluation of the safety and efficacy profile of medical nanoparticles (Med-NPs). Measuring particle average size and particle size distribution is a challenging task which requires the combination of orthogonal high-resolution sizing techniques, espe...

journal_title：Molecular pharmaceutics

authors： Caputo F,Arnould A,Bacia M,Ling WL,Rustique E,Texier I,Mello AP,Couffin AC

更新日期：2019-02-04 00:00:00

abstract：:The present work reports a thorough conformational analysis of iodinated contrast media: iomeprol, iopamidol (the world's most utilized contrast agent), and iopromide. Its main aim is the understanding of the complex structural features of these atropisomeric molecules, characterized by the presence of many conformers...

journal_title：Molecular pharmaceutics

authors： Fontanive L,D'Amelio N,Cesàro A,Gamini A,Tavagnacco L,Paolantoni M,Brady JW,Maiocchi A,Uggeri F

更新日期：2015-06-01 00:00:00

abstract：:It is well established that polymers adopt a range of conformations and solution-state organization in response to varying solution environments, although very little work has been done to understand how these effects might impact the physical stability and bioavailability of spray-dried amorphous dispersions (SDDs). ...

journal_title：Molecular pharmaceutics

authors： Defrese MK,Farmer MA,Long Y,Timmerman LR,Bae Y,Marsac PJ

更新日期：2020-12-07 00:00:00

abstract：:The successful applicability of gene therapy approaches will heavily rely on the development of efficient and safe nonviral gene delivery vectors, for example, cell-penetrating peptides (CPPs). CPPs can condense oligonucleotides and plasmid DNA (pDNA) into nanoparticles, thus allowing the transfection of genetic mater...

journal_title：Molecular pharmaceutics

authors： Veiman KL,Mäger I,Ezzat K,Margus H,Lehto T,Langel K,Kurrikoff K,Arukuusk P,Suhorutšenko J,Padari K,Pooga M,Lehto T,Langel Ü

更新日期：2013-01-07 00:00:00

abstract：:In the drug discovery setting, the ability to rapidly identify drug absorption risk in preclinical species at high doses from easily measured physical properties is desired. This is due to the large number of molecules being evaluated and their high attrition rate, which make resource-intensive in vitro and in silico ...

journal_title：Molecular pharmaceutics

authors： Wuelfing WP,Daublain P,Kesisoglou F,Templeton A,McGregor C

更新日期：2015-04-06 00:00:00

abstract：:How genotypic variation results in phenotypic differences is still a challenge for biology. In the field of drug metabolism, the means by which specific cytochrome P4502D6 (CYP2D6) genotypes yield different phenotypes at various levels (molecular, cellular, and organismal) is an important question, as differences in C...

journal_title：Molecular pharmaceutics

authors： Gao J,Tian X,Zhou J,Cui MZ,Zhang HF,Gao N,Wen Q,Qiao HL

更新日期：2017-03-06 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：:We report on tailored lipid-polymer hybrid nanoparticles (NPs) delivering nitric oxide (NO) under the control of visible light as a tool for overcoming doxorubicin (DOX) resistance. The NPs consist of a polymeric core and a coating. They are appropriately designed to entrap DOX in the poly(lactide-co-glycolide) core a...

journal_title：Molecular pharmaceutics

authors： Fraix A,Conte C,Gazzano E,Riganti C,Quaglia F,Sortino S

更新日期：2020-06-01 00:00:00

abstract：:Diabetic wounds are a worldwide health problem causing extremely heavy public health burden and require effective treatment. Optimal strategies for treating nonhealing diabetic wounds include stem-cell-based therapy and delivery of novel drug substances, such as functional microRNAs (miRNAs); however, miRNA easily deg...

journal_title：Molecular pharmaceutics

authors： Lv Q,Deng J,Chen Y,Wang Y,Liu B,Liu J

更新日期：2020-05-04 00:00:00

abstract：:Organic anion transporting polypeptide (OATP) 1B1 plays an important role in the hepatic uptake of various drugs. Because OATP1B1 is a site of drug-drug interactions (DDIs), evaluating the inhibitory potential of drug candidates on OATP1B1 is required during drug development. For establishing a highly sensitive, high-...

