97695-14-2Relevant articles and documents
Synthesis of native-like crosslinked duplex RNA and study of its properties
Onizuka, Kazumitsu,Hazemi, Madoka E.,Thomas, Justin M.,Monteleone, Leanna R.,Yamada, Ken,Imoto, Shuhei,Beal, Peter A.,Nagatsugi, Fumi
, p. 2191 - 2199 (2017)
A variety of enzymes have been found to interact with double-stranded RNA (dsRNA) in order to carry out its functions. We have endeavored to prepare the covalently crosslinked native-like duplex RNA, which could be useful for biochemical studies and RNA nanotechnology. In this study, the interstrand covalently linked duplex RNA was formed by a crosslinking reaction between vinylpurine (VP) and the target cytosine or uracil in RNA. We measured melting temperatures and CD spectra to identify the properties of the VP crosslinked duplex RNA. The crosslinking formation increased the thermodynamic stability without disturbing the natural conformation of dsRNA. In addition, a competitive binding experiment with the duplex RNA binding enzyme, ADAR2, showed the crosslinked dsRNA bound the protein with nearly the same binding affinity as the natural dsRNA, confirming that it has finely preserved the natural traits of duplex RNA.
PHARMACEUTICAL COMPOSITION COMPRISING NOVEL AZOLOPYRIMIDINE HETEROCYCLIC COMPOUND AS ACTIVE INGREDIENT
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Paragraph 0146-0148, (2022/01/24)
The present invention relates to a pharmaceutical composition for the prophylaxis or treatment of cancer comprising a novel azolopyrimidine heterocyclic compound as an active ingredient, and the pharmaceutical composition for the prophylaxis or treatment of cancer of the present invention can be used as a small molecular immunotherapy anticancer agent which modulates an adenosine pathway by comprising the azolopyrimidine heterocyclic compound.
INHIBITORS OF E1 ACTIVATING ENZYMES
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Page/Page column 118-119, (2008/06/13)
This invention relates to compounds that inhibit El activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
Synthesis of 4-Thiouridine, 6-Thioinosine, and 6-Thioguanosine 3′,5′-O-Bisphosphates as Donor Molecules for RNA Ligation and Their Application to the Synthesis of Photoactivatable TMG-Capped U1 snRNA Fragments
Kadokura, Michinori,Wada, Takeshi,Seio, Kohji,Sekine, Mitsuo
, p. 5104 - 5113 (2007/10/03)
4-Thiouridine, 6-thioguanosine, and 6-thioinosine 3′,5′-bisphosphates (9, 20, and 28) were synthesized in good yields by considerably improved methods. In the former two compounds, uridine and 2-N-phenylacetylguanosine were converted via transient O-trimethylsilylation to the corresponding 4- and 6-O-benzenesulfonyl intermediates (2 and 13), which, in turn, were allowed to react with 2-cyanoethanethiol in the presence of N-methylpyrrolidine to give 4-thiouridine (3) and 2-N-phenylacetyl-6-thioguanosine derivatives (14), respectively. In situ dimethoxytritylation of these thionucleoside derivatives gave the 5′-masked products 4 and 15 in high overall yields from 1 and 11. 6-S-(2-Cyanoethyl)-5′-O-(4,4′-dimethoxytrityl)-6-thioinosine (23) was synthesized via substitution of the 5′-O-tritylated 6-chloropurine riboside derivative 22 with 2-cyanoethanethiol. These S-(2-cyanoethyl)thionucleosides were converted to the 2′-O-(tert-butyldimethylsilyl)ribonucleoside 3′-phosphoramidite derivatives 7, 18, and 26 or 3′,5′-bisphosphate derivatives 8, 19, and 27. Treatment of 8, 19, and 27 with DBU gave thionucleoside 3′,5′-bisphosphate derivatives 9, 20, and 28, which were found to be substrates of T4 RNA ligase. These thionucleoside 3′,5′-bisphosphates were examined as donors for ligation with m32,2,7 G5′ pppAmUmA, i.e., the 5′-terminal tetranucleotide fragment of U1 snRNA. The 4-thiouridine 3′,5′-bisphosphate derivative 9 was found to serve as the most active substrate of T4 RNA ligase with a reaction efficiency of 96%.
