This effect is caused by the combination of PARP inhibitor-induced DNA double-strand break (DSB) formation and functional deficiency of homologous recombination (HR) repair, which is the main repair pathway for DNA damage. On the other hand, the clonal evolution in tumors as a tumor ...
[20].Oconnor L O, Rulten S L, Cranston A, et al. The PARP Inhibitor AZD2461 Provides Insights into the Role of PARP3 Inhibition for Both Synthetic Lethality and Tolerability with Chemotherapy in Preclinical Models.[J]. Cancer Research, 2016, 76(20): 6084-6094.DOI:10.1158/0008-5472.CAN...
[20].Oconnor L O, Rulten S L, Cranston A, et al. The PARP Inhibitor AZD2461 Provides Insights into the Role of PARP3 Inhibition for Both Synthetic Lethality and Tolerability with Chemotherapy in Preclinical Models.[J]. Cancer Research, 2016, 76(20): 6084-6094.DOI:10.1158/0008-5472.CAN...
TIMP~1 阻止胶原降解等ꎬ促进 ECM 合成和细胞 增殖ꎬ收缩肝窦ꎮ PARP~1 主要调控机制见图 1ꎮ 图 1 肝细胞 DNA 损伤使 PARP~1 过度激活促进 HF 的 机制 Fig.1 Mechanism by which hepatocyte DNA injury pro~ motes HF by overactivating PARP~1 2.1 调节肝细胞 NAD+ 和能量代谢ꎬ线粒体稳态...
[20].Oconnor L O, Rulten S L, Cranston A, et al. The PARP Inhibitor AZD2461 Provides Insights into the Role of PARP3 Inhibition for Both Synthetic Lethality and Tolerability with Chemotherapy in Preclinical Models.[J]. Cancer Research, 2016, 76(20): 6084-6094.DOI:10.1158/0008-5472.CAN...
Poly(ADP-ribose)polymerase (PARP) inhibition and anticancer activity of simmiparib, a new inhibitor undergoing clinical trials. Cancer Letters 2017; 386: 47-56 【14】Hopkins TA, Shi Y, Rodriguez LE, et al. Mechanistic Dissection of PARP1 Trapping and the Impact on In Vivo Tolerability and ...
Mechanism of Action Resource Library HCP Resources Patient Resources ProstateHRRm* orBRCAm* MetastaticCastration-Resistant Home Efficacy Combination Therapy inBRCAm* mCRPC Monotherapy in HRRm* mCRPC HRR/BRCATesting Dosing & Management Safety & Tolerability ...
This review mainly introduces the concept of synthetic lethality and homologous recombination, describes the mechanism of action of PARP inhibitors within this concept, discusses problems such as resistance, enumerates the current progress and achievements of clinical trials for PARP inhibitors in pancreatic...
Mechanism PARP inhibitors (PARPi) are oral-targeted therapies, which competitively bind to the NAD + sites of PARP1 and PARP2 inducing a catalytic inhibition (Fig.2a, b). Five different molecules are currently under development or recently approved: olaparib, rucaparib, niraparib, veliparib...
H. Nonhomologous end joining drives poly(ADP-ribose) polymerase (PARP) inhibitor lethality in homologous recombination-deficient cells. Proc. Natl Acad. Sci. USA 108, 3406–3411 (2011). CAS PubMed PubMed Central Google Scholar Zahradka, P. & Ebisuzaki, K. A shuttle mechanism for DNA-...