Targeting PI3K: Emerging Therapy for Chronic Lymphocytic Leukemia and Beyond
Wei, Manman2; Wang, Xiang1; Song, Zilan2; Jiao, Mingkun2; Ding, Jian1; Meng, Ling-Hua1; Zhang, Ao2
刊名MEDICINAL RESEARCH REVIEWS
2015-07
卷号35期号:4页码:720-752
关键词chronic lymphocytic leukemia PI3K inhibitor molecularly targeted therapy idelalisib
ISSN号0198-6325
DOI10.1002/med.21341
文献子类Review
英文摘要Chronic lymphocytic leukemia (CLL) remains the most incurable leukemia. Early chemotherapeutic treatments, including alkylating agents, purine nucleoside derivatives, and immunotherapeutic antibodies, only show limited benefits for patients but severe off-target related side effects. Recent advances in understanding of the critical molecular pathways of regulating proliferation and survival of B-CLL cells have spurred a new therapeutical strategy by selectively targeting phosphoinositide 3-kinase delta (PI3K). Idelalisib, a first-in-class PI3K-selective small molecule has received the FDA's fast-track approval in July of 2014 as a new treatment of CLL, indolent B-cell non-Hodgkin's lymphoma, and relapsed small lymphocytic lymphoma. Undoubtedly, the success of idelalisib has provided a solid support in the development of PI3K-specific inhibitors and reformed the concept of treating CLL. However, the number of reported selective inhibitors of PI3K is very limited and very few have advanced into clinical trials. The mechanism of their actions remains elusive. More profound understanding on the modes of action of new PI3K inhibitors will further validate the PI3K-targeting strategy, and help to identify biomarkers capable of stratifying patients who will most likely benefit from the therapy. (C) 2014 Wiley Periodicals, Inc.
资助项目Chinese NSF[81125021] ; Chinese NSF[81373277] ; Chinese NSF[81430080] ; Chinese NSF[81321092] ; Major State Basic Research Development Program[2015CB910603]
WOS关键词B-CELL RECEPTOR ; PHOSPHATIDYLINOSITOL 3-KINASE INHIBITOR ; VIVO ANTITUMOR-ACTIVITY ; PHOSPHOINOSITIDE 3-KINASE ; SELECTIVE INHIBITOR ; KINASE INHIBITOR ; PI3-KINASE DELTA ; SURVIVAL SIGNALS ; CLINICAL-TRIALS ; IN-VITRO
WOS研究方向Pharmacology & Pharmacy
语种英语
出版者WILEY-BLACKWELL
WOS记录号WOS:000356068800004
内容类型期刊论文
源URL[http://119.78.100.183/handle/2S10ELR8/276486]  
专题药理学第一研究室
中科院受体结构与功能重点实验室
新药研究国家重点实验室
药物化学研究室
通讯作者Zhang, Ao
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, Synthet Organ & Med Chem Lab, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China;
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GB/T 7714
Wei, Manman,Wang, Xiang,Song, Zilan,et al. Targeting PI3K: Emerging Therapy for Chronic Lymphocytic Leukemia and Beyond[J]. MEDICINAL RESEARCH REVIEWS,2015,35(4):720-752.
APA Wei, Manman.,Wang, Xiang.,Song, Zilan.,Jiao, Mingkun.,Ding, Jian.,...&Zhang, Ao.(2015).Targeting PI3K: Emerging Therapy for Chronic Lymphocytic Leukemia and Beyond.MEDICINAL RESEARCH REVIEWS,35(4),720-752.
MLA Wei, Manman,et al."Targeting PI3K: Emerging Therapy for Chronic Lymphocytic Leukemia and Beyond".MEDICINAL RESEARCH REVIEWS 35.4(2015):720-752.
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