The PARP‐1 inhibitor olaparib causes retention of γ‐H2AX foci in brca1 heterozygote cells following exposure to gamma radiation . J Cancer Ther 2013;4:44–52.Bourton EC, Plowman PN, Harvey AJ, et al. The PARP-1 inhibitor Olaparib causes retention of γ-H2AX foci in BRCA1 heterozygote ...
2.分子对接与虚拟筛选 为了发现具有药物开发潜力的新PARP1抑制剂，通过使用DOCK6（UCSF）将天然化合物对接到PARP1的结合位点进行虚拟筛选，已知抑制剂奥拉帕尼（Olaparib）作为参考药物用于选择命中化合物。DOCK程序首先将所有天然化合物对接到PARP1进行打分，得分与奥拉帕尼比较，然后选择具有较高得分的化合物进行第二轮对接...
Olaparib, PARP1 inhibitor in ovarian cancer. Expert Opin Invest Drugs. 2012;21(10):1575–84.Claudia Marchetti, Ludovica Imperiale, Maria Luisa Gasparri, Innocenza Palaia, Sandro Pignata, Terenzio Boni, Filippo Bellati, Pierluigi Benedetti Panici. (2012) Olaparib, PARP1 inhibitor in ovarian ...
参考文献:Chen Z, Wang K, Zhao L and Gong L (2023) BRCA2 mutation in advanced lung squamous cell carcinoma treated with Olaparib and a PD-1 inhibitor: a case report. Front. Oncol. 13:1190100. doi: 10.3389/fonc.2023.1190100
Olaparib (KU0059436) 是 PARP1/PARP2 的小分子抑制剂 (IC50=5/1 nM),对 PARP tankyrase-1 的抑制活性较弱 (IC50=1.5 μM),具有选择性和口服活性。Olaparib 具有自噬和线粒体自噬激活活性。 规格价格库存数量 5 mg¥ 265现货 10 mg¥ 396现货 ...
Olaparib (AZD2281,KU0059436, AZD-2281, KU-0059436),又称奥拉帕尼或奥拉帕利,是一种可口服的PARP1/2抑制剂,IC50分别为5和1 nM,破坏PARP介导DNA修复机制,诱导细胞凋亡,表现出抗肿瘤活性。 产品性质 英文别名(English Synonym) Olaparib,AZD2281,KU0059436, AZD-2281, KU-0059436 ...
PETRA: first-in-human phase 1/2a trial of the first-in-class new generation poly(ADP-ribose) polymerase-1 selective inhibitor (PARP1i) saruparib (AZD5305) in patients with advanced solid tumors with BRCA1/2, PALB2 or RAD51C/D mutations. Abstract presented at: American Association for ...
The poly (ADP-ribose) polymerase-1 (PARP-1) enzyme is an important target in the treatment of breast cancer. Currently, treatment options include the drugs Olaparib, Niraparib, Rucaparib, and Talazoparib; however, these drugs can cause severe side effects including hematological toxicity and ...
Olaparib (KU0059436) 是 PARP1/PARP2 的小分子抑制剂 (IC50=5/1 nM),对 PARP tankyrase-1 的抑制活性较弱 (IC50=1.5 μM),具有选择性和口服活性。Olaparib 具有自噬和线粒体自噬激活活性。 AutophagyMitophagyPARP ¥ 265 现货 规格 数量 客户已引用 ...
一代PARP1抑制剂能靶向PARP1/PAPR2,为非选择性抑制剂,目前已有多款药物先后上市,如Olaparib(Merck/AZ),Niraparib(GSK/Zai lab),Rucaparib(Clovis),Talazoparib(Pfizer/Medivation),氟唑帕利(恒瑞),帕米帕利(百济)等。这类药物在卵巢癌,乳腺癌、前列腺癌等适应症上获得成功,证明了PARP1/PAPR2是极具价值的合成...