journal_title：Molecular pharmaceutics

authors： Izumi S,Nozaki Y,Komori T,Takenaka O,Maeda K,Kusuhara H,Sugiyama Y

更新日期：2016-02-01 00:00:00

abstract：:Despite advances in cancer therapies, glioblastoma multiforme treatment remains inefficient due to the brain-blood barrier (BBB) inhibitory activity and to the low temozolomide (TMZ) chemotherapeutic selectivity. To improve therapeutic outcomes, in this work we propose two strategies, (i) photodynamic therapy (PDT) as...

journal_title：Molecular pharmaceutics

authors： Pellosi DS,Paula LB,de Melo MT,Tedesco AC

更新日期：2019-03-04 00:00:00

abstract：:In this work, we demonstrated that the simple substitution of the 1,2,4-triazole moiety in 5-( 4H-1,2,4-triazol-4-yl)isophthalic acid (5-TIA) by the 1 H-1,2,3-triazol-5-yl unit enables the preparation of a hydrogelator (click-TIA). In sharp contrast to 5-TIA, its isostere click-TIA undergoes self-assembly in water upo...

journal_title：Molecular pharmaceutics

authors： Häring M,Rodríguez-López J,Grijalvo S,Tautz M,Eritja R,Martín VS,Díaz Díaz D

更新日期：2018-08-06 00:00:00

abstract：:Amino acids derivative are well established molecular probes for diagnosis of a variety of cancer using positron emission tomography (PET). Recently, boramino acid (BAAs) was found as a prospective molecular platform for developing PET tracer. The objective of this study was to develop a 18F-labeled alanine derivative...

journal_title：Molecular pharmaceutics

authors： Liu H,Han Y,Li J,Qin M,Fu Q,Wang C,Liu Z

更新日期：2018-03-05 00:00:00

abstract：:The aim of this work was to develop a phosphate buffer based dissolution method for enteric-coated formulations with improved biopredictivity for fasted conditions. Two commercially available enteric-coated aspirin products were used as model formulations (Aspirin Protect 300 mg, and Walgreens Aspirin 325 mg). The dis...

journal_title：Molecular pharmaceutics

authors： Al-Gousous J,Amidon GL,Langguth P

更新日期：2016-06-06 00:00:00

abstract：:Although nanocarriers hold promise for cancer chemotherapy, their intracellular drug delivery pathways are not fully understood. In particular, the influence of nanocarrier stability on cellular uptake is still uncertain. By physically loading hydrophobic FRET probes, we revealed different intracellular drug delivery ...

journal_title：Molecular pharmaceutics

authors： Lee SY,Tyler JY,Kim S,Park K,Cheng JX

更新日期：2013-09-03 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：:The 1:1 cocrystal of the antifungal agent ketoconazole with p-aminobenzoic acid was successfully crystallized and systematically characterized by a physical and pharmacological point of view. Crystal structure determination confirmed the cocrystal identity, giving full insight in its crystal packing and degree of diso...

journal_title：Molecular pharmaceutics

authors： Martin F,Pop M,Kacso I,Grosu IG,Miclăuş M,Vodnar D,Lung I,Filip GA,Olteanu ED,Moldovan R,Nagy A,Filip X,Bâldea I

更新日期：2020-03-02 00:00:00

abstract：:The tumor microenvironments are often acidic and overexpress specific enzymes. In this work, we synthesized a poly(AA-b-NIPAAm) copolymer (PAA-b-PNIPAAm) using a reversible addition-fragmentation chain transfer (RAFT) polymerization method. PAA-b-PNIPAAm and a cationic protein (protamine) were self-assembled into nano...

journal_title：Molecular pharmaceutics

authors： Don TM,Lu KY,Lin LJ,Hsu CH,Wu JY,Mi FL

更新日期：2017-12-04 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：:The aim of the research work was to develop and characterize a concanavalin-A (Con-A) conjugated gastroretentive multiparticulate delivery system of clarithromycin (CM) for the effective treatment of colonization of Helicobacter pylori (H. pylori). Ethylcellulose (EC) microspheres containing CM were prepared using emu...

