Biomimetic 3D Clusters Using Human Adipose Derived Mesenchymal Stem Cells and Breast Cancer Cells: A Study on Migration and Invasion of Breast Cancer Cells.

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：:Our primary objective is to characterize the self-association of rafoxanide in alkaline media. The second objective is to illustrate the feasibility of using rafoxanide micellar solution as the feed solution to prepare amorphous solid dispersion via spray drying. Rafoxanide is a poorly water-soluble drug. It is a weak...

journal_title：Molecular pharmaceutics

authors： Meng F,Liu T,Schneider E,Alzobaidi S,Gil M,Zhang F

更新日期：2017-05-01 00:00:00

abstract：:A combination of microbubbles (MBs) and ultrasound (US) is an emerging method for noninvasive and targeted enhancement of anti-cancer drug uptake. This method showed an increase local drug extravasation in tumor tissue while reducing the systemic adverse effects in various tumor models. The present study aims to evalu...

journal_title：Molecular pharmaceutics

authors： Bressand D,Novell A,Girault A,Raoul W,Fromont-Hankard G,Escoffre JM,Lecomte T,Bouakaz A

更新日期：2019-09-03 00:00:00

abstract：:The encapsulation of glucocorticoids, such as dexamethasone, in nanoparticles (NPs) faces two main issues: a low drug loading and the destabilization of the nanoparticle suspension due to drug crystallization. Here, we successfully formulated a prodrug of dexamethasone, dexamethasone palmitate (DXP), into nanoparticle...

journal_title：Molecular pharmaceutics

authors： Lorscheider M,Tsapis N,Simón-Vázquez R,Guiblin N,Ghermani N,Reynaud F,Canioni R,Abreu S,Chaminade P,Fattal E

更新日期：2019-07-01 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：:By the combined use of powder and single-crystal X-ray diffraction, solid-state NMR, and molecular modeling, the crystal structures of two systems containing the unusually large tenapanor drug molecule have been determined: the free form, ANHY, and a dihydrochloride salt form, 2HCl. Dynamic nuclear polarization (DNP) ...

journal_title：Molecular pharmaceutics

authors： Nilsson Lill SO,Widdifield CM,Pettersen A,Svensk Ankarberg A,Lindkvist M,Aldred P,Gracin S,Shankland N,Shankland K,Schantz S,Emsley L

更新日期：2018-04-02 00:00:00

abstract：:Whether luteolin inhibits HBV replication has not been validated and the underlying mechanism of which has never been elucidated. In this study, we show that luteolin reduces HBV DNA replication in HepG2.2.15 cells. Luteolin effectively inhibited the expression of hepatocyte nuclear factor 4α (HNF4α) and its binding t...

journal_title：Molecular pharmaceutics

authors： Bai L,Nong Y,Shi Y,Liu M,Yan L,Shang J,Huang F,Lin Y,Tang H

更新日期：2016-02-01 00:00:00

abstract：:This paper develops a structure-activity relationship understanding of the way in which surfactant-like dendrons with hydrophilic spermine surface groups and a variety of lipophilic units at their focal points can self-assemble and subsequently bind to DNA with high affinity. The choice of functional group at the foca...

journal_title：Molecular pharmaceutics

authors： Jones SP,Gabrielson NP,Wong CH,Chow HF,Pack DW,Posocco P,Fermeglia M,Pricl S,Smith DK

更新日期：2011-04-04 00:00:00

abstract：:The Biopharmaceutical Classification System (BCS) guidance issued by the FDA allows waivers for in vivo bioavailability and bioequivalence studies for immediate-release (IR) solid oral dosage forms only for BCS class I drugs. However, a number of drugs within BCS class III have been proposed to be eligible for biowaiv...

journal_title：Molecular pharmaceutics

authors： Tsume Y,Amidon GL

更新日期：2010-08-02 00:00:00

abstract：:Structural features of lysine-conjugated antibody-drug conjugate (ADC) from humanized IgG1 were studied by small-angle X-ray scattering (SAXS). As the physicochemical properties of the cytotoxic drug (payload) and linker may impact the conformational and colloidal stabilities of the conjugated monoclonal antibody (mAb...

