Acetal derivatives as prodrugs of resveratrol.

abstract：:L cells have attracted particular interest because of the pleiotropic effects of their secreted peptides (i.e., glucagon-like peptide (GLP) 1 and 2, peptide YY (PYY)). L cells express different G-protein-coupled receptors (GPCRs) that can be activated by endogenous ligands found in the gut lumen. We herein hypothesize...

journal_title：Molecular pharmaceutics

authors： Beloqui A,Alhouayek M,Carradori D,Vanvarenberg K,Muccioli GG,Cani PD,Préat V

更新日期：2016-12-05 00:00:00

abstract：:It is well-known that renal cell carcinomas (RCCs) are resistant to classical cytotoxic anticancer drugs. Therefore, facilitating the impact of anticancer drugs by altering the cell phenotype should be a useful strategy for circumventing this. We developed a multifunctional envelope-type nanodevice (MEND) as an in viv...

journal_title：Molecular pharmaceutics

authors： Sakurai Y,Hatakeyama H,Akita H,Harashima H

更新日期：2014-08-04 00:00:00

abstract：:A big hurdle for the use of protein-based drugs is that they are easily degraded by proteases in the human body. In an attempt to solve this problem, we show the possibility to functionalize TM encapsulin nanoparticles with an mEETI-II knottin miniprotein from the cysteine-stabilized knot class. The resulting particle...

journal_title：Molecular pharmaceutics

authors： Klem R,de Ruiter MV,Cornelissen JJLM

更新日期：2018-08-06 00:00:00

abstract：:Itraconazole is a drug of choice for the treatment of severe fungal infections and parasitic diseases, but its use is limited by its low water solubility and varying bioavailability. New self-emulsifying drug delivery systems (SEDDS) based on PEGylated bile acids (BA-PEGs) were designed and prepared, where the number ...

journal_title：Molecular pharmaceutics

authors： Le Dévédec F,Strandman S,Hildgen P,Leclair G,Zhu XX

更新日期：2013-08-05 00:00:00

abstract：:Despite advances in cancer therapies, glioblastoma multiforme treatment remains inefficient due to the brain-blood barrier (BBB) inhibitory activity and to the low temozolomide (TMZ) chemotherapeutic selectivity. To improve therapeutic outcomes, in this work we propose two strategies, (i) photodynamic therapy (PDT) as...

journal_title：Molecular pharmaceutics

authors： Pellosi DS,Paula LB,de Melo MT,Tedesco AC

更新日期：2019-03-04 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：:Gene therapy represents a potential efficient approach of disease prevention and therapy. However, due to their poor in vivo stability, gene molecules need to be associated with delivery systems to overcome extracellular and intracellular barriers and allow access to the site of action. Cationic polymeric nanoparticle...

journal_title：Molecular pharmaceutics

authors： Navarro G,Pan J,Torchilin VP

更新日期：2015-02-02 00:00:00

abstract：:Liposomes are widely used for systemic delivery of chemotherapeutic agents to reduce their nonspecific side effects. Gemcitabine (Gem) makes a great candidate for liposomal encapsulation due to the short half-life and nonspecific side effects; however, it has been difficult to achieve liposomal Gem with high drug load...

journal_title：Molecular pharmaceutics

authors： Tamam H,Park J,Gadalla HH,Masters AR,Abdel-Aleem JA,Abdelrahman SI,Abdelrahman AA,Lyle LT,Yeo Y

更新日期：2019-07-01 00:00:00

abstract：:The endothelial cells lining the capillaries supplying the brain with oxygen and nutrients form a formidable barrier known as the blood-brain barrier (BBB), which exhibits selective permeability to small drug molecules and virtually impermeable to macromolecular therapeutics. Current in vitro BBB models fail to replic...

journal_title：Molecular pharmaceutics

authors： Wang JD,Khafagy el-S,Khanafer K,Takayama S,ElSayed ME

更新日期：2016-03-07 00:00:00

abstract：:Peritoneal fibrosis (PF) is a common complication of long-term peritoneal dialysis (PD). It is considered as the main reason for dialysis inadequacy and PD withdrawal. Transforming growth factor beta (TGF-β) regulates the expression of stromal cell-derived factor 1 (SDF-1α) and its receptor C-X-C chemokine receptor ty...