journal_title：Molecular pharmaceutics

authors： Jain SK,Jangdey MS

更新日期：2009-01-01 00:00:00

abstract：:In women with human epidermal growth factor 2 (HER2)-positive breast cancer, the improved control of systemic disease with new therapies has unmasked brain metastases that historically would have remained clinically silent. The efficacy of therapeutic agents against brain metastases is limited by their inability to pe...

journal_title：Molecular pharmaceutics

authors： Wyatt EA,Davis ME

更新日期：2020-02-03 00:00:00

abstract：:Constitutively activated signal transducer and activator of transcription-3 (STAT3) in tumor and dendritic cells (DCs) plays a critical role in tumor-induced immunosuppression. This is considered a major challenge in effective immunotherapy of cancer. Herein we describe the development of a polymeric nanocarrier for t...

journal_title：Molecular pharmaceutics

authors： Molavi O,Mahmud A,Hamdy S,Hung RW,Lai R,Samuel J,Lavasanifar A

更新日期：2010-04-05 00:00:00

abstract：:Biophysical tools have been invaluable in formulating therapeutic proteins. These tools characterize protein stability rapidly in a variety of solution conditions, but in general, the techniques lack the ability to discern site-specific information to probe how solution environment acts to stabilize or destabilize the...

journal_title：Molecular pharmaceutics

authors： Krause ME,Martin TT,Laurence JS

更新日期：2012-04-02 00:00:00

abstract：:The reaction of singlet oxygen with water to form hydrogen peroxide was catalyzed by antibodies and has been termed as the antibody catalyzed water oxidation pathway (ACWOP) (Nieva and Wentworth, Trends Biochem. Sci. 2004, 29, 274-278; Nieva et al. Immunol. Lett. 2006, 103, 33-38). While conserved and buried tryptopha...

journal_title：Molecular pharmaceutics

authors： Sreedhara A,Lau K,Li C,Hosken B,Macchi F,Zhan D,Shen A,Steinmann D,Schöneich C,Lentz Y

更新日期：2013-01-07 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：:Design and development of amphiphilic block copolymer-based nanocarriers exhibiting enhanced colloidal stability upon dilution in the blood and cellular glutathione-responsive rapid drug release is highly desired for tumor-targeting chemotherapy. Herein, we report a novel ABA-type triblock copolymer consisting of a hy...

journal_title：Molecular pharmaceutics

authors： Biswas D,An SY,Li Y,Wang X,Oh JK

更新日期：2017-08-07 00:00:00

abstract：:Olive pollen is one of the most important causes of respiratory allergy, with Ole e 1 being the most clinically relevant sensitizing allergen. Peptide-based vaccines represent promising therapeutic approaches, but the use of adjuvants is required to strengthen the weak immunogenicity of small peptides. We propose the ...

journal_title：Molecular pharmaceutics

authors： Benedé S,Ramos-Soriano J,Palomares F,Losada J,Mascaraque A,López-Rodríguez JC,Rojo J,Mayorga C,Villalba M,Batanero E

更新日期：2020-03-02 00:00:00

abstract：:The purpose of this study was to examine and compare the melanoma targeting and imaging properties of (64)Cu-NOTA-GGNle-CycMSH(hex) {(64)Cu-1,4,7-triazacyclononane-1,4,7-triacetic acid-Gly-Gly-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-CONH2} and (64)Cu-DOTA-GGNle-CycMSH(hex) {(64)Cu-1,4,7,10-tetraazacyclononane-1,4,7,10-tetraac...

journal_title：Molecular pharmaceutics

authors： Guo H,Miao Y

更新日期：2012-08-06 00:00:00

abstract：:Lipoplexes, composed of Lipofectamine and mRNA encoding HIV Gag protein, were shown to be internalized by dendritic cells (DCs) and promote antigen presentation to stimulate HIV-specific T cell responses. Using confocal microscopy, we showed that one-third of fluorescently labeled mRNA containing lipoplexes are coloca...

journal_title：Molecular pharmaceutics

authors： De Haes W,Van Mol G,Merlin C,De Smedt SC,Vanham G,Rejman J

更新日期：2012-10-01 00:00:00