Low Molecular Weight Nucleoside Gelators: A Platform for Protein Aggregation Inhibition.

abstract：:Water-soluble camptothecin (CPT)-polyoxetane conjugates were synthesized using a clickable polymeric platform P(EAMO) that was made by polymerization of acetylene-functionalized 3-ethyl-3-(hydroxymethyl)oxetane (i.e., EAMO). CPT was first modified with a linker 6-azidohexanoic acid via an ester linkage to yield CPT-az...

journal_title：Molecular pharmaceutics

authors： Zolotarskaya OY,Wagner AF,Beckta JM,Valerie K,Wynne KJ,Yang H

更新日期：2012-11-05 00:00:00

abstract：:The use of adult stem cells for therapeutic purposes has met with great success in recent years. Among several types of adult stem cells, mesenchymal stem cells (MSCs) derived from bone marrow (BM) and other sources have gained popularity for basic research and clinical applications because of their therapeutic potent...

journal_title：Molecular pharmaceutics

authors： Wu H,Ye Z,Mahato RI

更新日期：2011-10-03 00:00:00

abstract：:Mucus layer, a selective diffusion barrier, has an important effect on the fate of drug delivery systems in the gastrointestinal tract. To study the fate of microemulsions in the mucus layer, four microemulsion formulations with different particle sizes and lipid compositions were prepared. The microemulsion-mucin int...

journal_title：Molecular pharmaceutics

authors： Zhang J,Lv Y,Wang B,Zhao S,Tan M,Lv G,Ma X

更新日期：2015-03-02 00:00:00

abstract：:Amphotericin B (AmB) is a lifesaving polyene antibiotic used widely to treat deep-seated mycoses. Both the pharmaceutical effectiveness as well as toxic side effects depend on molecular organization of the drug. In the present study, we analyzed steady-state fluorescence, fluorescence anisotropy spectra, fluorescence ...

journal_title：Molecular pharmaceutics

authors： Wasko P,Luchowski R,Tutaj K,Grudzinski W,Adamkiewicz P,Gruszecki WI

更新日期：2012-05-07 00:00:00

abstract：:A promising strategy to enable patient stratification for targeted therapies is to monitor the target expression in a tumor by radionuclide molecular imaging. Affibody molecules (7 kDa) are nonimmunoglobulin scaffold proteins with a 25-fold smaller size than intact antibodies. They have shown an apparent potential as ...

journal_title：Molecular pharmaceutics

authors： Westerlund K,Honarvar H,Norrström E,Strand J,Mitran B,Orlova A,Eriksson Karlström A,Tolmachev V

更新日期：2016-05-02 00:00:00

abstract：:To develop a radioactive metal complex platform for tumor theranostics, we introduced three radiopharmaceutical derivatives of 1,4,7,10-tetraazacyclododecane-1,4,7-trisacetic acid-benzothiazole aniline (DO3A-BTA, L1) labeled with medical radioisotopes for diagnosis (68Ga/64Cu) and therapy (177Lu). The tumor-targeting ...

journal_title：Molecular pharmaceutics

authors： Park JA,Lee JW,Kim HK,Shin UC,Lee KC,Kim TJ,Chang Y,Kim KM,Kim JY,Lee YJ

更新日期：2018-03-05 00:00:00

abstract：:The ability to select patients who will respond to therapy is especially acute for autoimmune/inflammatory diseases, where the costs of therapies can be high and the progressive damage associated with ineffective treatments can be irreversible. In this article we describe a clinical test that will rapidly predict the ...

journal_title：Molecular pharmaceutics

authors： Kelderhouse LE,Robins MT,Rosenbalm KE,Hoylman EK,Mahalingam S,Low PS

更新日期：2015-10-05 00:00:00

abstract：:The formation mechanism of drug nanoparticles was investigated using solid-state nuclear magnetic resonance (NMR) techniques for the efficient discovery of an optimized nanoparticle formulation. The cogrinding of nifedipine (NIF) with polymers, including hydroxypropyl methylcellulose (HPMC) and polyvinylpyrrolidone (P...

journal_title：Molecular pharmaceutics

authors： Ueda K,Higashi K,Moribe K

更新日期：2016-03-07 00:00:00

abstract：:Multidrug resistance (MDR), a major obstacle to successful cancer chemotherapy, may be induced by amplification of the MDR1 gene and overexpression of the P-glycoprotein (P-gp), which acts as drug efflux pump decreasing intracellular drug accumulation. In this study, an antisense oligodeoxynucleotide--doxorubicin conj...

