Predicting the Risk of Phospholipidosis with in Silico Models and an Image-Based in Vitro Screen.

abstract：:Similar to glycolysis, glutaminolysis acts as a vital energy source in tumor cells, providing building blocks for the metabolic needs of tumor cells. To capture glutaminolysis in tumors, 18F-(2S,4R)4-fluoroglutamine ([18F]FGln) and 18F-fluoroboronoglutamine ([18F]FBQ) have been successfully developed for positron emis...

journal_title：Molecular pharmaceutics

authors： Chen J,Li C,Hong H,Liu H,Wang C,Xu M,Han Y,Liu Z

更新日期：2019-12-02 00:00:00

abstract：:p53 is a key tumor suppressor gene involved in key cellular processes and implicated in cancer therapy. However, it is inactivated in more than 50% of all cancers due to mutation or overexpression of its negative regulators. This leads to drug resistance and poor chemotherapeutic outcome as most clinical drugs act via...

journal_title：Molecular pharmaceutics

authors： Chow MJ,Babak MV,Wong DY,Pastorin G,Gaiddon C,Ang WH

更新日期：2016-07-05 00:00:00

abstract：:The Flory-Huggins interaction parameter has been shown to be useful in predicting the thermodynamic miscibility of a polymer and a small molecule in a binary mixture. In the present paper, this concept was extended and evaluated to determine whether or not the Flory-Huggins interaction parameter can be applied to smal...

journal_title：Molecular pharmaceutics

authors： Pajula K,Taskinen M,Lehto VP,Ketolainen J,Korhonen O

更新日期：2010-06-07 00:00:00

abstract：:Microcrystalline vinpocetine, coground with cross-linked polyvinylpyrrolidone, affords hybrids containing nanosized drug nanocrystals, the size and size distributions of which depend on milling times and drug-to-polymer weight ratios. Using an innovative approach to microstructural characterization, we analyzed wide-a...

journal_title：Molecular pharmaceutics

authors： Hasa D,Giacobbe C,Perissutti B,Voinovich D,Grassi M,Cervellino A,Masciocchi N,Guagliardi A

更新日期：2016-09-06 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：:This study investigated the role of the prostaglandin (PG) pathway in locally applied, simvastatin-induced oral bone growth. The possibility of enhancing long-term bone augmentation with an alendronate-based carrier was initiated. Mandibles of 44 mature female rats were treated bilaterally with the following combinati...

journal_title：Molecular pharmaceutics

authors： Lee Y,Liu X,Nawshad A,Marx DB,Wang D,Reinhardt RA

更新日期：2011-08-01 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：:Tumor hypoxia plays a major role in radio- and chemotherapy resistance in solid tumors. Carbonic Anhydrase IX (CAIX) is an endogenous hypoxia-related protein, which is associated with poor patient outcome. The quantitative assessment of CAIX expression of tumors may steer cancer treatment by predicting therapy respons...

journal_title：Molecular pharmaceutics

authors： Huizing FJ,Hoeben BAW,Franssen GM,Boerman OC,Heskamp S,Bussink J

更新日期：2019-02-04 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：:The barrier epithelia of the cornea and retina control drug and nutrient access to various compartments of the human eye. While ocular transporters are likely to play a critical role in homeostasis and drug delivery, little is known about their expression, localization and function. In this study, the mRNA expression ...

journal_title：Molecular pharmaceutics

authors： Dahlin A,Geier E,Stocker SL,Cropp CD,Grigorenko E,Bloomer M,Siegenthaler J,Xu L,Basile AS,Tang-Liu DD,Giacomini KM

更新日期：2013-02-04 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：:A deep convolutional generative adversarial network (dcGAN) model was developed in this study to screen and design target-specific novel compounds for cannabinoid receptors. In the adversarial process of training, two models, the discriminator D and the generator G, are iteratively trained. D is trained to discover th...

journal_title：Molecular pharmaceutics

authors： Bian Y,Wang J,Jun JJ,Xie XQ

更新日期：2019-11-04 00:00:00

abstract：:Many cancer therapy regimes still rely heavily on the systemic administration of toxic chemotherapeutic agents. Ultrasound contrast agents consisting of microbubbles (MBs) have emerged as a drug delivery vehicle to overcome the challenges associated with systemic chemotherapy. Here, we describe the development of non-...

journal_title：Molecular pharmaceutics

authors： Jablonowski LJ,Teraphongphom NT,Wheatley MA

更新日期：2017-10-02 00:00:00

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：:Organic anion transporting polypeptides 1B1 and 1B3 are transporters selectively expressed on the basolateral membrane of the hepatocyte. Several studies reveal that they are involved in drug-drug interactions, cancer, and hyperbilirubinemia. In this study, we developed a set of classification models for OATP1B1 and 1...

journal_title：Molecular pharmaceutics

authors： Kotsampasakou E,Brenner S,Jäger W,Ecker GF

更新日期：2015-12-07 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：:Novel strategy has been developed for fabricating the biocompatible reduction and pH dual-responsive core cross-linked (CCL) micelles as drug delivery system (DDS) for the controlled anticancer drug delivery, via the atom transfer radical polymerization (ATRP) of tert-butyl acrylate (tBA) with N,N'-bis(acryloyl)cystam...

