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Bcl-2 、 Bcl-xL 抑制剂与抗癌. 孙鲁超 5091719014. 细胞凋亡信号转导途径. 1. Fas/ CD95 信号转导途径. 2. TNFR_1 信号转导途径. 3. TRAIL 介导的凋亡信号通路. 4. MAPK、JAK_STAT 信号转导途径. 5. G 蛋白信号转导途径. J Environ Occup Med , Feb 2004 Vol. 21 No. 1. Fas/ CD95 信号转导途径.

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slide3
细胞凋亡信号转导途径

1

Fas/ CD95 信号转导途径

2

TNFR_1 信号转导途径

3

TRAIL 介导的凋亡信号通路

4

MAPK、JAK_STAT 信号转导途径

5

G蛋白信号转导途径

J Environ Occup Med, Feb 2004 Vol. 21 No. 1

fas cd95
Fas/ CD95 信号转导途径
  • Fas/ CD95 是典型的死亡受体, 属于I型膜蛋白。在胞质内有一段约80 个氨基酸组成的肽链, 称为“死亡结构域”( death domain, DD) 。Fas 的配体( FasL) 以同源三聚体形式存在,该三聚体为一种叫Fas 相关死亡蛋白( Fas associated death domain protein,FADD) 提供了高亲和力位点。FADD 是一种胞质内蛋白, 包含一个N 末端的死亡效应域( death effect domain, DED) 和一个C 末端的DD。
tnfr 1
TNFR_1 信号转导途径

TNFR_1 信号转导的途径与Fas 信号转导途径相似

bcl 2
Bcl-2家族
  • Bcl-2亚家族可以抑制线粒体释放细胞色素C, 从而影响APAF-1与Caspase-9-前体的结合及Caspase-9的活化, 抑制细胞凋亡。BH3 亚家族的成员可以通过与Bcl-2 亚家族的同源区, 竞争结合Bcl-2, 从而使APAF-1 与Caspase-9前体结合, 启动凋亡。
  • Bcl-2家族的成员通常以二聚体的形式发挥作用,Bcl-2/Bcl-2,Bcl-2/Bax和Bcl-2/Bcl-xL抑制细胞凋亡
ha14 1
HA14-1
  • Ethyl [2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)]-4H-chromene-3-carboxylate

Tetrahedron Letters Volume 49, Issue 20, 12 May 2008, Pages 3276-3278

slide9

To the best of our knowledge, only analogues modified on the aromatic ring have been reported. The biological tests have shown that the bromine in position 6 could be replaced by some alkyl or aryl groups

slide11

Reagents and conditions: (i) ethylvinylether (6.3 equiv), camphorsulfonic

acid (0.2 equiv), THF, 10 C, 4 h then Et3N and K2CO3

(90%); (ii) ethylcyanoacetate (1.1 equiv), EtOH, 3A ˚ mol. Sieves, rt,

overnight (65%); (iii) Amberlyst 15, 4A ˚ mol. Sieves, CH2Cl2, rt, 5 h (80%);

(iv) general procedure: malonate or cyanoacetamide (1.1 equiv), EtOH,

4 A˚ mol. Sieves, piperidine (cat), rt, 5 h, 5a (70%), 5b (79%), 5c (81%), 5d

(73%).

ha14 1 sv30
HA14-1类似物SV30
  • However, HA14-1 is a relatively unstable molecule, which further, is a mixture of two stereoisomers.
  • One of our groups has recently prepared SV30, a new analogue of HA14-1 which is a single stereoisomer, and furthermore appears more stable than HA14-1.

Journal of Controlled Release 151 (2011) 74–82

slide14

(*) Patients with small-cell carcinoma.

(†) Patients with pulmonary carcinoid tumors

Journal of Clinical Oncology 2011;29(7):909-16

slide15

Summary of changes made to ABT-737 ( 32 ) resulting in ABT-263

Expert Opinion on Drug Discovery, Volume 3, Number 9, September 2008 , pp. 1123-1143(21)

slide16

NMR-derived structure of diphenylmethane compound 1 bound to Bcl-2

Bioorganic & Medicinal Chemistry Letters 20 (2010) 6587–6591

slide19

成骨细胞凋亡受体内激素和生长因子等因素调节,Xian 等研究发现IGF- 1能对多种因素引起的细胞凋亡有抑制作用, 保护成骨细胞免于有害物质的毒性作用, 使成骨细胞增加。

  • Bcl- 2 家族在调节成骨细胞凋亡中起重要作用。……Bcl- 2 和Bax在软骨和成骨细胞中的表达, 维持骨基质合成和降解的平衡, 调节着骨形成和骨吸收的平衡。

CHINESE JOURNAL OF INT EGRAT IVE MEDICINE ON

CARDIO- / CEREBROVASCU LAR DISEASEJune 2008Vo1. 6No. 6

slide20

珍珠菜提取物ZE4可通过上调Fas/Fas L 基因, 上调TRA IL 及DR5表达, 下调Bcl- 2表达, 上调Caspase 3表达等途径诱导SMMC-7721肿瘤细胞发生凋亡, 具有良好的抗肿瘤效果。

上海中医药杂志 2010年 第44卷 第3期

slide21

姜黄素可通过抑制Bcl表达增加Bax的表达进一步激活半胱氨酸天冬氨酸蛋白酶8、半胱氨酸天冬氨酸蛋白酶3,抑制肺腺癌A549细胞生长,提高对肿瘤坏死因子相关凋亡诱导配体敏感性。姜黄素可通过抑制Bcl表达增加Bax的表达进一步激活半胱氨酸天冬氨酸蛋白酶8、半胱氨酸天冬氨酸蛋白酶3,抑制肺腺癌A549细胞生长,提高对肿瘤坏死因子相关凋亡诱导配体敏感性。

中国临床康复 第10卷 第31期