Target General Information
Target ID T57700
Target Name Proto-oncogene c-Kit
Synonyms C-kit; CD117 antigen; Proto-oncogene tyrosine-protein kinase Kit; SCFR; KIT
Target Type Successful
Gene Name KIT
Biochemical Class Kinase
UniProt ID KIT_HUMAN
Target Gene Expression Profiles in the Disease-Relevant Drug Targeted Tissue of the Patients and Healthy Individuals
Disease Acute myelocytic leukemia
Example drug Imatinib Approved [536294], [541030], [1572592]
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: 1.65
Z-score: 2.12
P-value: 9.88E-36
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 Renal cancer
Example drug Pazopanib HCl Approved [530677], [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: -1.17
Z-score: -2.77
P-value: 5.94E-06
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: -0.87
Z-score: -1.40
P-value: 1.82E-13
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 Alzheimer's disease
Example drug PLX-3397 Phase 3 [525099], [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: -0.10
Z-score: -0.14
P-value: 2.06E-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 Rectal cancer
Example drug Imatinib Phase 3 [536294], [541030], [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: -1.49
Z-score: -3.60
P-value: 9.00E-05
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: -1.16
Z-score: -4.48
P-value: 1.04E-06
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 Breast cancer
Example drug Sorafenib Phase 2 [528230], [541050], [1572592]
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: -2.83
Z-score: -2.30
P-value: 1.89E-108
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: -2.63
Z-score: -1.77
P-value: 2.46E-14
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
Example drug Sorafenib Phase 2 [528230], [541050], [1572592]
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: -0.44
Z-score: -0.75
P-value: 1.26E-09
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 Lung cancer
Example drug Imatinib Phase 2 [536294], [541030], [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: -0.78
Z-score: -1.33
P-value: 2.26E-22
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: -0.91
Z-score: -1.19
P-value: 1.80E-18
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 Gastric cancer
Tissue Gastric tissue
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: -1.17
Z-score: -7.37
P-value: 3.70E-04
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: -1.47
Z-score: -1.56
P-value: 7.06E-04
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 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: 0.12
Z-score: 0.37
P-value: 1.01E-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: 5.26
Z-score: 3.69
P-value: 5.81E-03
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 Ovarian cancer
Tissue Ovarian tissue
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: -2.87
Z-score: -1.97
P-value: 3.50E-04
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: 0.08
Z-score: 0.08
P-value: 5.87E-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 Thyroid cancer
Tissue Thyroid
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: -3.47
Z-score: -5.35
P-value: 3.35E-88
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: -3.04
Z-score: -5.97
P-value: 1.89E-52
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 541030(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: 5687).
Ref 541050(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: 5711).
Ref 528230Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature. Methods Enzymol. 2006;407:597-612.
Ref 536294Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19.
Ref 530677Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
Ref 525099ClinicalTrials.gov (NCT02371369) PLX3397 Phase 3 Study for Pigmented Villonodular Synovitis (PVNS) or Giant Cell Tumor of the Tendon Sheath (GCT-TS). U.S. National Institutes of Health.
Ref 1572592NCBI GEO: archive for functional genomics data sets--update.

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