Targeted transferrin-modified polymeric micelles: enhanced efficacy in vitro and in vivo in ovarian carcinoma.

abstract：:Lipophilic cations such as phosphonium salts can accumulate in mitochondria of heart in response to the negative inner-transmembrane potentials. Two phosphonium salts [(18)F]FMBTP and [(18)F]mFMBTP were prepared and evaluated as potential myocardial perfusion imaging (MPI) agents in this study. The cations were radiol...

journal_title：Molecular pharmaceutics

authors： Zhao Z,Yu Q,Mou T,Liu C,Yang W,Fang W,Peng C,Lu J,Liu Y,Zhang X

更新日期：2014-11-03 00:00:00

abstract：:The goal of this study was to develop a (66)Ga-based positron emission tomography (PET) tracer for noninvasive imaging of CD105 expression during tumor angiogenesis, a hallmark of cancer. (66)Ga was produced using a cyclotron with (nat)Zn or isotopically enriched (66)Zn targets. TRC105, a chimeric anti-CD105 monoclona...

journal_title：Molecular pharmaceutics

authors： Engle JW,Hong H,Zhang Y,Valdovinos HF,Myklejord DV,Barnhart TE,Theuer CP,Nickles RJ,Cai W

更新日期：2012-05-07 00:00:00

abstract：:Lipid nanoemulsions are being investigated for the parenteral administration of poorly soluble drugs. A narrow particle size distribution in these formulations is a prerequisite for meaningful research and safe administration to patients. Autoclaving a poloxamer-stabilized trimyristin nanoemulsion resulted in moderate...

journal_title：Molecular pharmaceutics

authors： Göke K,Roese E,Bunjes H

更新日期：2018-08-06 00:00:00

abstract：:The human organic anion-transporting polypeptides OATP1B1 (SLCO1B1) and OATP1B3 (SLCO1B3) are liver-enriched membrane transporters of major importance to hepatic uptake of numerous endogenous compounds, including bile acids, steroid conjugates, hormones, and drugs, including the 3-hydroxy-3-methylglutaryl Co-A reducta...

journal_title：Molecular pharmaceutics

authors： DeGorter MK,Ho RH,Leake BF,Tirona RG,Kim RB

更新日期：2012-04-02 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：:Cyclic RGD (cRGD) peptide-conjugated boronated albumin was developed to direct toward integrin αvβ3, which overexpresses on many cancer cells. A stepwise conjugation of c[RGDfK(Mal)] and maleimide-conjugated closo-dodecaborate (MID) to bovine serum albumin (BSA) afforded cRGD-MID-BSA, which was noncytotoxic toward bot...

journal_title：Molecular pharmaceutics

authors： Kawai K,Nishimura K,Okada S,Sato S,Suzuki M,Takata T,Nakamura H

更新日期：2020-10-05 00:00:00

abstract：:Drug transporter expression and function at the blood-brain barrier is altered in Alzheimer's disease (AD). However, the impact of AD on the expression of transporters and metabolizing enzymes in peripheral tissues has received little attention. The current study evaluated the expression of drug transporters and metab...

journal_title：Molecular pharmaceutics

authors： Pan Y,Omori K,Ali I,Tachikawa M,Terasaki T,Brouwer KLR,Nicolazzo JA

更新日期：2018-09-04 00:00:00

abstract：:Dissolution is a crucial process for the oral delivery of drug products. Before being absorbed through epithelial cell membranes to reach the systemic circulation, drugs must first dissolve in the human gastrointestinal (GI) tract. In vivo and in vitro dissolutions are complex because of their dependency upon the drug...

journal_title：Molecular pharmaceutics

authors： Salehi N,Al-Gousous J,Mudie DM,Amidon GL,Ziff RM,Amidon GE

更新日期：2020-10-05 00:00:00

abstract：:Rho-GTPases are small GTP-binding proteins that contribute to the epithelial-to-mesenchymal transition by regulating several cellular processes including organization of the actin cytoskeleton, cell motility, transcription, and cell proliferation. Overexpression of RhoC-GTPases (RhoC) in breast cancer has been implica...

journal_title：Molecular pharmaceutics

authors： Kaushal N,Durmaz YY,Bao L,Merajver SD,ElSayed ME

更新日期：2015-07-06 00:00:00

abstract：:We have developed a macromolecular prodrug platform based on poly(l-lysine succinylated) (PLS) that targets scavenger receptor A1 (SR-A1), a receptor expressed by myeloid and endothelial cells. We demonstrate the selective uptake of PLS by murine macrophage, RAW 264.7 cells, which was eliminated upon cotreatment with ...

journal_title：Molecular pharmaceutics

authors： Stevens DM,Adiseshaiah P,Dasa SSK,Potter TM,Skoczen SL,Snapp KS,Cedrone E,Patel N,Busman-Sahay K,Rosen EP,Sykes C,Cottrell M,Dobrovolskaia MA,Estes JD,Kashuba ADM,Stern ST

