Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:Q86TM3 (cage)
 29,987 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The purpose of this study was to develop an instrument (the Purdue instrument) and the corresponding methodologies to measure the electrostatic charge development (chargeability) of dry powders when they are in dynamic contact with stainless steel surfaces. The system used an inductive noncontact sensor located inside an aluminum Faraday cage and was optimized to measure the charging capabilities of a fixed volume of powder (0.5 cc). The chargeability of 5,5-diphenyl-hydantoin, calcium sulfate dihydrate, cimetidine, 3 grades of colloidal silicon dioxide, magnesium stearate, 4 grades of microcrystalline cellulose, salicylic acid, sodium carbonate, sodium salicylate, spray-dried lactose, and sulfinpyrazone were tested at 4 linear velocities, and the particle size distribution effect was assessed for 3 different grades of colloidal silicon dioxide and 4 different grades of microcrystalline cellulose. The chargeability values exhibited a linear relationship for the range of velocities studied, with colloidal silicon dioxide exhibiting the maximum negative chargeability and with spray-dried lactose being the only compound to exhibit positive chargeability. The instrument sensitivity was improved by a factor of 2 over the first generation version, and the electrostatic charge measurements were reproducible with relative standard deviations ranging from nondetectable to 33.7% (minimum of 3 replicates). These results demonstrate the feasibility of using the Purdue instrument to measure the electrostatic charge control capabilities of pharmaceutical dry powders with a reasonable level of precision.
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PMID:Chargeability measurements of selected pharmaceutical dry powders to assess their electrostatic charge control capabilities. 1728 49

p19(ARF) is a tumor suppressor that is frequently deleted in human cancer. It lies at chromosome 9p21 and shares exons 2 and 3 with p16(ink4a), which is also inactivated by these cancer-associated deletions. The "canonical pathway" by which p19(ARF) is thought to suppress tumorigenesis through activation of the p53 tumor suppressor. In response to hyperproliferative signals, such as expression of oncogenes, p19(ARF) is induced and binds to the MDM2 ubiquitin ligase, sequestering it in the nucleolus to allow the accumulation of p53. However, p19(ARF) also has MDM2 and p53 independent functions. In human colon cancer, p19(ARF) is only rarely deleted, but it is more frequently silenced by DNA promoter methylation. Here we show that inactivation of p19(ARF) in mice increases the number of cycling cells in the crypts of the colonic epithelium. Moreover, inactivation of p19(ARF) exacerbated the ulceration of the colonic epithelium caused by dextran sodium sulfate (DSS). These effects were similar to those observed in mice lacking myeloid translocation gene-related-1 (Mtgr1), and mice lacking both of these genes showed an even greater sensitivity to DSS. Surprisingly, inactivation of p19(ARF) restored the loss of the secretory lineage in mice deficient in Mtgr1, suggesting an additional role for p19(ARF) in the small intestinal epithelium.
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PMID:Inactivation of the p19(ARF) tumor suppressor affects intestinal epithelial cell proliferation and integrity. 1844 38

Increase in bladder mucosal permeability can be reproduced by intravesical administration of protamine sulfate (PS); however, the influence of PS once administered into the bladder disappears within several days. We developed a chronic animal model of urothelial injury using PS. Insertion of a polyethylene catheter through the bladder dome was performed in female Wistar rats. The other end of the catheter was connected to an osmotic pump for continuous delivery of PS or vehicle for 2 wk. Urinary frequency (UF) and voided volume (VV) were measured in the metabolic cage. The fifth group of rats received a high dose of PS (10 mg/ml) for 2 wk and were followed for a further 2 wk without PS. The sixth group received a high dose of PS for 2 wk and loxoprofen (0.1 mg.kg(-1).day(-1)) for 4 wk. UF was increased, and VV was reduced in rats treated with a high dose of PS but not changed in rats treated with a vehicle or a low dose of PS (1 mg/ml). UF was further increased in the fifth group, while unchanged in the sixth group. Histological sections in rats treated with a high dose of PS demonstrated a loss of the upper layer of urothelial cells and an increased number of mast cells. PGE2 level in the bladder was significantly elevated in the fifth group. These results indicate that chronic urotherial injury leads to an increase in UF and a decrease in VV. Increased PGE2 level in the bladder is likely to be associated with long-lasting storage dysfunction.
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PMID:Long-lasting breaches in the bladder epithelium lead to storage dysfunction with increase in bladder PGE2 levels in the rat. 1855 Aug 66

