ANGPT2

Synonyms

ANGPT2, Angiopoietin 2, ANG-2, Angiopoietin-2B, Angiopoietin-2a, Angiopoietin-2, Tie2-Ligand, AGPT2, ANG2

Description

Binds to TEK/TIE2, competing for the ANGPT1 binding site, and modulating ANGPT1 signaling. Can induce tyrosine phosphorylation of TEK/TIE2 in the absence of ANGPT1. In the absence of angiogenic inducers, such as VEGF, ANGPT2-mediated loosening of cell-matrix contacts may induce endothelial cell apoptosis with consequent vascular regression. In concert with VEGF, it may facilitate endothelial cell migration and proliferation, thus serving as a permissive angiogenic signal.

KO Status

RenLite: F0

Drug Information

Drugs in clinical trials: 11
Latest Research Phase: NDA/BLA

Drug Name

Code

Phase

Company

Indications

Clinical Trials

Faricimab

RG-7716, RO-6867461

NDA/BLA

F. Hoffmann-La Roche Ltd

Macular Edema, Diabetic macular oedema, Wet Macular Degeneration, Retinal Vein Occlusion, Macular Degeneration, Diabetes Mellitus, Choroidal Neovascularization

Vanucizumab

RG-7221, RO-5520985, B800Z06O8K (UNII code)

Phase 2 Clinical

F. Hoffmann-La Roche Ltd

Solid tumours, Neoplasms, Colorectal Neoplasms

LY-3127804

LY-3127804

Phase 2 Clinical

Eli Lilly And Company

Solid tumours, Pneumonia, Coronavirus Disease 2019 (COVID-19)

Aflibercept/Nesvacumab

REGN 910-3

Phase 2 Clinical

Regeneron Pharmaceuticals Inc

Diabetic macular oedema, Macular Degeneration

BI-836880

BI-836880

Phase 2 Clinical

Ablynx

Wet Macular Degeneration, Carcinoma, Squamous Cell, Macular Degeneration, Carcinoma, Non-Small-Cell Lung

Trebananib

AMG-386, 20060439

Phase 2 Clinical

Amgen Inc, Takeda Pharmaceutical Co Ltd

Ovarian Neoplasms, Solid tumours, Carcinoma, Renal Cell, Carcinoma, Rectal Neoplasms, Kidney Diseases, Colonic Neoplasms, Breast Neoplasms, Peritoneal Neoplasms, Genital Neoplasms, Female, Colorectal Neoplasms, Fallopian Tube Neoplasms, Carcinoma, Non-Small-Cell Lung, Neoplasm Metastasis, Gastrointestinal Neoplasms

RO-7250284

RO-7250284

Phase 1 Clinical

F. Hoffmann-La Roche Ltd

Macular Degeneration

RG-6120

RG-6120

Phase 1 Clinical

F. Hoffmann-La Roche Ltd

Macular Degeneration

MEDI-3617

ANG-2-mAb, MEDI-3617, Anti-ANG-2-mAb

Phase 1 Clinical

Medimmune

Ovarian Neoplasms, Solid tumours, Melanoma

AMG-780

AMG-780

Phase 1 Clinical

Amgen Inc

Solid tumours, Neoplasms

References


Title

Authors

Source

Complete sequencing and characterization of 21,243 full-length human cDNAs

Ota T., Suzuki Y., Nishikawa T., Otsuki T., Sugiyama T., Irie R., Wakamatsu A., Hayashi K., Sato H., Nagai K., Kimura K., Makita H., Sekine M., Obayashi M., Nishi T., Shibahara T., Tanaka T., Ishii S., Sugano S.,

Nat. Genet. 36:40-45(2004)

DNA sequence and analysis of human chromosome 8

Nusbaum C., Mikkelsen T.S., Zody M.C., Asakawa S., Taudien S., Garber M., Kodira C.D., Schueler M.G., Shimizu A., Whittaker C.A., Chang J.L., Cuomo C.A., Dewar K., FitzGerald M.G., Yang X., Allen N.R., Anderson S., Asakawa T., Lander E.S.,

Nature 439:331-335(2006)

The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC)

The MGC Project Team,

Genome Res. 14:2121-2127(2004)

Angiopoietin-1 and angiopoietin-2 share the same binding domains in the Tie-2 receptor involving the first Ig-like loop and the epidermal growth factor-like repeats

Fiedler U., Krissl T., Koidl S., Weiss C., Koblizek T., Deutsch U., Martiny-Baron G., Marme D., Augustin H.G.,

J. Biol. Chem. 278:1721-1727(2003)

Biological characterization of angiopoietin-3 and angiopoietin-4

Lee H.J., Cho C.H., Hwang S.J., Choi H.H., Kim K.T., Ahn S.Y., Kim J.H., Oh J.L., Lee G.M., Koh G.Y.,

FASEB J. 18:1200-1208(2004)

Tyrosine phosphatase beta regulates angiopoietin-Tie2 signaling in human endothelial cells

Yacyshyn O.K., Lai P.F.H., Forse K., Teichert-Kuliszewska K., Jurasz P., Stewart D.J.,

Angiogenesis 12:25-33(2009)

Angiopoietin 2 is a partial agonist/antagonist of Tie2 signaling in the endothelium

Yuan H.T., Khankin E.V., Karumanchi S.A., Parikh S.M.,

Mol. Cell. Biol. 29:2011-2022(2009)

Control of vascular morphogenesis and homeostasis through the angiopoietin-Tie system

Augustin H.G., Koh G.Y., Thurston G., Alitalo K.,

Nat. Rev. Mol. Cell Biol. 10:165-177(2009)

Structure of the angiopoietin-2 receptor binding domain and identification of surfaces involved in Tie2 recognition

Barton W.A., Tzvetkova D., Nikolov D.B.,

Structure 13:825-832(2005)

Crystal structures of the Tie2 receptor ectodomain and the angiopoietin-2-Tie2 complex

Barton W.A., Tzvetkova-Robev D., Miranda E.P., Kolev M.V., Rajashankar K.R., Himanen J.P., Nikolov D.B.,

Nat. Struct. Mol. Biol. 13:524-532(2006)