Target Information

Target General Infomation
Target ID
T30926
Former ID
TTDI02247
Target Name
mRNA of GRB2
Gene Name
GRB2
Synonyms
Adapter protein GRB2 (mRNA); GRB2 (mRNA); Growth factor receptorbound protein 2 (mRNA); Protein Ash (mRNA); SH2/SH3 adapter GRB2 (mRNA); GRB2
Target Type
Clinical Trial
Disease Acute lymphoblastic leukemia; Acute myeloid leukemia; Chronic myelogenous leukemia; Hematological malignancies; Myelodysplastic syndrome [ICD9:204.0, 205.0, 205.1, 238.7, 200-209; ICD10: C91.0, C92.0, C92.1, D46, C81-C86]
Function
Isoform 2 does not bind to phosphorylated epidermal growthfactor receptor (EGFR) but inhibits EGF-induced transactivation of a RAS-responsive element. Isoform 2 acts as a dominant negative protein over GRB2 and by suppressing proliferative signals, may trigger active programmed cell death.
BioChemical Class
Target of antisense drug
UniProt ID
P62993
Sequence
MEAIAKYDFKATADDELSFKRGDILKVLNEECDQNWYKAELNGKDGFIPKNYIEMKPHPW
FFGKIPRAKAEEMLSKQRHDGAFLIRESESAPGDFSLSVKFGNDVQHFKVLRDGAGKYFL
WVVKFNSLNELVDYHRSTSVSRNQQIFLRDIEQVPQQPTYVQALFDFDPQEDGELGFRRG
DFIHVMDNSDPNWWKGACHGQTGMFPRNYVTPVNRNV
Drugs and Mode of Action
Drug(s) BP-100-1-01 Drug Info Phase 2 Acute lymphoblastic leukemia; Acute myeloid leukemia; Chronic myelogenous leukemia; Hematological malignancies; Myelodysplastic syndrome [549112]
Modulator BP-100-1-01 Drug Info [523107], [533092]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
NetPath Pathway EGFR1 Signaling Pathway
Pathway Interaction Database Fc-epsilon receptor I signaling in mast cells
BCR signaling pathway
ErbB4 signaling events
Insulin Pathway
GMCSF-mediated signaling events
IL4-mediated signaling events
TCR signaling in na&amp
#xef
ve CD4+ T cells
Plasma membrane estrogen receptor signaling
Signaling events mediated by Hepatocyte Growth Factor Receptor (c-Met)
Signaling events mediated by PTP1B
EPHB forward signaling
Signaling events regulated by Ret tyrosine kinase
TCR signaling in na&amp
ve CD8+ T cells
Signaling events mediated by TCPTP
Angiopoietin receptor Tie2-mediated signaling
SHP2 signaling
IL2-mediated signaling events
IGF1 pathway
EGF receptor (ErbB1) signaling pathway
IL5-mediated signaling events
EGFR-dependent Endothelin signaling events
IL2 signaling events mediated by PI3K
ErbB1 downstream signaling
ErbB2/ErbB3 signaling events
IL3-mediated signaling events
IL6-mediated signaling events
PDGFR-beta signaling pathway
Neurotrophic factor-mediated Trk receptor signaling
Nephrin/Neph1 signaling in the kidney podocyte
PDGFR-alpha signaling pathway
Internalization of ErbB1
Signaling events mediated by Stem cell factor receptor (c-Kit)
EPO signaling pathway
IL2 signaling events mediated by STAT5
Signaling events mediated by VEGFR1 and VEGFR2
a6b1 and a6b4 Integrin signaling
Regulation of Ras family activation
Trk receptor signaling mediated by PI3K and PLC-gamma
EPHA2 forward signaling
VEGFR3 signaling in lymphatic endothelium
FGF signaling pathway
Signaling events mediated by focal adhesion kinase
TGF-beta receptor signaling
References
Ref 549112Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032443)
Ref 523107ClinicalTrials.gov (NCT01159028) Clinical Trial of BP1001 (L-Grb-2 Antisense Oligonucleotide) in CML, AML, ALL & MDS. U.S. National Institutes of Health.
Ref 533092Liposomal delivery of nucleic acid-based anticancer therapeutics: BP-100-1.01. Expert Opin Drug Deliv. 2015 Jul;12(7):1107-20.

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