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Mizuno, Naomi; Kato, Yukio; Iwamoto, M.; Urae, Akinori; Amamoto, Toshiaki; Niwa, Toshiyuki; Sugiyama, Yuichi

doi:10.1023/a:1010991313633

Cited by 30 publications

(31 citation statements)

References 25 publications

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“…4,5) However, during evolution, animals have developed these proteins not to transport xenobiotic molecules but to uptake nutrients or excrete possibly toxic compounds ingested in food. Diversely regulated expression of many transporters in the intestine should be important to respond to every compound in natural foods.…”

Section: Discussionmentioning

confidence: 99%

“…The polar distribution of several transporters on the cell surface has been characterized 2,3) and their roles as drug transporters have also been extensively studied. 4,5) However, our knowledge about the regulation of the intestinal transport processes is limited compared with that of the transporters in other tissues. We were the first to report that the transcriptional regulation of intestinal fatty acid transport systems is coordinately regulated with intracellular fatty acid metabolism by a nutrient nuclear receptor, peroxisome proliferator-activated receptor (PPAR)a.…”

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confidence: 99%

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PPAR.ALPHA. Agonists Positively and Negatively Regulate the Expression of Several Nutrient/Drug Transporters in Mouse Small Intestine

Hirai

Fukui

Motojima

2007

Biological & Pharmaceutical Bulletin

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A systematic analysis to examine the effects of peroxisome proliferator-activated receptor (PPAR)a a agonists on the expression levels of all the nutrient/drug plasma-membrane transporters in the mouse small intestine was performed. Transporter mRNAs that were induced or repressed by two independent PPARa a-specific agonists were identified by a genome-wide microarray method, and the changes were confirmed by real-time PCR using RNA isolated from the intestines and livers of wild-type and PPARa a-null mice. Expression levels of seven nutrient/drug transporters (Abcd3, Octn2/Slc22a5, FATP2/Slc27a2, Slc22a21, Mct13/Slc16a13, Slc23a1 and Bcrp/ Abcg2) in the intestine were up-regulated and the expression level of one (Mrp1/Abcc1) was down-regulated by PPARa a; although the previously report that the H ؉ /peptide co-transporter 1 (Pept1) is up-regulated by PPARa a was not replicated in our study. We propose that the transport processes can be coordinately regulated with intracellular metabolism by nutrient nuclear receptors.

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Section: Discussionmentioning

confidence: 99%

mentioning

confidence: 99%

PPAR.ALPHA. Agonists Positively and Negatively Regulate the Expression of Several Nutrient/Drug Transporters in Mouse Small Intestine

Hirai

Fukui

Motojima

2007

Biological & Pharmaceutical Bulletin

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“…These include the use of influx transporters, blocking of efflux transporters, or receptor-mediated endocytosis (2). Alternative approaches aim to enhance paracellular permeation of drugs by loosening the TJ (3,4).…”

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confidence: 99%

Molecular Determinants of the Interaction between Clostridium perfringens Enterotoxin Fragments and Claudin-3

Winkler¹,

Gehring

Wenzel

et al. 2009

Journal of Biological Chemistry

106

144

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“…Drug transporters molecules are expressed in many tissues such as the intestine, liver, kidney, and brain, and play key roles in drug absorption, distribution, and excretion. The information on the functional characteristics of drug transporters provides important information to allow improvements in drug delivery or drug design by targeting specific transporter proteins [70].…”

Section: Design Drugs Targeting Protein-protein Interactionmentioning

confidence: 99%

Protein Based Drug Discovery

Joshi¹,

Boraste²,

Khairnar³

et al. 2009

Int J of Drug Disc

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Abstract-New drug target discovery is currently very popular with a great potential for advancing biomedical research and chemical genomics. Drug discovery is the process of discovering and designing drugs that includes target identification, target validation, lead identification, lead optimization and introduction of the new drugs to the public. G protein-coupled receptors are one of the most important drug targets. In the current scenario of drug research, approximately 60% of drug target molecules are located at the cell surface, and half of them are GPCRs. Fragment-based drug discovery is established as an alternative approach to high-throughput screening for generating novel small molecule drug candidates. Nanotechnology-based drug delivery systems have seen recent popularity due to their favorable physical, chemical, and biological properties, and great efforts have been made to target nanoDDSs to specific cellular receptors. Protein-protein interactions regulate a wide variety of important cellular pathways, and therefore represent a highly populated class of targets for drug discovery. An analysis of individual proteinprotein interaction systems has recently yielded success in the discovery of drug-like inhibitors.

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Abstract: The saturation of both the plasma protein binding and elimination accounts for the nonlinear pharmacokinetic profile. The binding to IGFBPs markedly limits both the distribution and elimination of IGF-1.

Cited by 30 publications

References 25 publications

PPAR.ALPHA. Agonists Positively and Negatively Regulate the Expression of Several Nutrient/Drug Transporters in Mouse Small Intestine

PPAR.ALPHA. Agonists Positively and Negatively Regulate the Expression of Several Nutrient/Drug Transporters in Mouse Small Intestine

Molecular Determinants of the Interaction between Clostridium perfringens Enterotoxin Fragments and Claudin-3

Protein Based Drug Discovery

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