Enhanced antiproliferative activity of transferrin-conjugated paclitaxel-loaded nanoparticles is mediated via sustained intracellular drug retention.

abstract：:Active targeting of nanostructures containing chemotherapeutic agents can improve cancer treatment. Here, a three-way junction pocket DNA nanostructure was developed for efficient doxorubicin (Dox) delivery into cancer cells. The three-way junction pocket DNA nanostructure is composed of three strands of AS1411 aptame...

journal_title：Molecular pharmaceutics

authors： Taghdisi SM,Danesh NM,Ramezani M,Yazdian-Robati R,Abnous K

更新日期：2018-05-07 00:00:00

abstract：:Despite being widely used in the clinical setting for sentinel lymph node detection (SLND), (99m)Tc-based colloids (e.g., (99m)Tc-human serum albumin colloids) present a set of properties that are far from ideal. Aiming to design novel compounds with improved biological properties, we describe herein the first class o...

journal_title：Molecular pharmaceutics

authors： Morais M,Subramanian S,Pandey U,Samuel G,Venkatesh M,Martins M,Pereira S,Correia JD,Santos I

更新日期：2011-04-04 00:00:00

abstract：:Molecular imaging of programmed cell death (apoptosis) in vivo is an innovative strategy for early assessment of treatment response and treatment efficacy in cancer patients. Externalization of phosphatidylserine (PS) to the cell membrane surface of dying cells makes this phospholipid an attractive molecular target fo...

journal_title：Molecular pharmaceutics

authors： Perreault A,Richter S,Bergman C,Wuest M,Wuest F

更新日期：2016-10-03 00:00:00

abstract：:Preferential interactions of formulation excipients govern their overall interactions with protein molecules, and molecular dynamics simulations allow for the examination of the interactions at the molecular level. We used molecular dynamics simulations to examine the interactions of sorbitol, sucrose, and trehalose w...

journal_title：Molecular pharmaceutics

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

更新日期：2019-08-05 00:00:00

abstract：:In this manuscript, we have reported a novel 2D fingerprint-based artificial neural network QSAR (FANN-QSAR) method in order to effectively predict biological activities of structurally diverse chemical ligands. Three different types of fingerprints, namely, ECFP6, FP2 and MACCS, were used in FANN-QSAR algorithm devel...

journal_title：Molecular pharmaceutics

authors： Myint KZ,Wang L,Tong Q,Xie XQ

更新日期：2012-10-01 00:00:00

abstract：:The safety and efficacy of anticancer antibody-drug conjugates (ADCs) depend on the selection of tumor-targeting monoclonal antibody (mAb), linker, and drug, as well as their specific chemical arrangement and linkage chemistry. In this study, we used a heterobifunctional cross-linker to conjugate docetaxel (DX) to cet...

journal_title：Molecular pharmaceutics

authors： Glatt DM,Beckford Vera DR,Prabhu SS,Mumper RJ,Luft JC,Benhabbour SR,Parrott MC

更新日期：2018-11-05 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：:Pancreatic ductal adenocarcinoma (PDAC) is highly chemo-resistant and has an extremely poor patient prognosis, with a survival rate at five years of <8%. There remains an urgent need for innovative treatments. Targeting polyamine biosynthesis through inhibition of ornithine decarboxylase with difluoromethylornithine (...

journal_title：Molecular pharmaceutics

authors： Gitto SB,Pandey V,Oyer JL,Copik AJ,Hogan FC,Phanstiel O 4th,Altomare DA

更新日期：2018-02-05 00:00:00

abstract：:Saquinavir mesylate (SQV) is the first-in-class and prototypical HIV protease inhibitor (PI) used in the treatment of HIV infection. SQV undergoes extensive hepatic metabolism and intestinal and bile secretion, and has poor and variable oral bioavailability. In previous studies, our group and others have described the...

journal_title：Molecular pharmaceutics

authors： Su Y,Zhang X,Sinko PJ

更新日期：2004-01-12 00:00:00

abstract：:Cholestasis is a significant risk factor for immediate hepatic failure due to ischemia reperfusion (I/R) injury in patients undergoing liver surgery or transplantation. We recently demonstrated that inhibition of Hedgehog (Hh) signaling with cyclopamine (CYA) before I/R prevents liver injury. In this study we hypothes...

