Luteolin Inhibits Hepatitis B Virus Replication through Extracellular Signal-Regulated Kinase-Mediated Down-Regulation of Hepatocyte Nuclear Factor 4α Expression.

abstract：:Glutamic acid is a commonly used linker to form dimeric peptides with enhanced binding affinity than their corresponding monomeric counterparts. We have previously labeled NOTA-Bn-NCS-PEG3-E[c(RGDyK)]2 (NOTA-PRGD2) [1] with [(18)F]AlF and (68)Ga for imaging tumor angiogenesis. The p-SCN-Bn-NOTA was attached to E[c(RGD...

journal_title：Molecular pharmaceutics

authors： Lang L,Ma Y,Kiesewetter DO,Chen X

更新日期：2014-11-03 00:00:00

abstract：:Lung cancer is a kind of malignant tumor with high morbidity and metastasis tendency. Gambogic acid (GA) has demonstrated significant antitumor activity in vitro, but its poor water-solubility and adverse effects restrict its application in vivo and in clinic. In this study, a passive-targeting GA delivery system was ...

journal_title：Molecular pharmaceutics

authors： Yang Y,Cai H,Yuan X,Xu H,Hu Y,Rui X,Wu J,Chen J,Li J,Gao X,Yin D

更新日期：2018-05-07 00:00:00

abstract：:Invasion and metastasis of cancer directly related to human death have been associated with interactions among many different types of cells and three-dimensional (3D) tissue matrices. Precise mechanisms related to cancer invasion and metastasis still remain unknown due to their complexities. Development of tumor micr...

journal_title：Molecular pharmaceutics

authors： Park MH,Song B,Hong S,Kim SH,Lee K

更新日期：2016-07-05 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：: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：:Lipid-based nanoparticles are considered as promising candidates for delivering siRNA into the cytoplasm of targeted cells. However, in vivo efficiency of these nanoparticles is critically dependent on formulation strategies of lipid-siRNA complexes. Adsorption of serum proteins to lipid-siRNA complexes and its charge...

journal_title：Molecular pharmaceutics

authors： Dar GH,Gopal V,Rao NM

更新日期：2015-02-02 00:00:00

abstract：:Despite holding promise for cancer immunotherapy, the strong pro-inflammatory properties of lipopolysaccharide (LPS) also account for severe localized and systemic side effects, restricting its administrable dosage and the possibility of chronic dosing. Herein, we exploited the surface-active properties of LPS molecul...

journal_title：Molecular pharmaceutics

authors： Shetab Boushehri MA,Yazeji T,Stein V,Lamprecht A

更新日期：2019-11-04 00:00:00

abstract：:Intra-articular (IA) injection of thermoresponsive hydrogels coupled with microparticles (MPs) possess the benefit of sustaining the anti-inflammatory drug effect within the joint cavity for rheumatoid arthritis treatment. Star-shaped thermoresponsive poly(polyethylene glycol) methacrylate [Poly(PEGMA)] copolymers wer...

journal_title：Molecular pharmaceutics

authors： Abou-ElNour M,Soliman ME,Skouras A,Casettari L,Geneidi AS,Ishak RAH

更新日期：2020-06-01 00:00:00

abstract：:The melanocortin 1 receptor (MC1R) is overexpressed in most melanoma metastases, making it a promising target for imaging of melanomas. In this study, the expression of MC1R in a large fraction of patients with melanoma was confirmed using mRNA and tissue microarray. Here, we have characterized the in vivo tumor and t...

journal_title：Molecular pharmaceutics

authors： Tafreshi NK,Silva A,Estrella VC,McCardle TW,Chen T,Jeune-Smith Y,Lloyd MC,Enkemann SA,Smalley KS,Sondak VK,Vagner J,Morse DL

更新日期：2013-08-05 00:00:00

abstract：:Metastatic breast cancer is incurable. The goal of this study was to develop a positron emission tomography (PET)/near-infrared fluorescent (NIRF) probe for imaging CD105 expression in breast cancer experimental lung metastasis. TRC105, a chimeric anti-CD105 antibody, was dual-labeled with a NIRF dye (IRDye 800CW) and...

journal_title：Molecular pharmaceutics

authors： Hong H,Zhang Y,Severin GW,Yang Y,Engle JW,Niu G,Nickles RJ,Chen X,Leigh BR,Barnhart TE,Cai W

更新日期：2012-08-06 00:00:00

abstract：:Deep generative adversarial networks (GANs) are the emerging technology in drug discovery and biomarker development. In our recent work, we demonstrated a proof-of-concept of implementing deep generative adversarial autoencoder (AAE) to identify new molecular fingerprints with predefined anticancer properties. Another...

journal_title：Molecular pharmaceutics

authors： Kadurin A,Nikolenko S,Khrabrov K,Aliper A,Zhavoronkov A

更新日期：2017-09-05 00:00:00

abstract：:Dry powder inhalations (DPI) of microparticles containing isoniazid (INH) and rifabutin (RFB) are under preclinical development for use in pulmonary tuberculosis. Microparticles containing 0.25, 2.5, or 25 mg of each drug were administered daily for 90 days to rhesus macaques (n = 4/group). Single inhalations or intra...

journal_title：Molecular pharmaceutics

authors： Kumar Verma R,Mukker JK,Singh RS,Kumar K,Verma PR,Misra A

更新日期：2012-04-02 00:00:00

abstract：:Peptide nucleic acids have a number of features that make them an ideal platform for the development of in vitro biological probes and tools. Unfortunately, their inability to pass through membranes has limited their in vivo application as diagnostic and therapeutic agents. Herein, we describe the development of catio...