journal_title：Molecular pharmaceutics

authors： Law-Hine D,Rudiuk S,Bonestebe A,Ienco R,Huille S,Tribet C

更新日期：2019-12-02 00:00:00

abstract：:Efficient drug delivery to the skin is essential for the treatment of major dermatologic diseases, such as eczema, psoriasis and acne. However, many compounds penetrate the skin barrier poorly and require optimized formulations to ensure their bioavailability. Here, stimulated Raman scattering (SRS) microscopy, a rece...

journal_title：Molecular pharmaceutics

authors： Saar BG,Contreras-Rojas LR,Xie XS,Guy RH

更新日期：2011-06-06 00:00:00

abstract：:Cell penetrating peptides (CPPs) have been extensively studied in polyelectrolyte complexes as a means to enhance the transfection efficiency of plasmid DNA (pDNA). Increasing the molecular weight of CPPs often enhances gene expression but poses a risk of increased cytotoxicity and immunogenicity compared to low molec...

journal_title：Molecular pharmaceutics

authors： Alhakamy NA,Berkland CJ

更新日期：2013-05-06 00:00:00

abstract：:P-glycoprotein (Pgp) is highly expressed on blood-brain barrier (BBB) and glioblastoma (GB) cells, particularly on cancer stem cells (SC). Pgp recognizes a broad spectrum of substrates, limiting the therapeutic efficacy of several chemotherapeutic drugs in eradicating GB SC. Finding effective and safe inhibitors of Pg...

journal_title：Molecular pharmaceutics

authors： Salaroglio IC,Abate C,Rolando B,Battaglia L,Gazzano E,Colombino E,Costamagna C,Annovazzi L,Mellai M,Berardi F,Capucchio MT,Schiffer D,Riganti C

更新日期：2019-08-05 00:00:00

abstract：:There is a great need for delivery strategies capable of efficiently localizing drugs to the damaged myocardium that do not require direct intramyocardial injection of therapeutic molecules. In the work discussed here, we exploited the myocardium-specific upregulation of matrix metalloproteinases (MMPs) that occurs du...

journal_title：Molecular pharmaceutics

authors： Nguyen J,Sievers R,Motion JP,Kivimäe S,Fang Q,Lee RJ

更新日期：2015-04-06 00:00:00

abstract：:Recently we characterized an unusual switch in the internalization mechanism of the monomeric and dimeric forms of the cell-penetrating peptide RDLWEMMMVSLACQY. Here, we observed both energy-dependent and energy-independent modes of peptide uptake by the target B-lymphocytes WI-L2-729HF2, suggesting that higher-order ...

journal_title：Molecular pharmaceutics

authors： Kim Y,Lillo A,Moss JA,Janda KD

更新日期：2005-11-01 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：: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：:An effective short interfering RNA (siRNA) delivery system protects the siRNA from degradation, facilitates its cellular uptake, and promotes its release into the cytoplasm. Local administration of siRNA presents advantages over systemic administration, such as the possibility to use lower doses and allow local and su...

journal_title：Molecular pharmaceutics

authors： Borgheti-Cardoso LN,Kooijmans SAA,Fens MHAM,van der Meel R,Vicentini FTMC,Fantini MCA,Bentley MVLB,Schiffelers RM

更新日期：2017-05-01 00:00:00

abstract：:The biodistribution of dendronized iron oxides, NPs10@D1_DOTAGA and melanin-targeting NPs10@D1_ICF_DOTAGA, was studied in vivo using magnetic resonance imaging (MRI) and planar scintigraphy through [177Lu]Lu-radiolabeling. MRI experiments showed high contrast power of both dendronized nanoparticles (DPs) and hepatobil...

journal_title：Molecular pharmaceutics

authors： Bordeianu C,Parat A,Piant S,Walter A,Zbaraszczuk-Affolter C,Meyer F,Begin-Colin S,Boutry S,Muller RN,Jouberton E,Chezal JM,Labeille B,Cinotti E,Perrot JL,Miot-Noirault E,Laurent S,Felder-Flesch D

更新日期：2018-02-05 00:00:00

abstract：:Constitutive activation of signal transducer and activator of transcription 3 (STAT3) in tumor cells and tumor associated dendritic cells (DCs) plays a major role in the progression of cancer. JSI-124 (cucurbitacin I) is a potent inhibitor of STAT3; however, its poor solubility and nonspecificity limit its effectivene...