journal_title：Molecular pharmaceutics

authors： Ren Y,Wang Y,Zhang Y,Wei D

更新日期：2008-07-01 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：:In our previous studies, ethylene glycol-linked amino acid diester prodrugs of oleanolic acid (OA), a Biopharmaceutics Classification System (BCS) class IV drug, designed to target peptide transporter 1 (PepT1) have been synthesized and evaluated. Unlike ethylene glycol, propylene glycol is of very low toxicity in viv...

journal_title：Molecular pharmaceutics

authors： Cao F,Gao Y,Wang M,Fang L,Ping Q

更新日期：2013-04-01 00:00:00

abstract：:Solid lipid nanoparticles (SLNs) are one of the most promising nanocarriers to increase the oral absorption of drugs with poor solubility and low permeability. However, the absorption mechanism of SLNs remains incomplete and thus requires further careful consideration. In this study, positively charged chitosan (CS) m...

journal_title：Molecular pharmaceutics

authors： Shi LL,Xie H,Lu J,Cao Y,Liu JY,Zhang XX,Zhang H,Cui JH,Cao QR

更新日期：2016-08-01 00:00:00

abstract：:This study aims to investigate the crystallization behavior and molecular dynamics of amorphous griseofulvin (GSF) in the presence of low-concentration poly(ethylene oxide) (PEO). We observe that the addition of 3% w/w PEO remarkably increases the crystal growth rate of GSF by two orders of magnitude in both the super...

journal_title：Molecular pharmaceutics

authors： Shi Q,Zhang C,Su Y,Zhang J,Zhou D,Cai T

更新日期：2017-07-03 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：:Due to overexpression of glycyrrhetinic acid (GA) receptor in liver cancer cells, glycyrrhetinic acid modified recombinant human serum albumin (rHSA) nanoparticles for targeting liver tumor cells may result in increased therapeutic efficacy and decreased adverse effects of cancer therapy. In this study, doxorubicin (D...

journal_title：Molecular pharmaceutics

authors： Qi WW,Yu HY,Guo H,Lou J,Wang ZM,Liu P,Sapin-Minet A,Maincent P,Hong XC,Hu XM,Xiao YL

更新日期：2015-03-02 00:00:00

abstract：:Iron oxide nanoparticles have great potential as diagnostic and therapeutic agents in cancer and other diseases; however, biological aggregation severely limits their function in vivo. Aggregates can cause poor biodistribution, reduced heating capability, and can confound their visualization and quantification by magn...

journal_title：Molecular pharmaceutics

authors： Hurley KR,Ring HL,Etheridge M,Zhang J,Gao Z,Shao Q,Klein ND,Szlag VM,Chung C,Reineke TM,Garwood M,Bischof JC,Haynes CL

更新日期：2016-07-05 00:00:00

abstract：:Electrostatic potential (ESP) is a useful physicochemical property of a molecule that provides insights into inter- and intramolecular associations, as well as prediction of likely sites of electrophilic and nucleophilic metabolic attack. Knowledge of sites of metabolic attack is of paramount importance in DMPK resear...

journal_title：Molecular pharmaceutics

authors： Ford KA

更新日期：2013-04-01 00:00:00

abstract：:Preferential interactions of formulation excipients govern their impact on the stability properties of proteins in solution. The ability to predict these interactions without the need to perform experiments would enable formulation design to begin early in the development of a new antibody therapeutic. With that in mi...

journal_title：Molecular pharmaceutics

authors： Cloutier TK,Sudrik C,Mody N,Sathish HA,Trout BL

更新日期：2020-09-08 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：:To predict the outcome of intestinal drug transporter induction on pharmacokinetics, signaling of the DNA message along with messenger RNA (mRNA) transcription and protein translation leading to transporter function must be understood. We quantified the gene expression of PXR and CAR, gene expression and protein abund...

journal_title：Molecular pharmaceutics

authors： Brueck S,Bruckmueller H,Wegner D,Busch D,Martin P,Oswald S,Cascorbi I,Siegmund W