We report a simple approach for the fabrication of cuprous oxide (Cu 2O) nanocages and nanoframes possessing an unusual truncated rhombic dodecahedral structure. An aqueous solution containing CuCl 2, sodium dodecyl sulfate (SDS) surfactant, NH 2OH.HCl reductant, HCl, and NaOH was prepared, with the reagents introduced in the order listed. Rapid seed-particle aggregation and surface reconstruction of the intermediate structure resulted in the growth of type-I nanoframes, which have only {110} skeleton faces and empty {100} faces, 45 min after mixing the reagents. Continued crystal growth for additional 75 min produced nanocages with filled {100} faces. The nanocages have diameters of 350-400 nm, and their walls are thicker than those of the nanoframes. Selective acidic etching over the {110} faces of the nanocages by HCl via the addition of ethanol followed by sonication of the solution led to the formation of type-II nanoframes, which have elliptical pores on the {110} faces. The morphologies of these nanoframes were carefully examined by electron microscopy. Without addition of ethanol, random etching of the nanocages can occur at a slow rate. Octahedral gold nanocrystals and high-aspect-ratio gold nanorods were successfully encapsulated in the interiors of these Cu 2O nanocages by adding the gold nanostructures into the reaction solution. The formation process for such core-cage composite structures was studied. These composite materials should display interesting properties and functions.
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PMID:Fabrication of truncated rhombic dodecahedral Cu2O nanocages and nanoframes by particle aggregation and acidic etching. 1876 49

Little is known about the stretching effects on the biochemical and morphological features of tendons submitted to a long period of immobilization. Our purpose was to evaluate the response of rat tendons to stretching procedures after immobilization. The animals were separated into five experimental groups: GI--control of immobilized and euthanized animals; GII--immobilized and euthanized animals; GIII--control of immobilized animals and afterward stretched or allowed free cage activity; GIV--immobilized and stretched animals; and GV--immobilized and allowed free cage activity. Analysis in SDS-PAGE showed no remarkable differences among the groups, but a prominent collagen band was observed in GV, as compared to GIV and the control group, both in the compression and tension regions. Hydroxyproline content was highest in the compression region of GII. No differences among the groups were observed in the tension region. In regard to the concentration of noncollagenous proteins, differences were detected only in the tension region, where larger concentrations were found in the GII. When GII and GIV were compared, highest values were found in the GII. A more abundant presence of sulfated glycosaminoglycans, especially chondroitin sulfate, was detected in GIV, at the compression region of tendons. The presence of dermatan sulfate was outstanding in the compression and tension regions of the GII and GV groups. In the Ponceau SS stained sections, analyzed under polarization microscopy, GII exhibited the highest disorganization of the collagen bundles, partially recovered after stretching or with only remobilization. Our results indicate that a revision in the stretching procedures, in terms of duration and periodicity of the sessions, could benefit the efficiency of the stretching in cases of previous immobilization of tendons.
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PMID:Structural and biochemical analysis of the effect of immobilization followed by stretching on the calcaneal tendon of rats. 1908 45

The artificial polycarboxyacidic compounds (PC), imitating the principle of furan-derived and negatively charged structures alternating in the polymeric backbone of nucleic acids, previously explored as interferon inductors and stimulators of antiviral immunity in vivo, were modified by the side groups to amplify the direct antiviral potency in vitro and investigated in the cell culture model of human diploid fibroblasts infected with human cytomegalovirus (CMV) in a microbicidal scheme. Reconstruction from the PC to membrane potent compounds (MPC) was carried out by covalent modification with lipotropic pharmacophores (of cage-hydrocarbon structures similar to rimantadine or camphor-like terpenoids), as well as by conversion of the carboxy groups to sulfate-anionic derivates, related to the CMV sensitive heparansulfate receptor (HSR) of the cells. Both the factors of the MPC structure-functional modulation (lipotropic and anionic) were found to be effective tools for amplification of the microbicidal activity. The maximum inhibitory effect against CMV and minimum cytotoxicity (with the best selectivity, the chemotherapeutic index of > or = 3000-5000) were achieved mainly through increasing the anionic groups content, elevating the MPC negative charge to the level comparable with one of the like charged viral genome and HSR. In relation with the previously found anti-HIV efficacy of the same MPCs in analogous experimental models and in view of the fact that CMV is one of the most dangerous opportunistic co-factors of HIV/AIDS pathogenesis, the obtained data can be used as a basis for further development of new generation microbicides, promising for combined prevention of sexually transmitted infections.
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PMID:[Carboxy mimetic derivatives of nucleic acid polymeric backbones inhibiting human cytomegalovirus. 1. In vitro microbicidal effect]. 1927 50

The objectives of the study were to determine the pharmacokinetics of oxymorphone (oxy) and of ammonium sulfate-loaded, liposome-encapsulated oxymorphone (LE-ASG oxy) and to evaluate the behavioral effects of both opioid preparations by using ethographic evaluation specific to rhesus monkeys. Rhesus monkeys (n = 8) were injected with 2.0 mg/kg LE-ASG oxy s.c.. Blood samples were collected at serial time points up to 144 h in six monkeys and up to 456 h in two monkeys. Separate groups of monkeys were injected with 0.1 mg/kg oxy s.c. (n = 4) or i.v. (n = 5). Blood samples were collected at serial time points up to 24 h after injection. Pharmacokinetic parameters were calculated by using commercially available software. Behavior was recorded in a different group of 10 monkeys administered LE-ASG oxy (2.0 mg/kg s.c.) or oxy (0.1 mg/kg s.c.) on separate occasions. Behavioral evaluations were made at serial time points while monkeys were in an extended cage with a compatible stimulus animal. Oxymorphone was rapidly eliminated from the serum in the oxy group. Measurable drug was present in serum for up to 4 h after oxy was administered subcutaneously or intravenously. LE-ASG oxy was present in serum in measurable concentrations for more than 2 weeks. Neither oxy nor LE-ASG oxy produced observable sedation. LE-ASG oxy decreased some environmentally directed behaviors, but this drug formulation increased watchfulness, decreased self-directed and elimination behaviors, increased nonspecific social contact, and decreased threat behaviors. LE-ASG oxy persisted for an extended period in rhesus monkey serum and produced behavioral changes consistent with this opioid.
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PMID:Pharmacokinetics and behavioral effects of an extended-release, liposome-encapsulated preparation of oxymorphone in rhesus macaques. 1935 68

