26825-95-6Relevant academic research and scientific papers
COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS
-
Paragraph 00165-00166, (2018/10/19)
The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.
COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF AGENTS
-
Paragraph 00687, (2019/01/08)
The disclosure features amino lipids and compositions involving the same. Nanoparticle compositions include an amino lipid as well as additional lipids such as phospholipids, structural lipids, PEG lipids, or a combination thereof. Nanoparticle compositions further including therapeutic and/or prophylactic agents such as RNA are useful in the delivery of therapeutic and/or prophylactic agents to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.
COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS
-
Paragraph 00539-00540, (2017/04/11)
The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.
COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF AGENTS
-
Paragraph 00618, (2017/07/14)
The disclosure features amino lipids and compositions involving the same. Nanoparticle compositions include an amino lipid as well as additional lipids such as phospholipids, structural lipids, PEG lipids, or a combination thereof. Nanoparticle compositions further including therapeutic and/or prophylactic agents such as RNA are useful in the delivery of therapeutic and/or prophylactic agents to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.
Evaluation of coumarin-based fluorogenic P450 BM3 substrates and prospects for competitive inhibition screenings
Neufeld, Katharina,Zu Berstenhorst, Sonja Meyer,Pietruszka, J?rg
, p. 70 - 81 (2014/06/09)
Fluorescence-based assays for the cytochrome P450 BM3 monooxygenase from Bacillus megaterium address an attractive biotechnological challenge by facilitating enzyme engineering and the identification of potential substrates of this highly promising biocatalyst. In the current study, we used the scarcity of corresponding screening systems as an opportunity to evaluate a novel and continuous high-throughput assay for this unique enzyme. A set of nine catalytically diverse P450 BM3 variants was constructed and tested toward the native substrate-inspired fluorogenic substrate 12-(4-trifluoromethylcoumarin-7- yloxy)dodecanoic acid. Particularly high enzyme-mediated O-dealkylation yielding the fluorescent product 7-hydroxy-4-trifluoromethylcoumarin was observed with mutants containing the F87V substitution, with A74G/F87V showing the highest catalytic efficiency (0.458 min-1 μM-1). To simplify the assay procedure and show its versatility, different modes of application were successfully demonstrated, including (i) the direct use of NADPH or its oxidized form NADP+ along with diverse NADPH recycling systems for electron supply, (ii) the use of cell-free lysates and whole-cell preparations as the biocatalyst source, and (iii) its use for competitive inhibition screens to identify or characterize substrates and inhibitors. A detailed comparison with known, fluorescence-based P450 BM3 assays finally emphasizes the relevance of our contribution to the ongoing research.
INHIBITORS OF BIOFILM FORMATION OF GRAM-POSITIVE AND GRAM-NEGATIVE BACTERIA
-
Page/Page column 71-72, (2009/07/18)
The present invention relates to the use of compounds as broad spectrum inhibitors of bacterial biofilm formation. In particular the invention refers to a family of compounds that block the quorum sensing system of Gram-negative and Gram-positive bacteria, a process for their manufacture, pharmaceutical compositions containing them and to their use for the treatment and prevention of bacterial damages and diseases, in particular for diseases where there is an advantage in inhibiting quorum sensing regulated phenotypes of pathogens.
The effect of twin-tailed sidearms on sodium cation transport in synthetic hydraphile cation channels
Shabany, Hossein,Pajewski, Robert,Abel, Ernesto,Mukhopadhyay, Anindita,Gokel, George W.
, p. 1393 - 1400 (2007/10/03)
The preparation of novel tris(macrocycle)s that transport Na+ through phospholipid bilayers is reported. All of the reported structures have the following structural elements: sidechain-macrocycle-spacer-macro-cycle-spacer-macrocycle-sidechain.
NEPHROTROPIC DRUGS
-
, (2008/06/13)
Disclosed are a drug having renal selectivity and a drug carrier for specifically transporting a drug supported thereon to a kidney. A segment structure specifically recognizable in the kidney is utilized. More specifically, since a segment structure repr
Renal drug targeting using a vector 'alkylglycoside'
Suzuki, Kokichi,Susaki, Hiroshi,Okuno, Satoshi,Sugiyama, Yuichi
, p. 57 - 64 (2007/10/03)
A specific sugar-modified peptide has previously been shown to have renal targeting potential in vivo and to have a specific binding site which has been identified in the kidney membrane fraction. In this report, we studied the inhibitory effects of glycosylated derivatives on the binding of [3H]Glc-O-C8-AVP [a glucosylated derivative of Arg8-vasopressin (AVP), K(d) = 55 nM] to clarify the structural requirements necessary for renal recognition. Glc-S-C7-Me (octyl β-D-thioglucoside) markedly inhibited the binding, to a much greater extent than Glc-O-C7-Me (octyl β-D-glucoside) and Gal-S-C7-Me (octyl β-D-thiogalactoside). Also, [3H]Glc-S-C7-Me was shown to have a specific binding site on the kidney membrane (K(d) = 17 nM, B(max) = 24 pmol/mg protein) rather than the liver membrane and, in addition, Glc-S- C7-Me exhibited effective and selective renal uptake in vivo. To examine the possibility that Glc-S-C7-Me might be of practical use as a renal targeting vector, AVP, tryptamine and 4-nitrobenz-2-oxa-1,3-diazole were modified with Glc-S-C8- and the tissue uptake of the resulting derivatives was evaluated. All of these derivatives showed clear renal targeting potential because the apparent uptake clearance by the kidney was greater than 3 ml/min/g kidney in each case. As far as the AVP derivatives were concerned, derivatives having different numbers of methylene groups were compared with Glc-S-C8-AVP. Glc- S-C11-AVP exhibited increased kidney targeting potential, whereas that of Glc-S-C5-AVP was reduced. These differences suggest that the 'alkylglycoside' moiety is important for renal uptake. In addition, these renally targeted derivatives inhibited the binding of [3H]Glc-S-C7-Me to the kidney membrane fraction. Our findings allow us to conclude that the alkylglycoside is a suitable candidate vector for renal targeting.
Structure-antitumor activity relationship of semi-synthetic spicamycin derivatives
Sakai,Kawai,Kamishohara,Odagawa,Suzuki,Uchida,Kawasaki,Tsuruo,Otake
, p. 1467 - 1480 (2007/10/03)
New derivatives of spicamycin modified at the fatty acid moieties of the molecule were synthesized and their structure-activity relationships were examined. The antitumor activity was greatly influenced by modification of the fatty acid moieties to tetradecadienoyl or dodecadienoyl analogues exhibiting better antitumor activity against COL-1 human colon cancer xenograft than SPM VIII.
