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细胞信号通路常用抑制剂之VEGFR-PDGFR篇
今天我来介绍一下VEGFR-PDGFR以及目前研究中常用的抑制剂~
Vascular endothelial growth factor receptor-Platelet derived growth factor receptor(): 血管内皮生长因子受体- 血小板源性生长因子受体
血管内皮生长因子受体：是一种受体酪氨酸激酶，可以通过与相应配体VEGR的结合引起受体分子在细胞膜上的二聚化，并使受体胞内激酶区特定的酪氨酸残基交叉磷酸化而被激活，从而活化一系列下游信号分子，如磷脂酶C-γ(PLC-γ)，蛋白激酶C(PKC)，磷脂酰肌醇-3-激酶(PI-3-K)， 丝裂原活化的蛋白激酶(MAPK)等，通过调节特定基因的表达实现VEGF的生物学效应。这个信号通路发挥了促进血管生成的作用，使其在正常的胚胎发育和病理的肿瘤发生等过程中都扮演着十分重要的角色。
血小板源性生长因子受体：是一种具有酪氨酸激酶活性的跨膜糖蛋白，由两种亚单位α及β构成，其分子量为170～180KD. 当受体与其配体结合后促使两个受体分子形成二聚体，激活细胞内结构域酪氨酸残基自身磷酸化，或促使激活特殊靶蛋白的酪氨酸残基磷酸化，从而将信号传入细胞内，通过调节相应靶基因的表达来调控细胞的生命活动，包括靶细胞的分裂增殖。
下面是抑制剂的介绍：
AEE788 is a novel multitargeted human epidermal receptor (HER) 1/2 and vascular endothelial growth factor receptor (VEGFR) 1/2 receptor family tyrosine kinases inhibitor with IC50 of 2, 6, 77, 59 nM for EGFR, ErbB2, KDR, and Flt-1.
Apatinib (YN968D1) is a small-molecule selective multitargeted tyrosine kinase inhibitor with an IC50 of 2.43 nM for the inhibition of VEGFR2.
Tivozanib also known as AV-951 is an orally bioavailable potent VEGFR-1, 2 and 3, c-Kit and PDGFR inhibitor with IC50 of 0.21, 0.16, 0.24, 1.63 and 1.72 nM, respectively.
Axitinib blocked phosphorylation of VEGFR-2 and VEGFR-3 with average IC50s of 0.2 and 0.1 to 0.3 nM.
BIBF1120 (Vargatef) is an inhibitor of VEGFR, PDGFR and FGFR. all three VEGFR subtypes (IC50=13–34nmol/L) , PDGFRa and PDGFRh (IC50=59and65nmol/L) , and FGFRtypes 1, 2, and 3 (IC50=69, 37, and 108 nmol/L,respectively).
BMS-794833 is a potent ATPcompetitive Met/VEGFR-2 kinase inhibitor and it also inhibits Ron (Met family),Axl and Flt-3 with IC50 values <3 nM.
Brivanib (BMS-540215) is a VEGFR -2 inhibitor with an IC50 of 25 nM and Ki of 26 nM.
A multiple inhibitor of VEGFR( IC50 of VEGFR-2(25 nM), VEGFR-1 (380nM), VEGFR-3 (10 nM)); FGFR (FGFR-1 (IC50=148 nM), FGFR-2 (IC50 =125 nM), and FGFR-3 (IC50 = 68 nM))tyrosine kinases.
VEGFR2 inhibitor. It inhibited VEGF-stimulated proliferation and KDR phosphorylation with IC50s of 0.4 and 0.5 nM, respectively.
CYC116 is an Aurora kinase/VEGFR2 inhibitor.
Dovitinib (TKI258) is a highly potent, novel multitargeted growth factor receptor kinase inhibitor with IC50 of 1, 2, 5, 10, 8, 27, 36 nM for FLT3, c-KIT, FGFR, VEGFR1/2/3, PDGFR? and CSF-1R, respectively.
Foretinib (GSK1363089, XL880) is a novel MET and VEGFR2/KDR kinases inhibitor with an IC50 of 0.4 and 0.8 nM for MET and KDR, respectively.
Imatinib (Gleevec) is a number of tyrosine kinase enzymes specific inhibitor.
Imatinib Mesylate is a multitargeted c-kit, PDGF-R and c-ABL inhibitor with IC50 of 3.9 and 2.9 μM for the inhibition of T-cell proliferation stimulated by DCs and PHA, respectively.
Ki8751 is a potent, selective VEGFR-2 tyrosine kinase inhibitor with IC50 of 0.9 nM, 40, 67, 170 nM for VEGF-2, c-Kit, PDGFRα and FGFR-2, respectively.
