Abstract：
:Lytic peptides have been demonstrated to exhibit obvious advantages in cancer therapy with binding ability toward tumor cells via electrostatic attractions, which are lack of active targeting and aggregation to tumor tissue. In the present study, five conjugated lytic peptides were redesigned and constructed to target gonadotropin releasing hormone receptors (GnRHr), meanwhile, the disulfide bridge was introduced to achieve redox sensitive delivery based on the experience from the preliminary work of lytic peptides P3 and P7. YX-1, was considered to be the most promising for in-depth study. YX-1 possessed high potency (IC50 = 3.16 ± 0.3 μM), low hemolytic effect, and cell membrane permeability in human A2780 ovarian cancer cells. Moreover, YX-1 had prominent pro-apoptotic activity by activating the mitochondria-cytochrome c-caspase apoptotic pathway. The study yielded the conjugate YX-1 with superior properties for antineoplastic activity, which makes it a promising potential candidate for targeting cancer therapy.
journal_name
Bioorg Chemjournal_title
Bioorganic chemistryauthors
Dai Y,Yue N,Liu C,Cai X,Su X,Bi X,Li Q,Li C,Huang W,Qian Hdoi
10.1016/j.bioorg.2019.102945subject
Has Abstractpub_date
2019-07-01 00:00:00pages
102945eissn
0045-2068issn
1090-2120pii
S0045-2068(18)31335-Xjournal_volume
88pub_type
杂志文章abstract：:The paper highlighted quinoxalines as potent ligands to corticotropin-releasing factor receptor types 1 and 2. The content includes design and structure-activity relationship of 50 model substances to CRFR1, CRFR2α and CRF2β, respectively. It is important to bear in mind, that our concept has based on challenging rese...
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更新日期：2019-05-01 00:00:00
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journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2016.12.002
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doi：10.1016/j.bioorg.2007.10.002
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doi：10.1016/S0045-2068(03)00026-9
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journal_title：Bioorganic chemistry
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abstract：:The chemical investigation of the fruits of a mangrove Sonneratia apetala collected from the Beibu Gulf led to the isolation of four new compounds, sonneradons A-D (1-4), as well as 18 known compounds (5-22). The structures of the new compounds were elucidated based on extensive spectroscopic analysis, and the structu...
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更新日期：2020-06-01 00:00:00
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journal_title：Bioorganic chemistry
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更新日期：2014-02-01 00:00:00
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journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.103170
更新日期：2019-10-01 00:00:00
