High-Content Surface and Total Expression siRNA Kinase Library Screen with VX-809 Treatment Reveals Kinase Targets that Enhance F508del-CFTR Rescue.

abstract：:Bioadhesive nanoparticles based on poly(vinyl methyl ether/maleic anhydride) (PVMMA) and poly(ethylene glycol) methyl ether-b-poly(d,l-lactic acid) (mPEG-b-PLA) were produced by the emulsification solvent evaporation method. Paclitaxel was utilized as the model drug, with an encapsulation efficiency of up to 90.2 ± 4....

journal_title：Molecular pharmaceutics

authors： Wang Q,Li C,Ren T,Chen S,Ye X,Guo H,He H,Zhang Y,Yin T,Liang XJ,Tang X

更新日期：2017-10-02 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：: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：:Helicobacter pylori inhabits the gastric epithelium and can promote the development of gastric disorders, such as peptic ulcers, acute and chronic gastritis, mucosal lymphoid tissue (MALT), and gastric adenocarcinomas. To use nanotechnology as a tool to increase the antibacterial activity of silver I [Ag(I)] compounds...

journal_title：Molecular pharmaceutics

authors： Almeida Furquim de Camargo B,Soares Silva DE,Noronha da Silva A,Campos DL,Machado Ribeiro TR,Mieli MJ,Borges Teixeira Zanatta M,Bento da Silva P,Pavan FR,Gallina Moreira C,Resende FA,Menegário AA,Chorilli M,Vieira de Godoy Nett

更新日期：2020-07-06 00:00:00

abstract：:The amorphization of the readily crystallizable therapeutic ingredient and food additive, menthol, was successfully achieved by inclusion of neat menthol in mesoporous silica matrixes of 3.2 and 5.9 nm size pores. Menthol amorphization was confirmed by the calorimetric detection of a glass transition. The respective g...

journal_title：Molecular pharmaceutics

authors： Cordeiro T,Castiñeira C,Mendes D,Danède F,Sotomayor J,Fonseca IM,Gomes da Silva M,Paiva A,Barreiros S,Cardoso MM,Viciosa MT,Correia NT,Dionisio M

更新日期：2017-09-05 00:00:00

abstract：:Polymer therapeutics have shown promise as tumor-targeted drug delivery systems in mice. The multivalency of polymers allows the attachment of different functional agents to a polymeric backbone, including chemotherapeutic and antiangiogenic drugs, as well as targeting moieties, such as the bone-targeting agent alendr...

journal_title：Molecular pharmaceutics

authors： Miller K,Eldar-Boock A,Polyak D,Segal E,Benayoun L,Shaked Y,Satchi-Fainaro R

更新日期：2011-08-01 00:00:00

abstract：:Conjugation with a cell penetrating peptide such as Tat presents an effective approach to improve the intracellular accumulation of molecules with low membrane permeability. This strategy, however, leads to a reduced cellular entry of molecules that can cross cell membrane effectively. We report here that covalent lin...

journal_title：Molecular pharmaceutics

authors： Zhang P,Lock LL,Cheetham AG,Cui H

更新日期：2014-03-03 00:00:00

abstract：:Ipratropium bromide, an anticholinergic drug used for the treatment of asthma and chronic obstructive pulmonary disease, has low oral bioavailability, but systemic exposure, superior to oral administration, can be achieved by inhalation. Therefore, we investigated the pulmonary absorption mechanism of ipratropium usin...

journal_title：Molecular pharmaceutics

authors： Nakamura T,Nakanishi T,Haruta T,Shirasaka Y,Keogh JP,Tamai I

更新日期：2010-02-01 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：:Iron oxide nanoparticles have great potential as diagnostic and therapeutic agents in cancer and other diseases; however, biological aggregation severely limits their function in vivo. Aggregates can cause poor biodistribution, reduced heating capability, and can confound their visualization and quantification by magn...

journal_title：Molecular pharmaceutics

authors： Hurley KR,Ring HL,Etheridge M,Zhang J,Gao Z,Shao Q,Klein ND,Szlag VM,Chung C,Reineke TM,Garwood M,Bischof JC,Haynes CL

更新日期：2016-07-05 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：:The purpose of the present study was to investigate the effect of seed particles on the precipitation behavior of weak base drugs in the small intestine. A simple in vitro infusion method was used to mimic in vivo processes. Dipyridamole, pioglitazone, topiroxostat, chlorpromazine, cinnarizine, and ketoconazole were u...

journal_title：Molecular pharmaceutics

authors： Koyama H,Ito M,Terada K,Sugano K

更新日期：2016-08-01 00:00:00

abstract：:Photodynamic therapy (PDT) is promising for clinical cancer therapy; however, the efficacy was limited as an individual treatment regimen. Here, an approach synergistically combining PDT and nitric oxide (NO) gas therapy along with destruction of the tumor extracellular matrix (ECM) was presented to eliminate cancer. ...