journal_title：Molecular pharmaceutics

authors： Tian K,Jia X,Zhao X,Liu P

更新日期：2017-03-06 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：: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：:Polysorbate 20 (PS20) is a commonly used surfactant in biopharmaceutical formulations. It is a heterogeneous surfactant containing a distribution of fatty acid esters, which are subject to hydrolytic degradation, generating free fatty acids (FFAs). The FFAs can form visible or subvisible particles in drug product on s...

journal_title：Molecular pharmaceutics

authors： Doshi N,Martin J,Tomlinson A

更新日期：2020-11-02 00:00:00

abstract：:Penetratin is a classical cell-penetrating peptide with the potential to assist in the transmembrane delivery of proteins or drugs. However, the synthesis and application of cholesterol-penetratin (Chol-P) conjugates as nonviral delivery systems for microRNAs or drugs have not previously been reported. In this study, ...

journal_title：Molecular pharmaceutics

authors： Zhang N,Huang Y,Wu F,Zhao Y,Li X,Shen P,Yang L,Luo Y,Yang L,He G

更新日期：2016-07-05 00:00:00

abstract：:Extracellular β-glucuronidase (β-GUS) in tumors has been investigated as a target enzyme for prodrug therapy. However, despite encouraging preclinical results, animal studies also indicate that the success of prodrug therapy might be limited by the insufficient prodrug-converting enzyme activity, especially in small t...

journal_title：Molecular pharmaceutics

authors： Antunes IF,Haisma HJ,Elsinga PH,Di Gialleonardo V,van Waarde A,Willemsen AT,Dierckx RA,de Vries EF

更新日期：2012-11-05 00:00:00

abstract：:Intracellular unbound drug concentrations determine affinity to targets in the cell interior. However, due to difficulties in measuring them, they are often overlooked in pharmacology. Here we present a simple experimental technique for the determination of unbound intracellular drug concentrations in cultured cells t...

journal_title：Molecular pharmaceutics

authors： Mateus A,Matsson P,Artursson P

更新日期：2013-06-03 00:00:00

abstract：:Lipid-core nanocapsules (LCNs) have been proposed as drug carriers to improve brain delivery by modulating drug pharmacokinetics (PK). However, it is not clear whether the LCNs carry the drug through the blood-brain barrier or increase free drug penetration due to changes in the barrier permeability. Quetiapine (QTP) ...

journal_title：Molecular pharmaceutics

authors： Carreño F,Paese K,Silva CM,Guterres SS,Dalla Costa T

更新日期：2016-04-04 00:00:00

abstract：:The primary cause of mortality for glioblastoma (GBM) is local tumor recurrence following standard-of-care therapies, including surgical resection. With most tumors recurring near the site of surgical resection, local delivery of chemotherapy at the time of surgery is a promising strategy. Herein drug-loaded polymer s...

journal_title：Molecular pharmaceutics

authors： Graham-Gurysh E,Moore KM,Satterlee AB,Sheets KT,Lin FC,Bachelder EM,Miller CR,Hingtgen SD,Ainslie KM

更新日期：2018-03-05 00:00:00

abstract：:As a result of its higher molecular mobility, the surface of an amorphous drug can grow crystals much more rapidly than the bulk, causing poor stability and slow dissolution of drug products. We show that a nanocoating of chitosan (a pharmaceutically acceptable polymer) can be deposited on the surface of amorphous ind...

journal_title：Molecular pharmaceutics

authors： Li Y,Yu J,Hu S,Chen Z,Sacchetti M,Sun CC,Yu L

更新日期：2019-03-04 00:00:00

abstract：:In the present age of pharmaceutical research and development, focused delivery of decision making data is more imperative than ever before. Resulting from several years' success, failure and consequential learning, this article also proffers advice and guidance on which in vitro and in vivo experiments to perform to ...

journal_title：Molecular pharmaceutics

authors： Grime KH,Barton P,McGinnity DF

更新日期：2013-04-01 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：:Metallacarborane moieties have been identified as promising pharmacophores. The pharmaceutical use of such compounds is, however, complicated by their low solubility and tendency to self-assemble in aqueous solution. In this work, we estimated the solubilities of a vast series of metallacarboranes [cobalt bis(dicarbol...

journal_title：Molecular pharmaceutics

authors： Rak J,Dejlová B,Lampová H,Kaplánek R,Matějíček P,Cígler P,Král V

更新日期：2013-05-06 00:00:00

abstract：:The controlled release of anticancer drugs at the tumor site is a central challenge in treating cancer. To achieve this goal, our strategy was based on tumor-specific targeting and ultrasound-triggered release of an anticancer agent from liposomal nanocarriers. To enhance the ultrasound-triggered drug release, we inco...

journal_title：Molecular pharmaceutics

authors： Zhou C,Xie X,Yang H,Zhang S,Li Y,Kuang C,Fu S,Cui L,Liang M,Gao C,Yang Y,Gao C,Yang C

更新日期：2019-07-01 00:00:00