journal_title：Molecular pharmaceutics

authors： Asifullah K,Zhou Z,He W,Gao K,Khan MW,Faisal R,Muhammad H,Sun M

更新日期：2019-06-03 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：:In this study, the photochemical internalization (PCI) technique was adopted in a nanoparticle-based antigen delivery system to enhance antigen-specific CD8+ T cell immune response for cancer immunotherapy. Pheophorbide A, a hydrophobic photosensitizer, grafted with polyethylenimine (PheoA-PEI) with endosome escape ac...

journal_title：Molecular pharmaceutics

authors： Zhang C,Zhang J,Shi G,Song H,Shi S,Zhang X,Huang P,Wang Z,Wang W,Wang C,Kong D,Li C

更新日期：2017-05-01 00:00:00

abstract：:Tablets which were binary mixtures of pioglitazone hydrochloride (PioHCl) with magnesium stearate (MgSt), croscarmellose sodium (CCS), microcrystalline cellulose, or lactose monohydrate were prepared. Two sets of experiments, using intact tablets, were performed. (i) Tablets containing PioHCl (90% w/w) and MgSt were e...

journal_title：Molecular pharmaceutics

authors： Koranne S,Govindarajan R,Suryanarayanan R

更新日期：2017-04-03 00:00:00

abstract：:Polymeric systems have been extensively studied as polyelectrolyte complexes to enhance the cellular delivery and transfection efficiency of genetic materials, such as plasmid DNA (pDNA). Here, self-assembled nanoparticles were formulated by complexation of hyaluronic acid (HA)-conjugated poly(ethylene glycol) (HA-PEG...

journal_title：Molecular pharmaceutics

authors： Aldawsari HM,Dhaliwal HK,Aljaeid BM,Alhakamy NA,Banjar ZM,Amiji MM

更新日期：2019-01-07 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：:In the drug discovery setting, the ability to rapidly identify drug absorption risk in preclinical species at high doses from easily measured physical properties is desired. This is due to the large number of molecules being evaluated and their high attrition rate, which make resource-intensive in vitro and in silico ...

journal_title：Molecular pharmaceutics

authors： Wuelfing WP,Daublain P,Kesisoglou F,Templeton A,McGregor C

更新日期：2015-04-06 00:00:00

abstract：:The maytansinoid antibody-drug conjugates (ADCs) in clinical development for cancer therapy each contain a derivative of the microtubule-targeting agent, maytansine, covalently attached to the antibody via an engineered linker. A sample of any of these conjugates contains molecules with different numbers of maytansino...

journal_title：Molecular pharmaceutics

authors： Goldmacher VS,Amphlett G,Wang L,Lazar AC

更新日期：2015-06-01 00:00:00

abstract：:The foreign body reaction (FBR), one of the body's defense mechanisms against foreign materials, results in loss of implant biocompatibility. A popular strategy to prevent FBR is the constant release of dexamethasone in the tissue surrounding the implant. However, FBR prevention has not been sufficiently studied in la...

journal_title：Molecular pharmaceutics

authors： Kastellorizios M,Tipnis N,Papadimitrakopoulos F,Burgess DJ

更新日期：2015-09-08 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

authors： Cao J,Su J,An M,Yang Y,Zhang Y,Zuo J,Zhang N,Zhao Y

更新日期：2021-01-04 00:00:00

abstract：:Drug repositioning is an important drug development strategy as it saves the time and efforts exerted in drug discovery. Since reepithelization of the cornea is a critical problem, we envisioned that the anticonvulsant phenytoin sodium can promote reepithelization of corneal ulcers as it was repurposed for skin wound ...

journal_title：Molecular pharmaceutics

authors： Mahmoud DB,Afifi SA,El Sayed NS

更新日期：2020-10-05 00:00:00

abstract：:The particular characteristics of the tumor microenvironment have the potential to strongly promote tumor growth, metastasis and angiogenesis and induce drug resistance. Therefore, the development of effective, systemic therapeutic approaches specifically based on the tumor microenvironment is highly desirable. Hypoxi...

journal_title：Molecular pharmaceutics

authors： Liu XQ,Xiong MH,Shu XT,Tang RZ,Wang J

更新日期：2012-10-01 00:00:00

abstract：:Porous silicon microparticles presenting pathogen-associated molecular patterns mimic pathogens, enhancing internalization of the microparticles and activation of antigen presenting dendritic cells. We demonstrate abundant uptake of microparticles bound by the TLR-4 ligands LPS and MPL by murine bone marrow-derived de...

