C1290

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关键词:'C1290'

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Cotargeting MAPK and PI3K signaling with concurrent radiotherapy as a strategy for the treatment of pancreatic cancer.

Terence M Williams et al.

Molecular cancer therapeutics, 11(5), 1193-1202 (2012-03-14)

There is an urgent need for the development of novel therapies to treat pancreatic cancer, which is among the most lethal of all cancers. KRAS-activating mutations, which are found in more than 90% of pancreatic adenocarcinomas, drive tumor dependency on

In vitro selective inhibition of human UDP-glucuronosyltransferase (UGT) 1A4 by finasteride, and prediction of in vivo drug-drug interactions.

Seung Jun Lee et al.

Toxicology letters, 232(2), 458-465 (2014-12-03)

In the present study, we evaluated the inhibitory potentials of finasteride for the major human hepatic UDP-glucuronosyltransferases (UGTs) (UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9, UGT2B7, and UGT2B15) in vitro using LC-MS/MS by specific marker reactions in human liver microsomes (except for

Characterization of a novel CYP2C9 mutation (1009C>A) detected in a warfarin-sensitive patient.

Shun-Bin Luo et al.

Journal of pharmacological sciences, 125(2), 150-156 (2014-07-31)

Warfarin is the most frequently prescribed anticoagulant for the long-term treatment in the clinic. Recent studies have shown that polymorphic alleles within the CYP2C9, VKORC1, and CYP4F2 genes are related to the warfarin dosage requirement. In this study, a novel

Physical characterization of drug:polymer dispersion behavior in polyethylene glycol 4000 solid dispersions using a suite of complementary analytical techniques.

Dipy M Vasa et al.

Journal of pharmaceutical sciences, 103(9), 2911-2923 (2014-05-16)

Fifteen model drugs were quenched from 3:1 (w/w) mixtures with polyethylene glycol 4000 (PEG4000). The resulting solids were characterized using powder X-ray diffraction (PXRD), analysis of pair distribution function-transformed PXRD data (where appropriate), hot-stage polarized light microscopy, and differential scanning

Metabolic drug-drug interaction potential of macrolactin A and 7-O-succinyl macrolactin A assessed by evaluating cytochrome P450 inhibition and induction and UDP-glucuronosyltransferase inhibition in vitro.

Soo Hyeon Bae et al.

Antimicrobial agents and chemotherapy, 58(9), 5036-5046 (2014-06-04)

Macrolactin A (MA) and 7-O-succinyl macrolactin A (SMA), polyene macrolides containing a 24-membered lactone ring, show antibiotic effects superior to those of teicoplanin against vancomycin-resistant enterococci and methicillin-resistant Staphylococcus aureus. MA and SMA are currently being evaluated as antitumor agents

PKB/Akt partners with Dab2 in albumin endocytosis.

Kelly Koral et al.

American journal of physiology. Renal physiology, 302(8), F1013-F1024 (2012-01-06)

Albumin in the glomerular filtrate is normally retrieved by concerted efforts of clathrin, LDL-type receptor megalin- and clathrin-associated sorting proteins. In glomerular diseases, albumin overload triggers a proapoptotic and inflammatory response contributing to tubulointerstitial fibrosis and tubular atrophy. The relationship

Selective detection and quantitation of organic molecule crystallization by second harmonic generation microscopy.

Duangporn Wanapun et al.

Analytical chemistry, 82(13), 5425-5432 (2010-06-03)

Second order nonlinear optical imaging of chiral crystals (SONICC) was applied to selectively detect crystal formation at early stages and characterize the kinetics of nucleation and growth. SONICC relies on second harmonic generation (SHG), a nonlinear optical effect that only

Pharmacogenomic analysis of ATP-sensitive potassium channels coexpressing the common type 2 diabetes risk variants E23K and S1369A.

Veronica Y Lang et al.

Pharmacogenetics and genomics, 22(3), 206-214 (2012-01-03)

The common ATP-sensitive potassium (KATP) channel variants E23K and S1369A, found in the KCNJ11 and ABCC8 genes, respectively, form a haplotype that is associated with an increased risk for type 2 diabetes. Our previous studies showed that KATP channel inhibition

NF-κB Signaling Negatively Regulates Osteoblast Dedifferentiation during Zebrafish Bone Regeneration.

Rashmi Mishra et al.

Developmental cell, 52(2), 167-182 (2019-12-24)

Dedifferentiation of mature cells is an intriguing cellular process associated with regeneration of several organs. During zebrafish fin regeneration, osteoblasts dedifferentiate to osteogenic progenitors that provide source cells for bone restoration. We performed a high-content in vivo chemical screen for regulators

Targeting the AKT/GSK3β/cyclin D1/Cdk4 survival signaling pathway for eradication of tumor radioresistance acquired by fractionated radiotherapy.

Tsutomu Shimura et al.

