Olaparib
From Proteopedia
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| - | <StructureSection load='' size='340' side='right' caption=' | + | <StructureSection load='' size='340' side='right' caption='Olaparib' scene='10/1001156/Cv/1'> |
Olaparib, sold under the brand name Lynparza, is a medication for the maintenance treatment of BRCA-mutated advanced ovarian cancer in adults (see [[BRCA]]). It is a PARP inhibitor, inhibiting [[Poly (ADP-ribose) polymerase|poly ADP ribose polymerase]] (PARP), an enzyme involved in DNA repair. It acts against cancers in people with hereditary BRCA1 or BRCA2 mutations, which include some ovarian, breast, and prostate cancers.<ref name="a7">PMID:19553641</ref> See also [https://en.wikipedia.org/wiki/Olaparib Olaparib]. | Olaparib, sold under the brand name Lynparza, is a medication for the maintenance treatment of BRCA-mutated advanced ovarian cancer in adults (see [[BRCA]]). It is a PARP inhibitor, inhibiting [[Poly (ADP-ribose) polymerase|poly ADP ribose polymerase]] (PARP), an enzyme involved in DNA repair. It acts against cancers in people with hereditary BRCA1 or BRCA2 mutations, which include some ovarian, breast, and prostate cancers.<ref name="a7">PMID:19553641</ref> See also [https://en.wikipedia.org/wiki/Olaparib Olaparib]. | ||
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<scene name='10/1001156/Overall/1'>Poly [ADP-ribose] polymerase 2 in complex with Olaparib</scene> ([[4tvj]]). | <scene name='10/1001156/Overall/1'>Poly [ADP-ribose] polymerase 2 in complex with Olaparib</scene> ([[4tvj]]). | ||
| - | <scene name='10/1001156/Binding_site/2'>Olaparib binding site</scene>. | + | <scene name='10/1001156/Binding_site/2'>Olaparib binding site</scene>. Water molecules are shown as red spheres. |
See also: | See also: | ||
Current revision
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References
- ↑ Fong PC, Boss DS, Yap TA, Tutt A, Wu P, Mergui-Roelvink M, Mortimer P, Swaisland H, Lau A, O'Connor MJ, Ashworth A, Carmichael J, Kaye SB, Schellens JH, de Bono JS. Inhibition of poly(ADP-ribose) polymerase in tumors from BRCA mutation carriers. N Engl J Med. 2009 Jul 9;361(2):123-34. PMID:19553641 doi:10.1056/NEJMoa0900212
- ↑ Menear KA, Adcock C, Boulter R, Cockcroft XL, Copsey L, Cranston A, Dillon KJ, Drzewiecki J, Garman S, Gomez S, Javaid H, Kerrigan F, Knights C, Lau A, Loh VM Jr, Matthews IT, Moore S, O'Connor MJ, Smith GC, Martin NM. 4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1. J Med Chem. 2008 Oct 23;51(20):6581-91. PMID:18800822 doi:10.1021/jm8001263