journal_title：Molecular pharmaceutics

authors： Meraz IM,Melendez B,Gu J,Wong ST,Liu X,Andersson HA,Serda RE

更新日期：2012-07-02 00:00:00

abstract：:There are an increasing number of studies showing the order of drug presentation plays a critical role in achieving optimal combination therapy. Here, a nanoparticle design is presented using ion pairing and drug-polymer conjugate for the sequential delivery of gefitinib (Gi) and doxorubicin (Dox) targeting epidermal ...

journal_title：Molecular pharmaceutics

authors： Zhou Z,Jafari M,Sriram V,Kim J,Lee JY,Ruiz-Torres SJ,Waltz SE

更新日期：2017-12-04 00:00:00

abstract：:meta-Tetra(hydroxyphenyl)chlorin (mTHPC) is one of the most potent second-generation photosensitizers, clinically used for photodynamic therapy (PDT) of head and neck squamous cell carcinomas. However, improvements are still required concerning its present formulation (i.e., Foscan, a solution of mTHPC in ethanol/prop...

journal_title：Molecular pharmaceutics

authors： Liu Y,Scrivano L,Peterson JD,Fens MHAM,Hernández IB,Mesquita B,Toraño JS,Hennink WE,van Nostrum CF,Oliveira S

更新日期：2020-04-06 00:00:00

abstract：:Solid-state hydrogen-deuterium exchange with mass spectrometric analysis (ssHDX) is a promising method for characterizing proteins in amorphous solids. Though analysis of HDX kinetics is informative and well-established in solution, application of these methods to solid samples is complicated by possible heterogeneiti...

journal_title：Molecular pharmaceutics

authors： Sophocleous AM,Topp EM

更新日期：2012-04-02 00:00:00

abstract：:The interaction with cervicovaginal mucus presents the potential to impact the performance of drug nanocarriers. These systems must migrate through this biological fluid in order to deliver their drug payload to the underlying mucosal surface. We studied the ability of dapivirine-loaded polycaprolactone (PCL)-based na...

journal_title：Molecular pharmaceutics

authors： das Neves J,Rocha CM,Gonçalves MP,Carrier RL,Amiji M,Bahia MF,Sarmento B

更新日期：2012-11-05 00:00:00

abstract：:Retinal pigment epithelium, which forms the outer blood-retinal barrier, is a critical barrier for transport of drugs to the retina. The purpose of this study was to develop a pigmented MDCK (P-MDCK) cell line as a rapidly established in vitro model for the outer blood-retinal barrier to assess the influence of melani...

journal_title：Molecular pharmaceutics

authors： Kadam RS,Scheinman RI,Kompella UB

更新日期：2012-11-05 00:00:00

abstract：:The tumor microenvironments are often acidic and overexpress specific enzymes. In this work, we synthesized a poly(AA-b-NIPAAm) copolymer (PAA-b-PNIPAAm) using a reversible addition-fragmentation chain transfer (RAFT) polymerization method. PAA-b-PNIPAAm and a cationic protein (protamine) were self-assembled into nano...

journal_title：Molecular pharmaceutics

authors： Don TM,Lu KY,Lin LJ,Hsu CH,Wu JY,Mi FL

更新日期：2017-12-04 00:00:00

abstract：:Organic anion transporting polypeptides 1B1 and 1B3 are transporters selectively expressed on the basolateral membrane of the hepatocyte. Several studies reveal that they are involved in drug-drug interactions, cancer, and hyperbilirubinemia. In this study, we developed a set of classification models for OATP1B1 and 1...

journal_title：Molecular pharmaceutics

authors： Kotsampasakou E,Brenner S,Jäger W,Ecker GF

更新日期：2015-12-07 00:00:00

abstract：:Approximately, 40-70% of active pharmaceutical ingredients (API) are severely limited by their extremely poor aqueous solubility, and consequently, there is a high demand for excipients that can be used to formulate clinically relevant doses of these drug candidates. Here, proof-of-concept studies demonstrate the pote...

journal_title：Molecular pharmaceutics

authors： Hettiarachchi G,Samanta SK,Falcinelli S,Zhang B,Moncelet D,Isaacs L,Briken V

更新日期：2016-03-07 00:00:00