International journal of radiation oncology, biology, physics, 80(2), 540-548 (2011-03-15)

Radioresistance is a major cause of treatment failure of radiotherapy (RT) in human cancer. We have recently revealed that acquired radioresistance of tumor cells induced by fractionated radiation is attributable to cyclin D1 overexpression as a consequence of the downregulation

Chlorpropamide--alcohol flush: the case in favour.

C Johnston et al.

Diabetologia, 26(1), 1-5 (1984-01-01)

Activation of FOXO3a is sufficient to reverse mitogen-activated protein/extracellular signal-regulated kinase kinase inhibitor chemoresistance in human cancer.

Jer-Yen Yang et al.

Cancer research, 70(11), 4709-4718 (2010-05-21)

Drug resistance is a central challenge of cancer therapy that ultimately leads to treatment failure. In this study, we characterized a mechanism of drug resistance that arises to AZD6244, an established mitogen-activated protein/extracellular signal-regulated kinase kinase (MEK) 1/2 inhibitor currently

N-methylnicotinamide and nicotinamide N-methyltransferase are associated with microRNA-1291-altered pancreatic carcinoma cell metabolome and suppressed tumorigenesis.

Hui-Chang Bi et al.

Carcinogenesis, 35(10), 2264-2272 (2014-08-15)

The cell metabolome comprises abundant information that may be predictive of cell functions in response to epigenetic or genetic changes at different stages of cell proliferation and metastasis. An unbiased ultra-performance liquid chromatography-mass spectrometry-based metabolomics study revealed a significantly altered

Autophagy of an Amyloid-like Translational Repressor Regulates Meiotic Exit.

Fei Wang et al.

Developmental cell, 52(2), 141-151 (2020-01-29)

We explored the potential for autophagy to regulate budding yeast meiosis. Following pre-meiotic DNA replication, we blocked autophagy by chemical inhibition of Atg1 kinase or engineered degradation of Atg14 and observed homologous chromosome segregation followed by sister chromatid separation; cells

In vivo induction of CYP in mice by carbamazepine is independent on PXR.

Aiming Liu et al.

Pharmacological reports : PR, 67(2), 299-304 (2015-02-26)

The antiepileptic drug carbamazepine (CBZ) is a typical inducer of cytochrome P450 (CYP) 3A and 2C in the clinic. It is considered a strong constitutive androstane receptor activator, however both CBZ and its main metabolite CBZ 10, 11-epoxide have been

Small scale screening to determine the ability of different polymers to inhibit drug crystallization upon rapid solvent evaporation.

Bernard Van Eerdenbrugh et al.

Molecular pharmaceutics, 7(4), 1328-1337 (2010-06-12)

In this study, the ability of 7 chemically diverse polymers [Eudragit E100 (E100), poly(acrylic acid) (PAA), poly(vinylpyrrolidone) (PVP), poly(vinylpyrrolidone-vinyl acetate) (PVPVA), poly(styrene sulfonic acid) (PSSA), hydroxypropylmethylcellulose (HPMC) and hydroxypropylmethylcellulose acetate succinate (HPMCAS)] to inhibit the crystallization of 8 readily crystallizable

Evaluation of the microstructure of semicrystalline solid dispersions.

Qing Zhu et al.

Molecular pharmaceutics, 7(4), 1291-1300 (2010-06-17)

As a result of an increase in the number of emerging therapies with dissolution limited bioavailability, formulation strategies such as solid dispersions that enhance the rate of solubilization are of interest. In this study, the microstructure of solid dispersions prepared

Inhibition of protein kinase B activity induces cell cycle arrest and apoptosis during early G₁ phase in CHO cells.

Angélique van Opstal et al.

Cell biology international, 36(4), 357-365 (2012-01-19)

Inhibition of PKB (protein kinase B) activity using a highly selective PKB inhibitor resulted in inhibition of cell cycle progression only if cells were in early G1 phase at the time of addition of the inhibitor, as demonstrated by time-lapse

Differential regulation of CIDEA and CIDEC expression by insulin via Akt1/2- and JNK2-dependent pathways in human adipocytes.

Minoru Ito et al.

Journal of lipid research, 52(8), 1450-1460 (2011-06-04)

Both insulin and the cell death-inducing DNA fragmentation factor-α-like effector (CIDE) family play important roles in apoptosis and lipid droplet formation. Previously, we reported that CIDEA and CIDEC are differentially regulated by insulin and contribute separately to insulin-induced anti-apoptosis and

Quantitative 35Cl nuclear quadrupole resonance in tablets of the antidiabetic medicine Diabinese.

Elizabeth Tate et al.

Analytical chemistry, 81(13), 5574-5576 (2009-06-06)

Pulsed (35)Cl nuclear quadrupole resonance (NQR) experiments have been performed on 250-mg tablets of the antidiabetic medicine Diabinese to establish the conditions needed for noninvasive quantitative analysis of the medicine in standard bottles. One important condition is the generation of

Antidiabetic properties of ethanolic extract of Cnidoscolus aconitifolius on alloxan induced diabetes mellitus in rats.