更新日期：2019-09-03 00:00:00

abstract：:The purpose of this study was to examine the melanoma targeting and imaging properties of two new (99m)Tc-labeled Arg-X-Asp-conjugated α-melanocyte stimulating hormone (α-MSH) peptides. RTD-Lys-(Arg(11))CCMSH {c[Asp-Arg-Thr-Asp-DTyr]-Lys-Cys-Cys-Glu-His-DPhe-Arg-Trp-Cys-Arg-Pro-Val-NH2} and RVD-Lys-(Arg(11))CCMSH pept...

journal_title：Molecular pharmaceutics

authors： Flook AM,Yang J,Miao Y

更新日期：2013-09-03 00:00:00

abstract：:The caveolin scaffolding domain peptide (CSP) is being developed for the therapeutic intervention of a lethal lung disease, idiopathic pulmonary fibrosis. While direct respiratory delivery of CSP7 (a 7-mer fragment of CSP) is considered an effective route, proper formulation and processing of the peptide are required....

journal_title：Molecular pharmaceutics

authors： Zhang Y,MacKenzie B,Koleng JJ,Maier E,Warnken ZN,Williams RO 3rd

更新日期：2020-02-03 00:00:00

abstract：:Nonsteroidal anti-inflammatory drugs (NSAIDs) can inhibit cell growth and metastasis, and induce cell apoptosis in cancerous cells. They have been shown to reduce incidence and mortality of gastric cancer by an unknown mechanism. NSAIDs often exert their effects by Cox-2 inhibition, and Cox-2 is overexpressed in gastr...

journal_title：Molecular pharmaceutics

authors： Jin H,Wang Z,Liu L,Gao L,Sun L,Li X,Zhao H,Pan Y,Shi H,Liu N,Hong L,Liang J,Wu Q,Yang Z,Wu K,Fan D

更新日期：2010-02-01 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：:Oncolytic adenoviruses rank among the most promising innovative agents in cancer therapy. We examined the potential of boosting the efficacy of the oncolytic adenovirus dl520 by associating it with magnetic nanoparticles and magnetic-field-guided infection in multidrug-resistant (MDR) cancer cells in vitro and upon in...

journal_title：Molecular pharmaceutics

authors： Tresilwised N,Pithayanukul P,Mykhaylyk O,Holm PS,Holzmüller R,Anton M,Thalhammer S,Adigüzel D,Döblinger M,Plank C

更新日期：2010-08-02 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：:This research determined the uptake of individual components of topically applied microemulsions into the stratum corneum (SC) and assessed their molecular effects on skin barrier function. The microemulsions comprised oleic acid, Tween20, Transcutol and water. The effects of selected formulations, and of the individu...

journal_title：Molecular pharmaceutics

authors： Hathout RM,Mansour S,Mortada ND,Geneidi AS,Guy RH

更新日期：2010-08-02 00:00:00

abstract：:For the purpose of improving the tumor delivery of doxorubicin (DOX), a kind of peptide-DOXO conjugate was designed and prepared, in which the peptide composed of an albumin-binding domain (ABD) and a tumor-specific internalizing sequence (RGDK or RPARPAR) was conjugated to a (6-maleimidocaproyl) hydrazone derivative ...

journal_title：Molecular pharmaceutics

authors： Liu L,Zhang C,Li Z,Wang C,Bi J,Yin S,Wang Q,Yu R,Liu Y,Su Z

更新日期：2017-11-06 00:00:00

abstract：:In the present research a salt of vincamine, a poorly bioavailable indole alkaloid derived from the leaves of Vinca minor L., was synthesized in the solid state by means of a mechanochemical process employing citric acid as a reagent. The mechanochemical process was adopted as a solvent-free alternative to classical c...

journal_title：Molecular pharmaceutics

authors： Hasa D,Perissutti B,Cepek C,Bhardwaj S,Carlino E,Grassi M,Invernizzi S,Voinovich D

更新日期：2013-01-07 00:00:00

abstract：:meta-Tetra(hydroxyphenyl)chlorin (mTHPC) is one of the most potent second-generation photosensitizers, clinically used for photodynamic therapy (PDT) of head and neck squamous cell carcinomas. However, improvements are still required concerning its present formulation (i.e., Foscan, a solution of mTHPC in ethanol/prop...

journal_title：Molecular pharmaceutics

authors： Liu Y,Scrivano L,Peterson JD,Fens MHAM,Hernández IB,Mesquita B,Toraño JS,Hennink WE,van Nostrum CF,Oliveira S

更新日期：2020-04-06 00:00:00