journal_title：Molecular pharmaceutics

authors： Garg SM,Vakili MR,Molavi O,Lavasanifar A

更新日期：2017-08-07 00:00:00

abstract：:The applicability of the computational docking approach was investigated to create a novel method for quick additive screening to inhibit the crystallization taking place in amorphous drugs. Surface energy and attachment energy were utilized to recognize the morphologically most important crystal faces. The surfaces (...

journal_title：Molecular pharmaceutics

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

更新日期：2012-10-01 00:00:00

abstract：:Carbonic anhydrase IX (CAIX) plays an important role in glioma cell proliferation, invasion, metastasis, and resistance to radiotherapy and chemotherapy. An effective and noninvasive PET molecular imaging agent targeting CAIX would help its diagnosis and treatment but is not currently available. Recently, a low-molecu...

journal_title：Molecular pharmaceutics

authors： Yang X,Zhu H,Yang X,Li N,Huang H,Liu T,Guo X,Xu X,Xia L,Deng C,Tian X,Yang Z

更新日期：2019-04-01 00:00:00

abstract：:Compared with peripheral tumors, glioma is very difficult to treat, not only because it has general features of tumor but also because the therapy has been restricted by the brain-blood barrier (BBB). The two main features of tumor growth are angiogenesis and proliferation of tumor cells. RNA interference (RNAi) can d...

journal_title：Molecular pharmaceutics

authors： Kuang Y,Jiang X,Zhang Y,Lu Y,Ma H,Guo Y,Zhang Y,An S,Li J,Liu L,Wu Y,Liang J,Jiang C

更新日期：2016-05-02 00:00:00

abstract：:Protein drugs play an important role in modern day medicine. Typically, these proteins are formulated as liquids requiring cold chain processing. To circumvent the cold chain and achieve better storage stability, these proteins can be dried in the presence of carbohydrates. We demonstrate that thermal gradient mid- an...

journal_title：Molecular pharmaceutics

authors： Mensink MA,Šibík J,Frijlink HW,van der Voort Maarschalk K,Hinrichs WLJ,Zeitler JA

更新日期：2017-10-02 00:00:00

abstract：:Photodynamic therapy, a procedure that uses a photosensitizer to enable light therapy selectively at diseased sites, remains underutilized in oncological clinic. To further improve its cancer selectivity, we developed a polymeric nanosystem by conjugating a photosensitizer IRDye 700DX (IR700) and cancer targeting RGD ...

journal_title：Molecular pharmaceutics

authors： Zhao Y,Li F,Mao C,Ming X

更新日期：2018-07-02 00:00:00

abstract：:Hydrophobic single-wall carbon nanohorns (SWNHs) were dispersed in aqueous media by noncovalently modifying their surfaces with conjugate molecules comprised of polyethylene glycol (PEG) and a peptide aptamer (NHBP-1) that specifically bind to the surfaces of the SWNHs. The conjugates were synthesized by coupling PEG ...

journal_title：Molecular pharmaceutics

authors： Matsumura S,Ajima K,Yudasaka M,Iijima S,Shiba K

更新日期：2007-09-01 00:00:00

abstract：:The transfer of genetic material into cells using nonviral vectors offers unique potential for therapeutics; however, the efficacy of delivery depends upon a poorly understood, multistep pathway, limiting the prospects for successful gene delivery. Mechanistic insight into DNA association and release has been hampered...

journal_title：Molecular pharmaceutics

authors： Prevette LE,Nikolova EN,Al-Hashimi HM,Banaszak Holl MM

更新日期：2012-09-04 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：: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

abstract：:We have recently reported that by converting a perforin inhibitor into an l-type amino acid transporter 1 (LAT1)-utilizing prodrug its cellular uptake can be greatly increased. The aim of the present study was to determine the in vivo and brain pharmacokinetics of two perforin inhibitors and their LAT1-utilizing prodr...

journal_title：Molecular pharmaceutics

authors： Gynther M,Pickering DS,Spicer JA,Denny WA,Huttunen KM

更新日期：2016-07-05 00:00:00