81246-83-5Relevant articles and documents
Preparation method of 5′-O-(4,4'-dimethoxytriphenylmethyl)-N2-isobutyryl guanosine
-
, (2022/01/10)
The present invention discloses a method for preparing 5 '-O- (4,4'-dimethoxytriphenylmethyl)-N2-isobutyryl guanosine, after the preparation of N2-isobutyryloylguanosine with guanosine as the starting material, dmt-Cl was added to participate in the react
UNA AMIDITES AND USES THEREOF
-
Paragraph 0346; 0391; 0392, (2020/12/29)
Disclosed herein are compositions and pharmaceutical formulations that comprise a binding moiety conjugated to a modified polynucleic acid molecule and a polymer. Also described herein include methods for treating a disease which utilize a composition or
CYCLIC DINUCLEOTIDES AS STING AGONISTS
-
, (2018/08/20)
Disclosed are compounds, compositions and methods for treating of diseases, syndromes, or disorders that are affected by the modulation of STING. Such compounds are represented by Formula (I) as follows: wherein R, R1B, R1C, R2B
COMPOUNDS FOR TREATING BACTERIAL INFECTIONS
-
Page/Page column 30-31, (2011/04/25)
The present invention relates to a novel class of guanine nucleotide analogs which inhibit RelA and Relseq synthetic activity and which possess anti-bacterial activity. The present invention also relates to pharmaceutical compositions that include such compounds, and to methods of use of such compounds or compositions for combating bacteria and treating bacterial infections.
ppGpp analogues inhibit synthetase activity of Rel proteins from Gram-negative and Gram-positive bacteria
Wexselblatt, Ezequiel,Katzhendler, Jehoshua,Saleem-Batcha, Raspudin,Hansen, Guido,Hilgenfeld, Rolf,Glaser, Gad,Vidavski, Roee R.
experimental part, p. 4485 - 4497 (2010/08/22)
A prominent feature of the stringent response is the accumulation of two unusual phosphorylated derivatives of GTP and GDP (pppGpp: 5′-triphosphate-3′-diphosphate, and ppGpp: 5′-3′-bis-diphosphate), collectively called (p)ppGpp, within a few seconds after the onset of amino-acid starvation. The synthesis of these 'alarmone' compounds is catalyzed by RelA homologues. Other features of the stringent response include inhibition of stable RNA synthesis and modulation of transcription, replication, and translation. (p)ppGpp accumulation is important for virulence induction, differentiation and antibiotic resistance. We have synthesized a group of (p)ppGpp analogues and tested them as competitive inhibitors of Rel proteins in vitro. 2′-Deoxyguanosine-3′-5′-di(methylene bisphosphonate) [compound (10)] was found as an inhibitor that reduces ppGpp formation in both Gram-negative and Gram-positive bacteria. In silico docking together with competitive inhibition analysis suggests that compound (10) inhibits activity of Rel proteins by competing with GTP/GDP for its binding site. As Rel proteins are completely absent in mammalians, this appears to be a very attractive approach for the development of novel antibacterial agents.
UNA (unlocked nucleic acid): A flexible RNA mimic that allows engineering of nucleic acid duplex stability
Langkjaer, Niels,Pasternak, Anna,Wengel, Jesper
experimental part, p. 5420 - 5425 (2009/12/06)
UNA (unlocked nucleic acid) monomers are acyclic derivatives of RNA lacking the C2′-C3′-bond of the ribose ring of RNA. Synthesis of phosphoramidite UNA building blocks of the nucleobases adenine, cytosine, guanine, and uracil is described herein together
Synthesis of guanosine 5′-conjugates and their use as initiator molecules for transcription priming
Wolf, Joern,Dombos, Valeska,Appel, Bettina,Mueller, Sabine
supporting information; experimental part, p. 899 - 907 (2008/10/09)
We have synthesised two guanosine derivatives that are linked to biotinylated adenosine moieties by using two different strategies, one that includes synthetic steps on the solid phase and another one that is performed entirely in solution. The synthesised derivatives were shown to function as initiator molecules in transcription priming experiments. The incorporation efficiency was determined to be approximately 2%. Even though this value is rather low, the use of either molecule in selection experiments seems reasonable. Basically, RNA libraries with sequence complexities of 10 15 to 1016 can be generated. Labelling of such a library with our initiator molecule would still produce 1013 to 10 14 labelled/functionalised sequences, and thus sufficient sequence space for selection. The Royal Society of Chemistry.
Synthesis and biological evaluation of novel selenonucleosides
Chen, Yao,Peng, Yingdan,Zhang, Jiancun,Fu, Lei
, p. 1001 - 1008 (2008/12/22)
A series of novel selenonucleoside analogues with 1,4-oxaselenane as the carbohydrate fragment has been synthesized from their corresponding dimesylated seconucleosides treated with NaHSe solution and subsequent deprotection. The synthesized selenonucleos
Synthesis, characterization, and biological properties of small branched RNA fragments containing chiral (Rp and Sp) 2′,5′-phosphorothioate linkages
Mourani, Rawan,Damha, Masad J.
, p. 203 - 229 (2007/10/03)
Synthetic branched RNA fragments were prepared to examine the stereochemical requirements for hydrolysis of RNA lariats by the yeast debranching enzyme (yDBR). Specifically, two branched trinucleoside diphosphates and a tetranucleoside triphosphate contai