journal_title：Molecular pharmaceutics

authors： Sun Z,Wang X,Liu J,Wang Z,Wang W,Kong D,Leng X

更新日期：2021-01-11 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：:Extracellular β-glucuronidase (β-GUS) in tumors has been investigated as a target enzyme for prodrug therapy. However, despite encouraging preclinical results, animal studies also indicate that the success of prodrug therapy might be limited by the insufficient prodrug-converting enzyme activity, especially in small t...

journal_title：Molecular pharmaceutics

authors： Antunes IF,Haisma HJ,Elsinga PH,Di Gialleonardo V,van Waarde A,Willemsen AT,Dierckx RA,de Vries EF

更新日期：2012-11-05 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：:Integrin αvβ3 is a cell adhesion molecule involved in the progression and invasion of glioblastoma, making it an attractive target for the diagnosis of glioblastoma. Although some integrin αvβ3 specific ligands, such as RGD and its mimetic peptides (Cilengitide), have been devoted in detecting glioblastoma, their clin...

journal_title：Molecular pharmaceutics

authors： Zhang L,Shan X,Meng X,Gu T,Guo L,An X,Jiang Q,Ge H,Ning X

更新日期：2019-09-03 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：:Preferential interactions of formulation excipients govern their overall interactions with protein molecules, and molecular dynamics simulations allow for the examination of the interactions at the molecular level. We used molecular dynamics simulations to examine the interactions of sorbitol, sucrose, and trehalose w...

journal_title：Molecular pharmaceutics

authors： Cloutier T,Sudrik C,Mody N,Sathish HA,Trout BL

更新日期：2019-08-05 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：:Poly(ethylcyanoacrylate) (PECA) nanoparticles containing the bioactive d-Lys(6)-GnRH were manufactured by an in situ interfacial polymerization process using a w/o-microemulsion template containing the peptide in the dispersed aqueous pseudophase of the microemulsion. Polymeric nanoparticles were characterized using P...

journal_title：Molecular pharmaceutics

authors： Kafka AP,Kleffmann T,Rades T,McDowell A

更新日期：2009-09-01 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：:Solubility limited compounds require enabling formulations such as amorphous solid dispersions (ASDs) to increase the apparent solubility by dissolving to a concentration higher than the equilibrium solubility of the drug. This may lead to subsequent precipitation and thus the loss of the solubility advantage. Althoug...

journal_title：Molecular pharmaceutics

authors： Han YR,Lee PI

更新日期：2017-01-03 00:00:00

abstract：:TGX-221 is a highly potent phosphoinositide 3-kinase β (PI3Kβ) inhibitor that holds great promise as a novel chemotherapeutic agent to treat prostate cancer. However, poor solubility and lack of targetability limit its therapeutic applications. The objective of this present study is to develop a peptide-drug conjugate...

journal_title：Molecular pharmaceutics

authors： Tai W,Shukla RS,Qin B,Li B,Cheng K

更新日期：2011-06-06 00:00:00

abstract：:Our work has focused on defining the utility of fluorine (19F)-labeled bile acid analogues and magnetic resonance imaging (MRI) to identify altered bile acid transport in vivo. In the current study, we explored the ability of this approach to differentiate fibroblast growth factor-15 (FGF15)-deficient from wild-type (...

journal_title：Molecular pharmaceutics

authors： Metry M,Felton J,Cheng K,Xu S,Ai Y,Xue F,Raufman JP,Polli JE

更新日期：2018-11-05 00:00:00

abstract：:The most abundant polyphenol in green tea, epigallocatechin-3-gallate (EGCg), has recently received considerable attention due to the discovery of numerous health-promoting bioactivities. Despite reports of its poor oral bioavailability, EGCg has been included in many dietary supplement formulations. Conventional pref...

journal_title：Molecular pharmaceutics

authors： Smith AJ,Kavuru P,Arora KK,Kesani S,Tan J,Zaworotko MJ,Shytle RD

更新日期：2013-08-05 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

authors： Jia N,Zhang S,Shao P,Bagia C,Janjic JM,Ding Y,Bai M

更新日期：2014-06-02 00:00:00

abstract：:The formation of a gel coat around xanthan (Xan) tablets, empty or loaded with pentoxifylline (PF), and its release in media differing in pH and ionic strength by NMR, MR imaging, and two release methods were studied. The T1 and T2 NMR relaxation times in gels depend predominantly on Xan concentration; the presence of...

journal_title：Molecular pharmaceutics

authors： Mikac U,Sepe A,Baumgartner S,Kristl J

更新日期：2016-03-07 00:00:00

abstract：:A highly versatile and step-economical route to a new class of guanidinium-rich molecular transporters and evaluation of their ability to complex, deliver, and release siRNA are described. These new drug/probe delivery systems are prepared in only two steps, irrespective of length or composition, using an organocataly...

journal_title：Molecular pharmaceutics

authors： Wender PA,Huttner MA,Staveness D,Vargas JR,Xu AF

更新日期：2015-03-02 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