Abstract:
:The synthesis of a dendrimer based on melamine that displays multiple copies of four orthogonally reactive groups, three on the surface and one on the interior, is described. The three groups on the surface are nucleophilic and include four free hydroxyl groups, four hydroxyl groups masked as tert-butyldiphenylsilyl (TBDPS) ethers, and 16 amines masked as tert-butoxycarbonyl (BOC) groups. The core of the dendrimer displays two electrophilic monochlorotriazines. The dendrimer is available in seven linear steps (eight total steps) at 55% overall yield for the longest linear sequence.
journal_name
Mol Pharmjournal_title
Molecular pharmaceuticsauthors
Lim J,Simanek EEdoi
10.1021/mp050030ekeywords:
subject
Has Abstractpub_date
2005-07-01 00:00:00pages
273-7issue
4eissn
1543-8384issn
1543-8392journal_volume
2pub_type
杂志文章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
pub_type: 杂志文章
doi:10.1021/mp300418r
更新日期:2013-01-07 00:00:00
abstract::The purpose of this study was to examine and compare the melanoma targeting and imaging properties of (64)Cu-NOTA-GGNle-CycMSH(hex) {(64)Cu-1,4,7-triazacyclononane-1,4,7-triacetic acid-Gly-Gly-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-CONH2} and (64)Cu-DOTA-GGNle-CycMSH(hex) {(64)Cu-1,4,7,10-tetraazacyclononane-1,4,7,10-tetraac...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp300246j
更新日期:2012-08-06 00:00:00
abstract::Nonviral transfections of six low passage human colon cancer cell lines using the artificial beta-catenin/TCF-dependent promoter CTP4 demonstrated a high promoter activity which was 1000- to 70000-fold higher than in HeLa control cells. Luciferase gene expression levels obtained with CTP4 in epithelial-like tumor cell...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp0600586
更新日期:2007-01-01 00:00:00
abstract::Graphene-based tumor cell nuclear targeting fluorescent nanoprobes (GTTNs) were synthesized in our laboratory as a kind of nanomaterial and showed good performance for both in vivo and in vitro imaging. GTTNs directly cross the cell membrane and specifically target the tumor cell nucleus via a cell membrane permeabili...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.0c00380
更新日期:2020-07-06 00:00:00
abstract::The impact of OATP drug uptake transporters in drug-drug interactions (DDIs) is increasingly recognized. OATP1B1 and OATP1B3 are human hepatic uptake transporters that can mediate liver uptake of a wide variety of drugs. Recently, we generated transgenic mice with liver-specific expression of human OATP1B1 or OATP1B3 ...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.5b00453
更新日期:2015-12-07 00:00:00
abstract::In this work, we investigated the relationship between various intermolecular hydrogen-bonding (H-bonding) interactions and the miscibility of the model hydrophobic drug naproxen with the hydrophilic polymer polyvinylpyrrolidone (PVP) across an entire composition range of solid dispersions prepared by quasi-equilibriu...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp3003495
更新日期:2012-11-05 00:00:00
abstract::Dendrimers are being explored in many preclinical studies as drug, gene, and imaging agent delivery systems. Understanding their detailed organ, tissue, cellular uptake, and retention can provide valuable insights into their effectiveness as delivery vehicles and the associated toxicity. This work explores a fluoresce...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp400371r
更新日期:2013-12-02 00:00:00
abstract::For efficient and receptor-specific siRNA delivery, a new post-PEGylation strategy was established to provide siRNA polyplexes with targeting and shielding agents. For this purpose, core nanoparticles were formed by complexing siRNA with sequence-defined cationic lipo-oligomers. The T-shaped bis-oleoyl-oligoethanamino...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.6b00102
更新日期:2016-07-05 00:00:00
abstract::Delivery of antigenic protein to the cytosol of antigen-presenting cells (APCs), such as macrophages (MPhi) and dendritic cells (DCs), is required for an efficient CD8 T-cell-mediated immune response. We have previously shown that co-encapsulation of antigenic protein inside pH-sensitive liposomes with listeriolysin O...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp049896v
更新日期:2005-01-01 00:00:00
abstract::Targeted therapies are emerging as a preferred strategy for treatment of cancer and other diseases. To evaluate the effect of high affinity receptors on the rate and extent of tumor penetration of receptor-targeted drugs, we have characterized the kinetics of folate-rhodamine uptake by folate receptor (FR)-expressing ...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp900158d
更新日期:2009-11-01 00:00:00
abstract::Accumulating evidence suggests that EphB4 plays key roles in cancer progression in numerous cancer types. In fact, therapies focusing on EphB4 have become potentially important components of various cancer treatment strategies. However, tumor sensitivity to EphB4 suppression may not be uniform for different cancers. I...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp300461b
更新日期:2013-01-07 00:00:00
abstract::We present a new approach for characterizing drug-polymer interactions in aqueous media, using sedimentation velocity analytical ultracentrifugation (AUC). We investigated the potential interaction of ketoconazole (KTZ), a poorly water-soluble drug, with polyacrylic acid (PAA) and a polyvinyl caprolactam-polyvinyl ace...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.0c00849
更新日期:2021-01-04 00:00:00
abstract::The success of targeted cancer therapy largely relies upon the selection of target and the development of efficient therapeutic agents that specifically bind to the target. In the current study, we chose a cannabinoid CB2 receptor (CB2R) as a new target and used a CB2R-targeted photosensitizer, IR700DX-mbc94, for phot...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp5001923
