Angiogenesis - Selective
Angiogenesis is the growth of new blood vessels from the existing vasculature. This process is involved in development, wound healing, embryo formation and tumor growth. Activation of angiogenesis leads to the release of pro-angiogenic growth factors such as VEGF, PDGF, FGF and TGF, which bind their receptors on endothelial cells within pre-existing vessels. As a result, it induces signal transduction of various pathways such as PI3K/Akt, Erk1/2, Smad and Notch, causing endothelial cells proliferation and migration. Endothelial cells use matrix metalloproteases and integrins to digest extracellular matrix and migrate into new area, where they lengthen and form tubes, generating new blood vessel.
During tumor angiogenesis, cancer cells stimulate formation of new blood vessel for delivering oxygen and nutrients to a tumor. As the tumor grows, cells at the center of the mass become starved of oxygen, causing hypoxia. It stabilizes the expression of a transcription factor, HIF-1α (hypoxia inducible factor-1), which binds HIF-1β to upregulate the expression of several angiogenesis-promoting genes. Moreover, growth factor signaling also stimulates HIF-1 activity in order to maintain oxygen homeostasis for growing cells.
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- B6185 ACP-196中文名: 阿卡替尼Target: BTKSummary: 不可逆的BTK抑制剂
- B5851 FG2216Target: Pyruvate dehydrogenases (PDH)Summary: HIF-脯氨酰羟化酶抑制剂
- B7157 OGT 2115Target: HeparanasesSummary: 乙酰肝素酶抑制剂
- B3708 RGD (Arg-Gly-Asp) Peptides1 CitationTarget: Integrin-ligand interactionsSummary: 抑制整合素结合到RGD基序
- B1115 BAY 87-2243Target: Hypoxia Inducible Factors (HIFs)Summary: 有效的HIF-1选择性抑制剂
- A8669 AC 55541Target: PARSummary: PAR2激动剂
- A8660 Cilengitide1 Citation中文名: 西仑吉肽Target: IntegrinsSummary: 整合素αvβ3和αvβ5的抑制剂
- A8233 DMXAA (Vadimezan)2 Citation中文名: 2,5-己酮可可碱Target: DT-diaphorasesSummary: 肿瘤血管破坏剂,细胞凋亡诱导剂。
- A4506 DMOGTarget: Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors (HIF-PHIs)Summary: 细胞通透的竞争性HIF-PH抑制剂
- A3302 CGI-17461 CitationTarget: BTKSummary: Btk抑制剂