Calcium condensed LABL-TAT complexes effectively target gene delivery to ICAM-1 expressing cells.

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：:In order to gain molecular level understanding of drug dissolution into aqueous media, we report the first molecular dynamics (MD) simulation of a drug crystal dissolving. The simulation was performed for acetaminophen crystal Form I dissolving in 0.15 M aqueous NaCl solution at 37 °C. The 10 ns simulation revealed in...

journal_title：Molecular pharmaceutics

authors： Gao Y,Olsen KW

更新日期：2013-03-04 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 present work investigates the influence of electrostatic surface potential distribution of monoclonal antibodies (MAbs) on intermolecular interactions and viscosity. Electrostatic models suggest MAb-1 has a less uniform surface charge distribution than MAb-2. The patches of positive and negative potential on MAb-1...

journal_title：Molecular pharmaceutics

authors： Yadav S,Laue TM,Kalonia DS,Singh SN,Shire SJ

更新日期：2012-04-02 00:00:00

abstract：:We have developed a novel water-dispersible oleic acid (OA)-Pluronic-coated iron oxide magnetic nanoparticle formulation that can be loaded easily with high doses of water-insoluble anticancer agents. Drug partitions into the OA shell surrounding iron oxide nanoparticles, and the Pluronic that anchors at the OA-water ...

journal_title：Molecular pharmaceutics

authors： Jain TK,Morales MA,Sahoo SK,Leslie-Pelecky DL,Labhasetwar V

更新日期：2005-05-01 00:00:00

abstract：:Photodynamic therapy (PDT) is promising for clinical cancer therapy; however, the efficacy was limited as an individual treatment regimen. Here, an approach synergistically combining PDT and nitric oxide (NO) gas therapy along with destruction of the tumor extracellular matrix (ECM) was presented to eliminate cancer. ...

journal_title：Molecular pharmaceutics

authors： Sun Z,Wang X,Liu J,Wang Z,Wang W,Kong D,Leng X

更新日期：2021-01-11 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：: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

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：:A number of folate-based radioconjugates have been synthesized and evaluated for nuclear imaging purposes of folate receptor (FR)-positive tumors and potential therapeutic application. A common shortcoming of radiofolates is, however, a significant accumulation of radioactivity in the kidneys. This situation has been ...

journal_title：Molecular pharmaceutics

authors： Farkas R,Siwowska K,Ametamey SM,Schibli R,van der Meulen NP,Müller C

更新日期：2016-06-06 00:00:00

abstract：:The pharmacological exploitation of resveratrol is hindered by rapid phase-II conjugative metabolism in enterocytes and hepatocytes. One approach to the solution of this problem relies on prodrugs. We report the synthesis and characterization as well as the assessment of in vivo absorption and metabolism of a set of p...

journal_title：Molecular pharmaceutics

authors： Mattarei A,Azzolini M,Carraro M,Sassi N,Zoratti M,Paradisi C,Biasutto L

更新日期：2013-07-01 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：:Amphotericin B is a lifesaving polyene antibiotic used in the treatment of systemic mycoses. Unfortunately, the pharmacological applicability of this drug is limited because of its severe toxic side effects. At the same time, the lack of a well-defined mechanism of selectivity hampers the efforts to rationally design ...

journal_title：Molecular pharmaceutics

authors： Grela E,Wieczór M,Luchowski R,Zielinska J,Barzycka A,Grudzinski W,Nowak K,Tarkowski P,Czub J,Gruszecki WI

更新日期：2018-09-04 00:00:00

abstract：:Current chemotherapy strategies for second-line treatment of relapsed ovarian cancer are unable to effectively treat residual disease post-cytoreduction. The findings presented herein suggest that tissue penetration of drug is not only an issue for large, unresectable tumors, but also for invisible, microscopic lesion...

journal_title：Molecular pharmaceutics

authors： Eetezadi S,De Souza R,Vythilingam M,Lessa Cataldi R,Allen C

更新日期：2015-11-02 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：:Plant or microbial lectins are known to exhibit potent antiviral activities against viruses with glycosylated surface proteins, yet the mechanism(s) by which these carbohydrate-binding proteins exert their antiviral activities is not fully understood. Hepatitis C virus (HCV) is known to possess glycosylated envelope p...

journal_title：Molecular pharmaceutics

authors： Kachko A,Loesgen S,Shahzad-Ul-Hussan S,Tan W,Zubkova I,Takeda K,Wells F,Rubin S,Bewley CA,Major ME

更新日期：2013-12-02 00:00:00

abstract：:The present study explores the potential of polyelectrolyte-coated liposomes for improving the oral deliverability of doxorubicin (Dox). As a part of formulation strategy, stearyl amine was selected as a formulation component to provide positive charge to liposomes, which were subsequently coated with anionic poly(acr...

journal_title：Molecular pharmaceutics

authors： Jain S,Patil SR,Swarnakar NK,Agrawal AK

更新日期：2012-09-04 00:00:00

abstract：:TGX-221 is a highly potent phosphoinositide 3-kinase β (PI3Kβ) inhibitor that holds great promise as a novel chemotherapeutic agent to treat prostate cancer. However, poor solubility and lack of targetability limit its therapeutic applications. The objective of this present study is to develop a peptide-drug conjugate...