Custom built: A promising new approach towards more efficient self-assembled cage receptors through computer-aided design is demonstrated. The resulting M(4)L(6) tetrahedral cage, internally functionalized with accurately positioned urea hydrogen-bonding groups (see structure; yellow: predicted, blue: experimental, space-filling: SO(4)(2-)), proved to be a remarkably strong sulfate receptor in water.
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PMID:Computer-aided design of a sulfate-encapsulating receptor. 1937 9

The binding and selectivity of halides (spherical) and oxyanions (tetrahedral) toward a recently reported pentafluorophenyl-substituted tripodal urea-based receptor L(1) are examined thoroughly in the solid state by single-crystal X-ray crystallography as well as in solution by multinuclear NMR techniques. Crystallographic results show proof of a fluoride encapsulation in the cavity of L(1) in complex [L(1)(F)][Bu(4)N], . Fluoride encapsulation inside the C(3v) symmetric cleft is observed via six hydrogen bonds to all six urea protons of the receptor. In case of complex crystallographic results show encapsulation of sulfate ion inside a supramolecular cage formed upon 1 : 2 (guest-host) complex formation between sulfate and L(1). Sulfate encapsulation is observed via fourteen hydrogen bonding interactions from all six urea moieties of two L(1) units. Our effort to isolate single crystal of halides/oxyanions complexes of L(2) always yield single crystals of free L(2) though literature shows anion binding with this receptor in solution. Solution state binding studies of L(1) are carried out by (1)H-NMR titration to calculate binding constants, which show the following anion binding sequence H(2)PO(4)(-) > SO(4)(2-)> CH(3)COO(-) > F(-) > Cl(-) >> Br(-) whereas there is no binding with I(-), NO(3)(-) and ClO(4)(-) guests. Comparison of phosphate and sulfate binding in L(1) and L(2), show higher binding with the pentafluorophenyl substituted receptor, L(1). Further (19)F and (31)P-NMR experiments in solution are also carried out to probe the binding of F(-) and H(2)PO(4)(-) with L(1), respectively. Extensive (1)H-NMR experiments in solution and crystallization in the presence of multiple anions are also undertaken to evaluate the selectivity of H(2)PO(4)(-) over other anions.
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PMID:Anion complexation of a pentafluorophenyl-substituted tripodal urea receptor in solution and the solid state: selectivity toward phosphate. 1945 65

A hexaamine cage with pyridyl spacers was synthesized in good yield by a [2+3] Schiff-base condensation followed by sodium borohydride reduction. The protonation constants of the receptor as well as its association constants with Cl(-), NO(3)(-), AcO(-), ClO(4)(-), SO(4)(2-), H(2)PO(4)(-), and H(2)AsO(4)(-) were determined by potentiometry at 298.2 +/- 0.1 K in H(2)O/MeOH (50:50 v/v) and at ionic strength 0.10 +/- 0.01 M in KTsO. These studies revealed that although dihydrogen phosphate is less charged than sulfate, it is still appreciably bound by the receptor at low pH, suggesting that the pyridyl nitrogen is accepting hydrogen bonds from dihydrogen phosphate. It is also shown that dihydrogen phosphate is capable of effectively competing with sulfate for the receptor at higher pH, being selective for hydrogen phosphate at pH about 7.0. (31)P NMR experiments supported these findings. The fact that the receptor shows such a marked preference for hydrogen phosphate based mainly in its hydrogen bond accepting/donating ability in a highly competitive medium such as water/methanol mixed solvent is quite remarkable. Single-crystal X-ray diffraction determinations of anion associations between H(6)pyr(6+) receptor and nitrate, sulfate, and phosphate are consistent with the existence of [(H(6)pyr)(NO(3))(3)(H(2)O)(3)](3+), [(H(6)pyr)(SO(4))(2)(H(2)O)(4)](2+), and [(H(6)pyr)(HPO(4))(2)(H(2)PO(4))(H(2)O)(2)](+) cations. One nitrate anion is embedded into the H(6)pyr(6+) cage of the first supermolecule whereas in the second and third ones the anions are located in the periphery of the macrobicycle.
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PMID:Polyaza cryptand receptor selective for dihydrogen phosphate. 1986 Mar 88


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