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| | <StructureSection load='5nj7' size='340' side='right'caption='[[5nj7]], [[Resolution|resolution]] 2.15Å' scene=''> | | <StructureSection load='5nj7' size='340' side='right'caption='[[5nj7]], [[Resolution|resolution]] 2.15Å' scene=''> |
| | == Structural highlights == | | == Structural highlights == |
| - | <table><tr><td colspan='2'>[[5nj7]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5NJ7 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5NJ7 FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[5nj7]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Bos_taurus Bos taurus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5NJ7 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5NJ7 FirstGlance]. <br> |
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=A6R:arsenoplatin-1'>A6R</scene></td></tr> | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.15Å</td></tr> |
| - | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Pancreatic_ribonuclease Pancreatic ribonuclease], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.27.5 3.1.27.5] </span></td></tr> | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=A6R:arsenoplatin-1'>A6R</scene></td></tr> |
| - | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5nj7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5nj7 OCA], [http://pdbe.org/5nj7 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5nj7 RCSB], [http://www.ebi.ac.uk/pdbsum/5nj7 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5nj7 ProSAT]</span></td></tr> | + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5nj7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5nj7 OCA], [https://pdbe.org/5nj7 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5nj7 RCSB], [https://www.ebi.ac.uk/pdbsum/5nj7 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5nj7 ProSAT]</span></td></tr> |
| | </table> | | </table> |
| | == Function == | | == Function == |
| - | [[http://www.uniprot.org/uniprot/RNAS1_BOVIN RNAS1_BOVIN]] Endonuclease that catalyzes the cleavage of RNA on the 3' side of pyrimidine nucleotides. Acts on single stranded and double stranded RNA.<ref>PMID:7479688</ref> | + | [https://www.uniprot.org/uniprot/RNAS1_BOVIN RNAS1_BOVIN] Endonuclease that catalyzes the cleavage of RNA on the 3' side of pyrimidine nucleotides. Acts on single stranded and double stranded RNA.<ref>PMID:7479688</ref> |
| | <div style="background-color:#fffaf0;"> | | <div style="background-color:#fffaf0;"> |
| | == Publication Abstract from PubMed == | | == Publication Abstract from PubMed == |
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| | | | |
| | ==See Also== | | ==See Also== |
| - | *[[Ribonuclease|Ribonuclease]] | + | *[[Ribonuclease 3D structures|Ribonuclease 3D structures]] |
| | == References == | | == References == |
| | <references/> | | <references/> |
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| | [[Category: Bos taurus]] | | [[Category: Bos taurus]] |
| | [[Category: Large Structures]] | | [[Category: Large Structures]] |
| - | [[Category: Pancreatic ribonuclease]]
| + | [[Category: Ferraro G]] |
| - | [[Category: Ferraro, G]] | + | [[Category: Merlino A]] |
| - | [[Category: Merlino, A]] | + | |
| - | [[Category: Arsenoplatin]]
| + | |
| - | [[Category: Hydrolase]]
| + | |
| - | [[Category: Metal based drug]]
| + | |
| - | [[Category: Ribonuclease]]
| + | |
| Structural highlights
Function
RNAS1_BOVIN Endonuclease that catalyzes the cleavage of RNA on the 3' side of pyrimidine nucleotides. Acts on single stranded and double stranded RNA.[1]
Publication Abstract from PubMed
Arsenoplatins are adducts of two chemically important anticancer drugs, cisplatin and arsenic trioxide, that have a Pt(II) bond to an As(III) hydroxide center. Screens of the NCI-60 human tumor cell lines reveal that arsenoplatin-1 (AP-1), [Pt(mu-NHC(CH3)O)2ClAs(OH)2], the first representative of this novel class of anticancer agents, displays a superior activity profile relative to the parent drugs As2O3 or cisplatin in a majority of cancer cell lines tested. These activity profiles are important because the success of arsenic trioxide in blood cancers (such as APL) has not been seen in solid tumors due to the rapid clearance of arsenous acid from the body. To understand the biological chemistry of these compounds, we evaluated interactions of AP-1 with the two important classes of biomolecules-proteins and DNA. The first structural studies of AP-1 bound to model proteins reveal that platinum(II) binds the Nepsilon of His in a manner that preserves the Pt-As bond. We find that AP-1 readily enters cells and binds to DNA with an intact Pt-As bond (Pt:As ratio of 1). At longer incubation times, however, the Pt:As ratio in DNA samples increases, suggesting that the Pt-As bond breaks and releases the As(OH)2 moiety. We conclude that arsenoplatin-1 has the potential to deliver both Pt and As species to a variety of hematological and solid cancers.
Arsenoplatin-1 Is a Dual Pharmacophore Anticancer Agent.,Miodragovic D, Merlino A, Swindell EP, Bogachkov A, Ahn RW, Abuhadba S, Ferraro G, Marzo T, Mazar AP, Messori L, O'Halloran TV J Am Chem Soc. 2019 Apr 24;141(16):6453-6457. doi: 10.1021/jacs.8b13681. Epub, 2019 Apr 15. PMID:30943017[2]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ delCardayre SB, Ribo M, Yokel EM, Quirk DJ, Rutter WJ, Raines RT. Engineering ribonuclease A: production, purification and characterization of wild-type enzyme and mutants at Gln11. Protein Eng. 1995 Mar;8(3):261-73. PMID:7479688
- ↑ Miodragovic D, Merlino A, Swindell EP, Bogachkov A, Ahn RW, Abuhadba S, Ferraro G, Marzo T, Mazar AP, Messori L, O'Halloran TV. Arsenoplatin-1 Is a Dual Pharmacophore Anticancer Agent. J Am Chem Soc. 2019 Apr 24;141(16):6453-6457. doi: 10.1021/jacs.8b13681. Epub, 2019 Apr 15. PMID:30943017 doi:http://dx.doi.org/10.1021/jacs.8b13681
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