Combinatorial Intracellular Delivery Screening of Anticancer Drugs.

abstract：:The 1:1 cocrystal of the antifungal agent ketoconazole with p-aminobenzoic acid was successfully crystallized and systematically characterized by a physical and pharmacological point of view. Crystal structure determination confirmed the cocrystal identity, giving full insight in its crystal packing and degree of diso...

journal_title：Molecular pharmaceutics

authors： Martin F,Pop M,Kacso I,Grosu IG,Miclăuş M,Vodnar D,Lung I,Filip GA,Olteanu ED,Moldovan R,Nagy A,Filip X,Bâldea I

更新日期：2020-03-02 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：:Multidrug resistance (MDR) is the major obstacle for chemotherapy. In a previous study, we have successfully synthesized a novel doxorubicin (DOX) derivative modified by triphenylphosphonium (TPP) to realize mitochondrial delivery of DOX and showed the potential of this compound to overcome DOX resistance in MDA-MB-43...

journal_title：Molecular pharmaceutics

authors： Liu HN,Guo NN,Wang TT,Guo WW,Lin MT,Huang-Fu MY,Vakili MR,Xu WH,Chen JJ,Wei QC,Han M,Lavasanifar A,Gao JQ

更新日期：2018-03-05 00:00:00

abstract：:Viral nanotechnology is an emerging and highly interdisciplinary field in which viral nanoparticles (VNPs) are applied in diverse areas such as electronics, energy and next-generation medical devices. VNPs have been developed as candidates for novel materials, and are often described as "programmable" because they can...

journal_title：Molecular pharmaceutics

authors： Pokorski JK,Steinmetz NF

更新日期：2011-02-07 00:00:00

abstract：:One hypothesis for persisting HIV-associated neurocognitive disorders (HAND) in effectively treated individuals is the limited permeation of antiretroviral agents (ARV) across the blood-brain barrier (BBB). However, the physicochemical factors limiting the brain entry of a given ARV and the mutual interactions of comb...

journal_title：Molecular pharmaceutics

authors： Marzolini C,Mueller R,Li-Blatter X,Battegay M,Seelig A

更新日期：2013-06-03 00:00:00

abstract：:Although nanocarriers hold promise for cancer chemotherapy, their intracellular drug delivery pathways are not fully understood. In particular, the influence of nanocarrier stability on cellular uptake is still uncertain. By physically loading hydrophobic FRET probes, we revealed different intracellular drug delivery ...

journal_title：Molecular pharmaceutics

authors： Lee SY,Tyler JY,Kim S,Park K,Cheng JX

更新日期：2013-09-03 00:00:00

abstract：:The bladder is an important tissue in which to evaluate xenobiotic drug interactions and toxicities due to the concentration of parent drug and hepatic/enteric-derived metabolites in the urine as a result of renal excretion. Breaching of the barrier provided by the bladder epithelial lining (the urothelium) can expose...

journal_title：Molecular pharmaceutics

authors： Baker SC,Shabir S,Southgate J

更新日期：2014-07-07 00:00:00

abstract：:Targeting of drugs administered systemically relies on the higher affinity of ligands for specific receptors to obtain selectivity in drug response. However, achieving the same goal inside the bladder is much easier with an intelligent pharmaceutical approach that restricts drug effects by exploiting the pelvic anatom...

journal_title：Molecular pharmaceutics

authors： Tyagi P,Wu PC,Chancellor M,Yoshimura N,Huang L

更新日期：2006-07-01 00:00:00

abstract：:In this manuscript, we have reported a novel 2D fingerprint-based artificial neural network QSAR (FANN-QSAR) method in order to effectively predict biological activities of structurally diverse chemical ligands. Three different types of fingerprints, namely, ECFP6, FP2 and MACCS, were used in FANN-QSAR algorithm devel...

journal_title：Molecular pharmaceutics

authors： Myint KZ,Wang L,Tong Q,Xie XQ

更新日期：2012-10-01 00:00:00

abstract：:In this work we measured self-diffusion coefficients of 5 drugs (aspirin, caffeine, ethionamide, salicylic acid, and paracetamol) and 11 biologically active compounds of similar structure in deuterated water and 1-octanol by NMR. It has been found that an increase in the van der Waals volume of the molecules of the st...

journal_title：Molecular pharmaceutics

authors： Blokhina SV,Volkova TV,Golubev VA,Perlovich GL

更新日期：2017-10-02 00:00:00

abstract：:The systemic pharmacokinetics and pharmacodynamics of small molecules are determined by subcellular transport phenomena. Although approaches used to study the subcellular distribution of small molecules have gradually evolved over the past several decades, experimental analysis and prediction of cellular pharmacokinet...

journal_title：Molecular pharmaceutics

authors： Zheng N,Tsai HN,Zhang X,Rosania GR

更新日期：2011-10-03 00:00:00

abstract：:Amino acids derivative are well established molecular probes for diagnosis of a variety of cancer using positron emission tomography (PET). Recently, boramino acid (BAAs) was found as a prospective molecular platform for developing PET tracer. The objective of this study was to develop a 18F-labeled alanine derivative...

journal_title：Molecular pharmaceutics

authors： Liu H,Han Y,Li J,Qin M,Fu Q,Wang C,Liu Z

更新日期：2018-03-05 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

authors： Lesniak WG,Mishra MK,Jyoti A,Balakrishnan B,Zhang F,Nance E,Romero R,Kannan S,Kannan RM