journal_title：Molecular pharmaceutics

authors： Fang H,Zhang K,Shen G,Wooley KL,Taylor JS

更新日期：2009-03-01 00:00:00

abstract：:Combinatorial chemistry has enabled the production of very potent drugs that might otherwise suffer from poor solubility and low oral bioavailability. One approach to increase solubility is to make the drug amorphous, which leads to problems associated with drug stability. To improve stability, one option is to molecu...

journal_title：Molecular pharmaceutics

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

更新日期：2014-07-07 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：:Our previous studies have shown that multidrug resistance protein 2 (MRP2) is overexpressed in tamoxifen-resistant MCF-7 breast cancer cells (TAMR-MCF-7 cells) and forkhead box-containing protein, O subfamily1 (FoxO1), functions as a key regulator of multidrug resistance 1 (MDR1) gene transcription. This study aimed t...

journal_title：Molecular pharmaceutics

authors： Choi HK,Cho KB,Phuong NT,Han CY,Han HK,Hien TT,Choi HS,Kang KW

更新日期：2013-07-01 00:00:00

abstract：:Today, about 50% of men and 15-30% of women suffer from hair loss as well as the associated psychological impact. Drug therapy, especially through topical administration, is the main treatment strategy for stimulating hair regrowth. However, challenges exist due to the skin barrier that hinders drug penetration. To th...

journal_title：Molecular pharmaceutics

authors： Yang G,Chen G,Gu Z

更新日期：2021-02-01 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：:Studies were conducted to develop antibody- and fluorescence-labeled superparamagnetic iron oxide nanoparticle (SPIO) nanotheranostics for magnetic resonance imaging (MRI) and fluorescence imaging of cancer cells and pH-dependent intracellular drug release. SPIO nanoparticles (10 nm) were coated with amphiphilic polym...

journal_title：Molecular pharmaceutics

authors： Zou P,Yu Y,Wang YA,Zhong Y,Welton A,Galbán C,Wang S,Sun D

更新日期：2010-12-06 00:00:00

abstract：:In women with human epidermal growth factor 2 (HER2)-positive breast cancer, the improved control of systemic disease with new therapies has unmasked brain metastases that historically would have remained clinically silent. The efficacy of therapeutic agents against brain metastases is limited by their inability to pe...

journal_title：Molecular pharmaceutics

authors： Wyatt EA,Davis ME

更新日期：2020-02-03 00:00:00

abstract：:Photodynamic therapy (PDT) is a light-induced chemical reaction that produces localized tissue damage for the treatment of cancers and other nonmalignant conditions. The activation of photosensitizers in a target tissue is accomplished with a specific light source in the presence of molecular oxygen. In the clinic, pa...

journal_title：Molecular pharmaceutics

authors： Shieh MJ,Peng CL,Chiang WL,Wang CH,Hsu CY,Wang SJ,Lai PS

更新日期：2010-08-02 00:00:00

abstract：:The potential use of poly(dimethylsiloxane) (PDMS) as an in vitro biomimetic analogue of the passive drug absorption process in the human gastrointestinal tract (GI) is assessed. PDMS is biomimetic because of similarities in small molecule transport, such as mechanism, ionization selectivity, lipophilicity. Nine molec...

journal_title：Molecular pharmaceutics

authors： Sinko PD,Gidley D,Vallery R,Lamoureux A,Amidon GL,Amidon GE

更新日期：2017-12-04 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：:Eperisone hydrochloride (EH) is widely used as a muscle relaxant for patients with muscular contracture, low back pain, or spasticity. Human serum albumin (HSA) is a highly soluble negatively charged, endogenous and abundant plasma protein ascribed with the ligand binding and transport properties. The current study wa...

journal_title：Molecular pharmaceutics

authors： Rabbani G,Baig MH,Lee EJ,Cho WK,Ma JY,Choi I

更新日期：2017-05-01 00:00:00

abstract：:The adenosine triphosphate-binding cassette transporter P-glycoprotein (ABCB1/Abcb1a) restricts at the blood-brain barrier (BBB) brain distribution of many drugs. ABCB1 may be involved in drug-drug interactions (DDIs) at the BBB, which may lead to changes in brain distribution and central nervous system side effects o...

journal_title：Molecular pharmaceutics

authors： Wanek T,Römermann K,Mairinger S,Stanek J,Sauberer M,Filip T,Traxl A,Kuntner C,Pahnke J,Bauer F,Erker T,Löscher W,Müller M,Langer O

更新日期：2015-09-08 00:00:00

abstract：:Doxorubicin (DOX) is one of the most commonly used antineoplastic agents, but its clinical application is oftentimes coupled with severe side effects. Selective delivery of DOX to tumors via nanosized drug carrier represents an attractive approach to this problem. Previously, we developed a dual functional nanomicella...

journal_title：Molecular pharmaceutics

authors： Lu J,Zhao W,Huang Y,Liu H,Marquez R,Gibbs RB,Li J,Venkataramanan R,Xu L,Li S,Li S

更新日期：2014-11-03 00:00:00

abstract：:An important aspect to ensure progress in biomedicine is the fundamental understanding of the interaction of cells and tissue with (bio)materials. The consideration of shear stress in drug delivery and/or tissue engineering remains largely unexplored. To illustrate the fundamental relevance, we employ a microfluidic s...

journal_title：Molecular pharmaceutics

authors： Hosta-Rigau L,Städler B

更新日期：2013-07-01 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 this study, the polymer-free electrospinning was performed in order to produce cyclodextrin/ibuprofen inclusion complex nanofibers, which could have potential as the fast dissolving oral drug delivery system. Ibuprofen is a poorly water-soluble nonsteroidal anti-inflammatory drug; however, the water solubility of i...

journal_title：Molecular pharmaceutics

authors： Celebioglu A,Uyar T

更新日期：2019-10-07 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