journal_title：Molecular pharmaceutics

authors： Pratap A,Panakanti R,Yang N,Lakshmi R,Modanlou KA,Eason JD,Mahato RI

更新日期：2011-06-06 00:00:00

abstract：:Fenretinide, a chemotherapeutic agent for cancer, is water-insoluble and has a very low oral bioavailability. Hence, the objective was to deliver it as an injectable depot and improve the drug solubility and release behavior from poly(lactide-co-glycolide) (PLGA) microspheres by incorporating nonionic surfactants with...

journal_title：Molecular pharmaceutics

authors： Zhang Y,Wischke C,Mittal S,Mitra A,Schwendeman SP

更新日期：2016-08-01 00:00:00

abstract：:Isoniazid (INH) is still one of the two most effective antitubercular drugs and is included in all recommended multitherapeutic regimens. Because of the increasing resistance of Mycobacterium tuberculosis to INH, mainly associated with mutations in the katG gene, new INH-based compounds have been proposed to circumven...

journal_title：Molecular pharmaceutics

authors： Teixeira VH,Ventura C,Leitão R,Ràfols C,Bosch E,Martins F,Machuqueiro M

更新日期：2015-03-02 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：: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：:The bicarbonate buffer capacity is usually considered in a phase-homogeneous system, at equilibrium, with no CO2 transfer between the liquid buffer phase and another phase. However, typically, an in vitro bicarbonate buffer-based system is a phase-heterogeneous system, as it entails continuously sparging (bubbling) th...

journal_title：Molecular pharmaceutics

authors： Al-Gousous J,Sun KX,McNamara DP,Hens B,Salehi N,Langguth P,Bermejo M,Amidon GE,Amidon GL

更新日期：2018-11-05 00:00:00

abstract：:Lung-delivered polymer nanoparticles provoked dysfunction of the essential lung surfactant system. A steric shielding of the nanoparticle surface with poloxamers could minimize the unwanted interference of polymer nanoparticles with the biophysical function of lung surfactant. The extent of poly(styrene) and poly(lact...

journal_title：Molecular pharmaceutics

authors： Beck-Broichsitter M,Bohr A,Ruge CA

更新日期：2017-10-02 00:00:00

abstract：:Progesterone receptor (PR) is a significant biomarker in diseases such as endometriosis and breast, ovarian, and uterine cancers that is associated with disease prognosis and therapeutic efficacy. While receptor status is currently determined by immunohistochemistry assays, the development of noninvasive PR imaging ag...

journal_title：Molecular pharmaceutics

authors： Sukerkar PA,MacRenaris KW,Meade TJ,Burdette JE

更新日期：2011-08-01 00:00:00

abstract：:Water-insoluble anticancer drugs, including paclitaxel, present severe clinical side effects when administered to patients, primarily associated with the toxicity of reagents used to solubilize the drugs. In efforts to develop alternative formulations of water-insoluble anticancer drugs suitable for intravenous admini...

journal_title：Molecular pharmaceutics

authors： Kim JH,Kim Y,Bae KH,Park TG,Lee JH,Park K

更新日期：2015-04-06 00:00:00

abstract：:Therapeutic monoclonal antibody (mAb) candidates that form highly viscous solutions at concentrations above 100 mg/mL can lead to challenges in bioprocessing, formulation development, and subcutaneous drug delivery. Earlier studies of mAbs with concentration-dependent high viscosity have indicated that mAbs with negat...

journal_title：Molecular pharmaceutics

authors： Buck PM,Chaudhri A,Kumar S,Singh SK

更新日期：2015-01-05 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：:Helicobacter pylori inhabits the gastric epithelium and can promote the development of gastric disorders, such as peptic ulcers, acute and chronic gastritis, mucosal lymphoid tissue (MALT), and gastric adenocarcinomas. To use nanotechnology as a tool to increase the antibacterial activity of silver I [Ag(I)] compounds...