更新日期：2013-12-02 00:00:00

abstract：:Fluid bed coating has been shown to be a suitable manufacturing technique to formulate poorly soluble drugs in glass solutions. Layering inert carriers with a drug-polymer mixture enables these beads to be immediately filled into capsules, thus avoiding additional, potentially destabilizing, downstream processing. In ...

journal_title：Molecular pharmaceutics

authors： Dereymaker A,Scurr DJ,Steer ED,Roberts CJ,Van den Mooter G

更新日期：2017-04-03 00:00:00

abstract：:Selective ligands to the peripheral benzodiazepine receptor (PBR) may induce apoptosis and cell cycle arrest. An overexpression of PBR in certain cancers allowed us to consider the use of highly selective ligands to PBR for receptor-mediated drug targeting to tumors. With this in mind, we prepared PBR-targeted nanopar...

journal_title：Molecular pharmaceutics

authors： Musacchio T,Laquintana V,Latrofa A,Trapani G,Torchilin VP

更新日期：2009-03-01 00:00:00

abstract：:New bifunctional hexa- and octadentate analogues of the hydroxamate-containing siderophore desferrichrome (DFC) have been synthesized and evaluated as 89Zr-chelating agents for immunoPET applications. The in vitro and in vivo inertness of these new ligands, Orn3-hx (hexadentate) and Orn-4hx derivatives (octadentate), ...

journal_title：Molecular pharmaceutics

authors： Adams CJ,Wilson JJ,Boros E

更新日期：2017-08-07 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：:RNA oligonucleotides capable of inducing controlled immunostimulation combined with specific oncogene silencing via an RNA interference (RNAi) mechanism provide synergistic inhibition of cancer cell growth. With this concept, we previously designed a potent immunostimulatory long double stranded RNA, referred to as li...

journal_title：Molecular pharmaceutics

authors： Sajeesh S,Lee TY,Hong SW,Dua P,Choe JY,Kang A,Yun WS,Song C,Park SH,Kim S,Li C,Lee DK

更新日期：2014-03-03 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：: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：:This study determined intraluminal ethanol concentrations (stomach and duodenum) in fed healthy volunteers after the consumption of common alcoholic beverages (beer, wine, and whisky). The results of this study were compared with a previous study in fasted volunteers. Five healthy volunteers were recruited in a crosso...

journal_title：Molecular pharmaceutics

authors： Rubbens J,Riethorst D,Brouwers J,Wolfs K,Adams E,Tack J,Augustijns P

更新日期：2017-12-04 00:00:00

abstract：:Sodium lauryl sulfate (SLS), as an effective surfactant, is often used as a solubilizer and/or wetting agent in various dosage forms for the purpose of improving the solubility and dissolution of lipophilic, poorly water-soluble drugs. This study aims to understand the impact of SLS on the solution behavior and bioava...

journal_title：Molecular pharmaceutics

authors： Chen Y,Wang S,Wang S,Liu C,Su C,Hageman M,Hussain M,Haskell R,Stefanski K,Qian F

更新日期：2016-08-01 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：:Targeted gene delivery using nonviral vectors is a highly touted scheme to reduce the potential for toxic or immunological side effects by reducing dose. In previous reports, TAT polyplexes with DNA have shown relatively poor gene delivery. The transfection efficiency has been enhanced by condensing TAT/DNA complexes ...

journal_title：Molecular pharmaceutics

authors： Khondee S,Baoum A,Siahaan TJ,Berkland C

更新日期：2011-06-06 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：: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

authors： Müller K,Kessel E,Klein PM,Höhn M,Wagner E

更新日期：2016-07-05 00:00:00

abstract：:Oleanolic acid (OA) is a well-known pentacyclic triterpenoid compound, which has been used as a dietary supplement and is supplied as an over-the-counter drug for the treatment of human liver diseases. These are reasons for the low bioavailability of OA which have restricted its wider application. In this study, two O...

journal_title：Molecular pharmaceutics

authors： Yu Z,Sun W,Peng W,Yu R,Li G,Jiang T

更新日期：2016-05-02 00:00:00

abstract：:An artificial stomach duodenum (ASD) model has been used to demonstrate the performance difference between two formulations of LY2300559, a low-solubility acidic developmental drug. The two formulations investigated were a conventional high-shear wet granulation (HSWG) formulation and a solid dispersion formulation. A...

journal_title：Molecular pharmaceutics

authors： Polster CS,Wu SJ,Gueorguieva I,Sperry DC

更新日期：2015-04-06 00:00:00

abstract：:The successful applicability of gene therapy approaches will heavily rely on the development of efficient and safe nonviral gene delivery vectors, for example, cell-penetrating peptides (CPPs). CPPs can condense oligonucleotides and plasmid DNA (pDNA) into nanoparticles, thus allowing the transfection of genetic mater...

journal_title：Molecular pharmaceutics

authors： Veiman KL,Mäger I,Ezzat K,Margus H,Lehto T,Langel K,Kurrikoff K,Arukuusk P,Suhorutšenko J,Padari K,Pooga M,Lehto T,Langel Ü

更新日期：2013-01-07 00:00:00

abstract：:Isoniazid (INH) is still one of the two most effective antitubercular drugs and is included in all recommended multitherapeutic regimens. Because of the increasing resistance of Mycobacterium tuberculosis to INH, mainly associated with mutations in the katG gene, new INH-based compounds have been proposed to circumven...

journal_title：Molecular pharmaceutics

authors： Teixeira VH,Ventura C,Leitão R,Ràfols C,Bosch E,Martins F,Machuqueiro M

更新日期：2015-03-02 00:00:00