journal_title：Molecular pharmaceutics

authors： Tai W,Shukla RS,Qin B,Li B,Cheng K

更新日期：2011-06-06 00:00:00

abstract：:Nanoenabled lipid-based drug delivery systems offer a platform to overcome challenges encountered with current failed leads in the treatment of parasitic and infectious diseases. When prepared with FDA or EMA approved excipients, they can be readily translated without the need for further toxicological studies, while ...

journal_title：Molecular pharmaceutics

authors： Smith L,Serrano DR,Mauger M,Bolás-Fernández F,Dea-Ayuela MA,Lalatsa A

更新日期：2018-07-02 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：: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：:Polymeric micelles are emerging as a highly integrated nanoplatform for cancer targeting, drug delivery and tumor imaging applications. In this study, we describe a multifunctional micelle (MFM) system that is encoded with a lung cancer-targeting peptide (LCP), and encapsulated with superparamagnetic iron oxide (SPIO)...

journal_title：Molecular pharmaceutics

authors： Guthi JS,Yang SG,Huang G,Li S,Khemtong C,Kessinger CW,Peyton M,Minna JD,Brown KC,Gao J

更新日期：2010-02-01 00:00:00

abstract：:Hydrophilic matrices are an effective option for oral controlled release but can face challenges in terms of bioavailability and efficacy when used in conjunction with poorly soluble, weakly basic drugs. Attenuated total reflectance Fourier transform infrared (ATR-FTIR) imaging provides dynamic information relating to...

journal_title：Molecular pharmaceutics

authors： Zahoor FD,Mader KT,Timmins P,Brown J,Sammon C

更新日期：2020-04-06 00:00:00

abstract：:Bisphosphonates (BPs) are a class of bone resorptive drug with a high affinity for the hydroxyapatite structure of bone matrices that are used for the treatment of osteoporosis. However, clinical application is limited by a common toxicity, BP-related osteonecrosis of the jaw. There is emerging evidence that BPs posse...

journal_title：Molecular pharmaceutics

authors： Massey AS,Pentlavalli S,Cunningham R,McCrudden CM,McErlean EM,Redpath P,Ali AA,Annett S,McBride JW,McCaffrey J,Robson T,Migaud ME,McCarthy HO

更新日期：2016-04-04 00:00:00

abstract：:Diagnostic imaging of the liver by ultrasound, computed tomography (CT) and magnetic resonance tomography (MRT) is generally limited to the visualization of the morphology. In order to exploit the intriguing liver tropism of the human hepatitis B virus (HBV) for molecular imaging of the liver, peptidic tracers derived...

journal_title：Molecular pharmaceutics

authors： Müller T,Mehrle S,Schieck A,Haberkorn U,Urban S,Mier W

更新日期：2013-06-03 00:00:00

abstract：:The small molecule fluorescein is commonly used to guide the repair of cerebral spinal fluid leaks (CSFLs) in the clinic. We modified fluorescein so that it is also visible by positron emission tomography (PET). This probe was used to quantitatively track the fast distribution of small molecules in the CSF of rats. We...

journal_title：Molecular pharmaceutics

authors： Guo H,Kommidi H,Maachani UB,Voronina JC,Zhang W,Magge RS,Ivanidze J,Wu AP,Souweidane MM,Aras O,Ting R

更新日期：2019-08-05 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：:This study describes the interactions between two amphiphilic molecules with antileishmanial activity, amphotericin B (AmB) and miltefosine [hexadecylphosphocholine (HePC)], the latter being effective by the oral route. The effect of HePC on the aggregation state of AmB in aqueous solution and the interactions between...

journal_title：Molecular pharmaceutics

authors： Ménez C,Legrand P,Rosilio V,Lesieur S,Barratt G

更新日期：2007-03-01 00:00:00

abstract：:To overcome the P-glycoprotein (P-gp)-induced multidrug resistance (MDR) of cancer cells, a novel copolymer, chitosan-graft-D-α-tocopheryl polyethylene glycol 1000 (TPGS) (CT) was synthesized for doxorubicin (DOX) delivery by the P-gp inhibiting virtue of TPGS. DOX-loaded CT nanoparticles (NPs) were fabricated by a mo...

journal_title：Molecular pharmaceutics

authors： Guo Y,Chu M,Tan S,Zhao S,Liu H,Otieno BO,Yang X,Xu C,Zhang Z

更新日期：2014-01-06 00:00:00

abstract：:The current recombinant human growth hormone (rhGH) therapy requires daily subcutaneous (sc) injections, which results in poor patient compliance, especially in young children. To reduce the dosing frequency, we generated a chimeric protein of rhGH and the Fc-domain of immunoglobulin G (IgG) (rhGH-Fc). The pharmacokin...

journal_title：Molecular pharmaceutics

authors： Kim SJ,Kwak HH,Cho SY,Sohn YB,Park SW,Huh R,Kim J,Ko AR,Jin DK

更新日期：2015-10-05 00:00:00