journal_title：Molecular pharmaceutics

authors： Almeida Furquim de Camargo B,Soares Silva DE,Noronha da Silva A,Campos DL,Machado Ribeiro TR,Mieli MJ,Borges Teixeira Zanatta M,Bento da Silva P,Pavan FR,Gallina Moreira C,Resende FA,Menegário AA,Chorilli M,Vieira de Godoy Nett

更新日期：2020-07-06 00:00:00

abstract：:Platinum(IV) complexes generally require reduction to reactive Pt(II) species to exert their chemotherapeutic activity. The process of reductive activation of (15)N-labeled (OC-6-43)-bis(acetato)diamminedichloridoplatinum(IV), in the presence of nicotinamide adenine dinucleotide (NADH) and horse heart cytochrome c (cy...

journal_title：Molecular pharmaceutics

authors： Lasorsa A,Stuchlíková O,Brabec V,Natile G,Arnesano F

更新日期：2016-09-06 00:00:00

abstract：:We present an in situ hydrophobic salt forming technique for the encapsulation of weakly hydrophobic, ionizable active pharmaceutical ingredients (API) into stable nanocarriers (NCs) formed via a rapid precipitation process. Traditionally, NC formation via rapid precipitation has been difficult with APIs in this class...

journal_title：Molecular pharmaceutics

authors： Pinkerton NM,Grandeury A,Fisch A,Brozio J,Riebesehl BU,Prud'homme RK

更新日期：2013-01-07 00:00:00

abstract：:Solubility limited compounds require enabling formulations such as amorphous solid dispersions (ASDs) to increase the apparent solubility by dissolving to a concentration higher than the equilibrium solubility of the drug. This may lead to subsequent precipitation and thus the loss of the solubility advantage. Althoug...

journal_title：Molecular pharmaceutics

authors： Han YR,Lee PI

更新日期：2017-01-03 00:00:00

abstract：:As a chronic inflammatory and angiogenic disease with increased morbidity and mortality, rheumatoid arthritis (RA) is characterized by the proliferation of synovial tissue and the accumulation of excessive mononuclear infiltration, which always results in the joint deformity, disability, and eventually the destruction...

journal_title：Molecular pharmaceutics

authors： Wang J,Li Y,Yang Y,Du J,Zhao M,Lin F,Zhang S,Wang B

更新日期：2017-09-05 00:00:00

abstract：:Pyropheophorbide-a (Pyro) is a highly promising photosensitizer for tumor photodynamic therapy (PDT), although its very limited tumor-accumulation ability seriously restricts its clinical applications. A higher accumulation of photosensitizers is very important for the treatment of deeply seated and larger tumors. The...

journal_title：Molecular pharmaceutics

authors： Li W,Tan S,Xing Y,Liu Q,Li S,Chen Q,Yu M,Wang F,Hong Z

更新日期：2018-04-02 00:00:00

abstract：:2-Methoxyestradiol (2MeO-E2) is an endogenous metabolite of estrogen which was initially considered to be inactive. During the last few decades it has been shown that 2MeO-E2 is a promising anticancer drug. In vitro experiments have demonstrated that it has several anticancer activities, and potential to alleviate hyp...

journal_title：Molecular pharmaceutics

authors： Verenich S,Gerk PM

更新日期：2010-12-06 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：:Rho-GTPases are small GTP-binding proteins that contribute to the epithelial-to-mesenchymal transition by regulating several cellular processes including organization of the actin cytoskeleton, cell motility, transcription, and cell proliferation. Overexpression of RhoC-GTPases (RhoC) in breast cancer has been implica...

journal_title：Molecular pharmaceutics

authors： Kaushal N,Durmaz YY,Bao L,Merajver SD,ElSayed ME

更新日期：2015-07-06 00:00:00

abstract：:Cancer stem cells (CSCs) are a subpopulation of cancer cells that have stem cell-like properties and are thought to be responsible for tumor drug resistance and relapse. Therapies that can effectively eliminate CSCs will, therefore, likely inhibit tumor recurrence. The objective of our study was to determine the susce...

journal_title：Molecular pharmaceutics

authors： Sadhukha T,Niu L,Wiedmann TS,Panyam J

更新日期：2013-04-01 00:00:00