KRN 633 is a cell-permeable, reversible, ATP-competitive VEGFR kinase inhibitor with IC50 of 170 nM, 160 nM, and 125 nM for VEGFR-1, VEGFR-2, VEGFR-3, respectively.
Linifanib (ABT-869) is a structurally novel, potent RTK and VEGF and PDGF receptor families inhibitor with IC50 of 0.2, 2, 4, and 7 nM for human endothelial cells, PDGFR-β, KDR, and CSF-1R, respectively.
Masitinib also known as Masivet, AB1010 is a tyrosine kinase, c-Kit, PDGFR, FGFR3, the FAK pathway inhibitor with IC50 of 150 ± 80, 200 ± 40 nM.
MGCD-265 is a multi-targeted kinase inhibitor, which targets the c-MET, VEGFR1, VEGFR2, VEGFR3, Tie-2 and Ron receptor tyrosine kinases.
Motesanib (AMG-706) is a multiple inhibitor of VEGFR1/2/3(IC50: 2 ηM /3 ηM /6 ηM),PDGFR (84ηM), kit (8ηM), and Ret (59ηM)receptors.
MP-470 is a multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Met, c-Kit, PDGFRalpha, Flt3, and c-Ret and with an IC50 of median 5 μM.
NVP-BHG712 is a small molecule specific EphB4, VEGFR2, c-raf, c-src and c-Abl kinase inhibitor with ED50 of 25 nM, 4.2, 0.4, 1.3 and 1.7μM, respectively.
OSI-930 is an inhibitor of the receptor tyrosine kinases c-Kit (IC50:9.5nM) and VEGFR-2 (IC50:10.1nM).
Pazopanib is a VEGFR inhibitor, IC50 of 10, 30, and 47 nM for VEGFR-1, -2, and -3.
PD173074 is a potent ATP-competitive, reversible FGFR and VEGFR inhibitor with IC50 of 5, 21.5 and ~100 nM for FGFR3, FGFR1 and VEGFR2, respectively.
Ponatinib (AP24534) is a novel potent, orally available small molecule multitargeted kinase inhibitor with IC50 of 0.37, 2, 1.5, 2.2, 1.1, 1and 0.24 nM for native pan-BCR-ABL, mutated form, VEGFR2, FGFR1, PDGFRα, mutant FLT3 phosphorylation and LYN.
PP121 is a multitargeted dual receptor tyrosine kinases inhibitor with IC50 of 0.052, 1.4, 0.15, 1.1, 0.06, 0.01and 0.002 μM for p110α, p110β, p110δ, p110γ, DNA-PK, mTOR and PDGFR, respectively.
RAF265 (CHIR-265) is an oral, highly selective RAF and VEGFR kinase inhibitor with IC50 of of 5 to 10 μM.
Raf265 derivative is a derivative of Raf265 that is an oral, highly selective RAF and VEGFR kinase inhibitor with IC50 of of 5 to 10 μM.
Regorafenib (BAY 73-4506) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf.
Sorafenib (Nexavar) is a novel, small molecular inhibitor of several tyrosine protein kinases (VEGFR and PDGFR) and RAF/MEK/ERK cascade inhibitor with an IC50 of 6, 22, 38 nM for Raf-1, wt BRAF and V599E mutant BRAF.
Sunitinib Malate (Sutent) is a multitargeted FLT3, PDGFRs, VEGFRs, and Kit kinase inhibitor with Ki of 0.009 and 0.008 ?M for Flk-1 and PDGFR.
Telatinib (BAY 57-9352) is an orally available, potent multitargeted VEGFR-2, VEGFR-3, PDGFR-β and c-Kit tyrosine kinases inhibitor with an IC50 of 19 nM for the inhibition of VEGFR-2 autophosphorylation.
TSU-68 (SU6668)is a novel multiple receptor tyrosine kinase inhibitor with IC50 of 2.1 ?M, 8 nM and 1.2 ?M for VEGF-R1, PDGF-Rβ and FGF-R1, respectively.
Vandetanib (Zactima) is a VEGFR and EGFR antagonist and a tyrosine kinase inhibitor with IC50 of 60, 90, 40 nM for HUVEC proliferation, PC-9 cells and tyrosine kinase activity, respectively.
Vatalanib (PTK787) is a novel VEGFR and c-Kit tyrosine kinases and angiogenesis inhibitor with IC50 of 0.037, 0.077, 0.27 and 0.73 μM for KDR, Flt-1, Flk and c-Kit, respectively.
XL184 (Cabozantinib) is a potent multitargeted VEGFR2, Met, FLT3, Tie2, Kit and Ret inhibitor with IC50 of 0.035, 1.8, 14.4, 14.3 and 4.6 nM for VEGFR2, Met, FLT3, Tie2 and Kit, respectively.
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HEK293F细胞瞬时表达PDGFR-β/Fc蛋白的条件优化