A A Oyagbemi et al.

African journal of medicine and medical sciences, 39 Suppl, 171-178 (2010-12-01)

This research was designed to investigate the antidiabetic properties of ethanolic extract of Cnidoscolus aconitifolius in alloxan-induced diabetes mellitus in Wistar male albino rats. Thirty male albino rats were used. Diabetes mellitus was induced in five of the six groups

Investigation of the Factors Responsible for the Poor Oral Bioavailability of Acacetin in Rats: Physicochemical and Biopharmaceutical Aspects.

Dong-Gyun Han et al.

Pharmaceutics, 13(2) (2021-02-03)

Acacetin, an important ingredient of acacia honey and a component of several medicinal plants, exhibits therapeutic effects such as antioxidative, anticancer, anti-inflammatory, and anti-plasmodial activities. However, to date, studies reporting a systematic investigation of the in vivo fate of orally

A high-pressure polymorph of chlorpropamide formed on hydrostatic compression of the α-form in saturated ethanol solution.

Yury V Seryotkin et al.

Acta crystallographica. Section B, Structural science, 69(Pt 1), 77-85 (2013-02-01)

The crystal structure of the high-pressure polymorph (α') of an antidiabetic drug, chlorpropamide [4-chloro-N-(propylaminocarbonyl)benzenesulfonamide, C(10)H(13)ClN(2)O(3)S], which is formed at ~2.8 GPa from the α-polymorph (P2(1)2(1)2(1)) on hydrostatic compression in saturated ethanol solution, has been determined. As a result of the

A simple and sensitive liquid chromatography-tandem mass spectrometry method for trans-ε-viniferin quantification in mouse plasma and its application to a pharmacokinetic study in mice.

Jiseon Kim et al.

Journal of pharmaceutical and biomedical analysis, 134, 116-121 (2016-12-03)

In this study, a simple and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for the quantification of trans-ε-viniferin in small volumes (10μl) of mouse plasma using chlorpropamide as an internal standard was developed and validated. Plasma samples were precipitated with

Association of hyperinsulinemia with chlorpropamide toxicity.

D C Klonoff

The American journal of medicine, 84(1), 33-38 (1988-01-01)

Clinical and metabolic features of chlorpropamide toxicity are described in two patients with diabetes mellitus and accidental chlorpropamide overdosage. Elevated serum insulin levels were found during hypoglycemia in both patients. The world's literature was reviewed for other cases of chlorpropamide

A conformational polymorphic transition in the high-temperature epsilon-form of chlorpropamide on cooling: a new epsilon'-form.

Tatiana N Drebushchak et al.

Acta crystallographica. Section B, Structural science, 65(Pt 6), 770-781 (2009-11-20)

Structural changes in the high-temperature -polymorph of chlorpropamide, 4-chloro-N-(propylaminocarbonyl)benzenesulfonamide, C(10)H(13)ClN(2)O(3)S, on cooling down to 100 K and on reverse heating were followed by single-crystal X-ray diffraction. At temperatures below 200 K the phase transition into a new polymorph (termed the

β-catenin confers resistance to PI3K and AKT inhibitors and subverts FOXO3a to promote metastasis in colon cancer.

Stephan P Tenbaum et al.

Nature medicine, 18(6), 892-901 (2012-05-23)

The Wnt–β-catenin and PI3K-AKT-FOXO3a pathways have a central role in cancer. AKT phosporylates FOXO3a, relocating it from the cell nucleus to the cytoplasm, an effect that is reversed by PI3K and AKT inhibitors. Simultaneous hyperactivation of the Wnt–β-catenin pathway and

A hypothesis for the molecular mechanism of action of chlorpropamide in the treatment of diabetes mellitus and diabetes insipidus.

R M Zusman et al.

Federation proceedings, 36(13), 2728-2729 (1977-12-01)

Effects of artemisinin antimalarials on Cytochrome P450 enzymes in vitro using recombinant enzymes and human liver microsomes: potential implications for combination therapies.

Therese Ericsson et al.

Xenobiotica; the fate of foreign compounds in biological systems, 44(7), 615-626 (2014-01-10)

1. Cytochrome P450 enzyme system is the most important contributor to oxidative metabolism of drugs. Modification, and more specifically inhibition, of this system is an important determinant of several drug-drug interactions (DDIs). 2. Effects of the antimalarial agent artemisinin and

The mTORC2 complex regulates terminal differentiation of C2C12 myoblasts.

Lili Shu et al.

Molecular and cellular biology, 29(17), 4691-4700 (2009-07-01)

Rapamycin, a selective inhibitor of mTORC1 signaling, blocks terminal myoblast differentiation. We found that downregulation of rictor, a component of the mTORC2 complex, but not downregulation of raptor, a component of the mTORC1 complex, prevented terminal differentiation (fusion) of C2C12

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