更新日期：2020-10-05 00:00:00

abstract：:The complement system plays an important role in host innate immunity, and its activation can be exploited as a potential strategy for vaccine adjuvants. Herein, a pH-responsive micellar vaccine platform (COOH-NPs) was developed using a carboxyl-modified diblock copolymer of poly(2-ethyl-2-oxazoline)-poly(d,l-lactide)...

journal_title：Molecular pharmaceutics

authors： Li C,Lu Y,Chen Q,Hu H,Zhao X,Qiao M,Chen D

更新日期：2019-06-03 00:00:00

abstract：:The ATP-binding cassette (ABC) drug transporter ABCG2 can actively efflux a wide variety of chemotherapeutic agents out of cancer cells and subsequently reduce the intracellular accumulation of these drugs. Therefore, the overexpression of ABCG2 often contributes to the development of multidrug resistance (MDR) in can...

journal_title：Molecular pharmaceutics

authors： Wu CP,Hsiao SH,Murakami M,Lu YJ,Li YQ,Huang YH,Hung TH,Ambudkar SV,Wu YS

更新日期：2017-08-07 00:00:00

abstract：:Some specific types of tumor cells and tumor endothelial cells represented CD13 proteins and act as receptors for Asn-Gly-Arg (NGR) motifs containing peptide. These CD13 receptors can be specifically recognized and bind through the specific sequence of cyclic NGR (cNGR) peptide and presented more affinity and specific...

journal_title：Molecular pharmaceutics

authors： Gupta M,Chashoo G,Sharma PR,Saxena AK,Gupta PN,Agrawal GP,Vyas SP

更新日期：2014-03-03 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：: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：:Renal ischemia/reperfusion (I/R) injury causes high mortality and morbidity during renal procedures, yet current drugs should be used at high doses or for long periods due to lack of tissue specificity. In previous work we described a novel mycophenolic acid-glucosamine conjugate (MGC) that targets the proximal tubule...

journal_title：Molecular pharmaceutics

authors： Wang X,Xiong M,Zeng Y,Sun X,Gong T,Zhang Z

更新日期：2014-10-06 00:00:00

abstract：:Amphotericin B (AmB) is a lifesaving polyene antibiotic used widely to treat deep-seated mycoses. Both the pharmaceutical effectiveness as well as toxic side effects depend on molecular organization of the drug. In the present study, we analyzed steady-state fluorescence, fluorescence anisotropy spectra, fluorescence ...

journal_title：Molecular pharmaceutics

authors： Wasko P,Luchowski R,Tutaj K,Grudzinski W,Adamkiewicz P,Gruszecki WI

更新日期：2012-05-07 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：: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

abstract：:Glioblastoma multiforme (GBM) is the most commonly encountered subtype of deadly brain cancer in human adults. It has a high recurrence rate and shows aggressive proliferation. The novel cytotoxic agent temozolomide (TMZ) is now frequently applied as the first-line chemotherapeutic treatment for GBM; however, a consid...

journal_title：Molecular pharmaceutics

authors： Bi Y,Li H,Yi D,Sun Y,Bai Y,Zhong S,Song Y,Zhao G,Chen Y

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：:Improving the therapeutic index of anticancer agents is an enormous challenge. Targeting decreases the side effects of the therapeutic agents by delivering the drugs to the intended destination. Nanocarriers containing the nuclear localizing peptide sequences (NLS) translocate to the cell nuclei. However, the nuclear ...

journal_title：Molecular pharmaceutics

authors： Anajafi T,Yu J,Sedigh A,Haldar MK,Muhonen WW,Oberlander S,Wasness H,Froberg J,Molla MS,Katti KS,Choi Y,Shabb JB,Srivastava DK,Mallik S

更新日期：2017-06-05 00:00:00

abstract：:The antiviral drug tenofovir (TFV) is orally administered as the fumarate salt of its disoproxil prodrug (TFV disoproxil fumarate (TDF)). TFV is a dianion at physiological pH and, as a result, has poor lipid membrane permeability. Administration of the lipophilic and cell-permeable prodrug, TFV disoproxil, enhances th...

journal_title：Molecular pharmaceutics

authors： Durand-Gasselin L,Van Rompay KK,Vela JE,Henne IN,Lee WA,Rhodes GR,Ray AS

更新日期：2009-07-01 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 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

authors： Hate SS,Reutzel-Edens SM,Taylor LS

更新日期：2019-01-07 00:00:00

abstract：:Deferoxamine mesylate (DFO) is an FDA-approved, hexadentate iron chelator routinely used to alleviate systemic iron burden in thalassemia major and sickle cell patients. Iron accumulation in these disease states results from the repeated blood transfusions required to manage these conditions. Iron accumulation has als...

journal_title：Molecular pharmaceutics

authors： Farr AC,Xiong MP

更新日期：2021-02-01 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

authors： Gaedtke L,Pelisek J,Lipinski KS,Wrighton CJ,Wagner E

更新日期：2007-01-01 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：: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：: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