Target General Information
Target ID T07303
Target Name VEGF-3 receptor
Synonyms VEGFR-3; VEGFR3; Fms-like tyrosine kinase 4; FLT-4; Tyrosine-protein kinase receptor FLT4; VEGF-3 receptor; FLT4
Target Type Successful
Gene Name FLT4
Biochemical Class Kinase
UniProt ID VGFR3_HUMAN
Target Gene Expression Profiles in the Disease-Relevant Drug Targeted Tissue of the Patients and Healthy Individuals
Disease Rectal cancer
Example drug Regorafenib Approved [532210], [541189], [1572592]
Tissue Rectal colon tissue
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: 0.12
Z-score: 1.23
P-value: 3.75E-02
Level of differential expression between the patients in the disease section of the tissue and the patients in the normal section of the tissue adjacent to the disease section Fold-change: 0.12
Z-score: 0.61
P-value: 8.75E-02
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles of the patients in the normal section of the tissue adjacent to the disease section
Target gene expression profiles in the tissue of healthy individual
Disease Renal cancer
Example drug Tivozanib Phase 3 [522960], [541307], [1572592]
Tissue Kidney
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: -0.17
Z-score: -0.69
P-value: 7.15E-01
Level of differential expression between the patients in the disease section of the tissue and the patients in the normal section of the tissue adjacent to the disease section Fold-change: -0.06
Z-score: -0.20
P-value: 2.66E-01
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles of the patients in the normal section of the tissue adjacent to the disease section
Target gene expression profiles in the tissue of healthy individual
Disease Lung cancer
Example drug PI-88 Phase 2 [537114], [1572592]
Tissue Lung tissue
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: -0.64
Z-score: -1.74
P-value: 4.66E-60
Level of differential expression between the patients in the disease section of the tissue and the patients in the normal section of the tissue adjacent to the disease section Fold-change: -0.89
Z-score: -2.29
P-value: 6.90E-51
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles of the patients in the normal section of the tissue adjacent to the disease section
Target gene expression profiles in the tissue of healthy individual
Disease Prostate cancer
Example drug PI-88 Phase 2 [537114], [1572592]
Tissue Prostate
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: 0.45
Z-score: 0.97
P-value: 8.36E-03
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
Disease Alzheimer's disease
Example drug MK-2461 Phase 1/2 [530708], [1572592]
Tissue Entorhinal cortex
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: -0.04
Z-score: -0.23
P-value: 6.00E-01
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
Disease Acute myelocytic leukemia
Tissue Bone marrow
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: 0.02
Z-score: 0.12
P-value: 7.70E-03
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
Disease Breast cancer
Tissue Breast tissue
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: -0.31
Z-score: -0.93
P-value: 1.41E-35
Level of differential expression between the patients in the disease section of the tissue and the patients in the normal section of the tissue adjacent to the disease section Fold-change: -0.28
Z-score: -0.91
P-value: 3.89E-09
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles of the patients in the normal section of the tissue adjacent to the disease section
Target gene expression profiles in the tissue of healthy individual
Disease Head and neck cancer
Tissue Head and neck tissue
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: 0.04
Z-score: 0.17
P-value: 1.14E-01
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
Disease Myelodysplastic syndromes
Tissue Bone marrow
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: -0.06
Z-score: -0.41
P-value: 9.59E-01
Level of differential expression between the patients in the disease section of the tissue and the patients in the normal section of the tissue adjacent to the disease section Fold-change: -0.26
Z-score: -0.69
P-value: 2.94E-01
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles of the patients in the normal section of the tissue adjacent to the disease section
Target gene expression profiles in the tissue of healthy individual
Target Gene Expression Profiles in Other Tissues of Healthy Individuals
Reference
Ref
Ref 541189(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5891).
Ref 541307(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6058).
Ref 537114Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
Ref 530708MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
Ref 532210Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
Ref 522960ClinicalTrials.gov (NCT01076010) An Extension Treatment Protocol for Subjects Who Have Participated in a Phase 3 Study of Tivozanib Versus Sorafenib in Renal Cell Carcinoma (Protocol AV-951-09-301). U.S. National Institutes of Health.
Ref 1572592NCBI GEO: archive for functional genomics data sets--update.

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