更新日期:2014-06-02 00:00:00
abstract::DEK protein is critical to the formation of neutrophil extracellular traps (NETs) in rheumatoid arthritis (RA). Blocking DEK using the aptamer DTA via articular injection has been shown to have robust anti-inflammatory efficacy in a previous study. However, DTA is prone to nuclease degradation and renal clearance in v...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.0c00954
更新日期:2021-01-04 00:00:00
abstract::The current regimen of factor IX (FIX) injection is of an episodic format, which leads to limited efficacy. A sustained release dosage form is beneficial in terms of reducing the injection frequency and improving the therapeutic effectiveness. The aim of this study was to formulate a new microsphere form of a FIX-cont...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp200133s
更新日期:2011-10-03 00:00:00
abstract::We report on the fabrication and characterization of dry hybrid lipid-silica nanoparticle based microcapsules with an internal porous matrix structure for encapsulation of poorly soluble drugs, and their delivery properties (in vitro release and lipolysis and in vivo pharmacokinetics demonstrated for indomethacin as a...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp900063t
更新日期:2009-05-01 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
pub_type: 杂志文章
doi:10.1021/mp400686z
更新日期:2014-02-03 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
pub_type: 杂志文章
doi:10.1021/mp200045p
更新日期:2011-08-01 00:00:00
abstract::Robust deposition of extracellular matrix is a significant barrier for delivery of nanotherapeutics and small-molecule anticancer drugs to different tumors including pancreatic ductal adenocarcinoma. Here, we investigated permeation and total uptake of polystyrene nanoparticles of different diameters in 3D multicellul...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.8b01078
更新日期:2019-03-04 00:00:00
abstract::2-Methoxyestradiol (2ME), a natural metabolite of estradiol, has antiproliferative and antiangiogenic activity. However, its clinical success is limited due to poor water solubility and poor pharmacokinetic parameters suggesting the need for a delivery vehicle. In this study we evaluated cathepsin B degradable star-sh...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp400261h
更新日期:2013-10-07 00:00:00
abstract::Bacterial capsular polysaccharides are components of many modern vaccines, but they are weakly immunogenic. Herein, we describe the delivery of pneumococcal capsular polysaccharide serotype-1 (PCP-1) in polylactide polymeric particles to enhance its immunogenicity. Immunization with PCP-1-entrapped particles elicited ...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp400589q
更新日期:2014-03-03 00:00:00
abstract::We have identified and characterized a new solid form of trehalose, the δ form (Tδ) using (13)C solid-state NMR spectroscopy (SSNMR). Tδ is formed from dehydrations of trehalose dihydrate (T(h)) performed at or below 100 °C, and it is generated concurrently with the α form of trehalose (Tα) and amorphous trehalose (T(...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp400104b
更新日期:2013-09-03 00:00:00
abstract::Gold nanoparticles (AuNPs) have a number of physical properties that make them appealing for medical applications. For example, the attenuation of X-rays by gold nanoparticles has led to their use in computed tomography imaging and as adjuvants for radiotherapy. AuNPs have numerous other applications in imaging, thera...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章,评审
doi:10.1021/mp3005885
更新日期:2013-03-04 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
pub_type: 杂志文章
doi:10.1021/mp4001298
更新日期:2013-07-01 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
pub_type: 杂志文章,评审
doi:10.1021/mp100190f
更新日期:2010-12-06 00:00:00
abstract::A novel design of anticancer drug delivery system, based on an electrostatic binding of negatively charged liposomes and cationic metalloporphyrins under physiological conditions, is reported. A lack of cytotoxicity of the iron(III) porphyrin-loaded liposomes and an efficient generation of a toxic hydroxyl radical (OH...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp049936v
更新日期:2004-09-01 00:00:00
abstract::Simvastatin is one of the most widely used active pharmaceutical ingredients for the treatment of hyperlipidemias. Because the compound is employed as a solid in drug formulations, particular attention should be given to the characterization of different polymorphs, their stability domains, and the nature of the phase...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.8b00818
更新日期:2018-11-05 00:00:00
abstract::The acetylcholinesterase inhibitor, acotiamide, improves gastric motility and is clinically used to treat functional dyspepsia. The present study aimed to identify the transporters involved in the distribution of acotiamide in stomach tissue. Acotiamide uptake by the gastric cancer-derived model cell line, Hs746 T, wa...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.9b00894
更新日期:2020-04-06 00:00:00
abstract::The tendency of highly supersaturated solutions of poorly water-soluble drugs to undergo liquid-liquid phase separation (LLPS) into drug-rich and water-rich phases when the concentration exceeds the amorphous solubility, for example, during dissolution of some amorphous solid dispersions, is thought to be advantageous...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/acs.molpharmaceut.8b01117
更新日期:2019-01-07 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
pub_type: 杂志文章
doi:10.1021/mp3007117
更新日期:2013-05-06 00:00:00