DNA damage and mutation have different biological consequences. While most DNA damages can undergo DNA repair, such repair is not 100% efficient. These errors can give rise to mutations or epigenetic alterations. Both of these types of alteration can be replicated and passed on to subsequent cell generations. These alterations can change gene function or regulation of gene expression and possibly contribute to progression to cancer.
DNA repair is a collection of processes by which a cell identifies and corrects damage to the DNA molecules that encode its genome. The DNA repair process is constantly active as it responds to damage in the DNA structure. When normal repair processes fail, and when cellular apoptosis does not occur, irreparable DNA damage may occur, including double-strand breaks and DNA crosslinkages (interstrand crosslinks or ICLs). This can eventually lead to malignant tumors, or cancer as per the two hit hypothesis.
(-)-Epigallocatechin Gallate(EGCG)是多酚类黄酮抗氧化剂,能抑制端粒酶和DNA甲基转移酶,还能阻断EGF和HER-2的受体活性。
MoreStaurosporine (AM-2282)是一种有效的PKC抑制剂,作用于PKCα, PKCγ和PKCη时,IC50分别为2 nM, 5 nM和4 nM,对PKCδ(20 nM), PKCε(73 nM)和PKCζ(1086 nM)作用效果稍弱。
MoreCurcumin是具有很好抗氧化活性的天然多酚类化合物,能激活Nrf2起到化疗防护效果。
MoreAnisomycin, a bacterial antibiotic, known as a peptidyl transferase inhibitor, induces apoptosis by activating several MAPKs and by inhibiting protein synthesis. Anisomycin是一种吡咯烷抗生素, 抑制蛋白质合成, 也是有效的SAPKs/JNKs激活剂。
MoreBisindolylmaleimide I (BMI, GF109203X) is a high selectivity, cell-permeable and ATP-competitive inhibitor of PKC and shows GSK-3 inhibition as well. GF 109203X是一种有效的PKC抑制剂,抑制PKCα,PKCβI,PKCβII和PKCγ,IC50分别为20 nM,17 nM,16nM和20 nM,作用于PKC比作用于EGFR,PDGFR和胰岛素受体选择性高3000倍以上。
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