Target's General Information
Target ID T95913
Target Name PI3-kinase gamma (PIK3CG)
Synonyms p120-PI3K; p110gamma; Serine/threonine protein kinase PIK3CG; PtdIns-3-kinase subunit p110-gamma; PtdIns-3-kinase subunit gamma; PtdIns-3-kinase p110; Phosphoinositol-3 kinase; Phosphoinositide-3-kinase catalytic gamma polypeptide; Phosphoinositide 3-Kinase gamma; Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit, gamma isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit gamma; PI3Kgamma; PI3K-gamma; PI3K; PI3-kinase subunit gamma; PI3-kinase p110 subunit gamma
Target Type Successful
Gene Name PIK3CG
Biochemical Class Kinase
UniProt ID PK3CG_HUMAN
Target's Expression Profile in Disease Related Tissue between Patients and Normal People
Disease Type 2 diabetes
Example drug CHU Registered [1], [2], [3]
Tissue Liver tissue
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: -0.05
Z-score: -0.55
P-value: 1.98E-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 Breast cancer
Example drug Buparlisib Phase 3 [2], [3], [4], [5]
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: -0.17
Z-score: -0.49
P-value: 1.16E-01
Level of differential expression between the patients in the disease section of the tissue section of the tissue adjacent to the disease section Fold-change: -0.05
Z-score: -0.13
P-value: 5.67E-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 Rheumatoid arthritis
Example drug IPI-145 Phase 3 [2], [3], [6], [7]
Tissue Synovial tissue
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: 0.25
Z-score: 0.73
P-value: 1.67E-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 Uterine cancer
Example drug PF-04691502 Phase 2 [2], [3], [8], [9]
Tissue Endometrium tissue
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: -0.07
Z-score: -0.3
P-value: 9.64E-01
Level of differential expression between the patients in the disease section of the tissue section of the tissue adjacent to the disease section Fold-change: 0.22
Z-score: 0.7
P-value: 6.08E-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 Myeloma
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: 0.17
Z-score: 0.58
P-value: 2.69E-02
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
Target's Expression Profile across Various Tissues of Healthy Individual
References
REF 1 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027532)
REF 2 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
REF 3 NCBI GEO: archive for functional genomics data sets--update. Nucleic Acids Res. 2013 Jan;41(Database issue):D991-5.
REF 4 URL: 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: 7878).
REF 5 ClinicalTrials.gov (NCT01610284) Phase III Study of BKM120/Placebo With Fulvestrant in Postmenopausal Patients With Hormone Receptor Positive HER2-negative Locally Advanced or Metastatic Breast Cancer Refractory to Aromatase Inhibitor. U.S. National Institutes of Health.
REF 6 URL: 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: 7795).
REF 7 PI3K-delta and PI3K-gamma inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. Chem Biol. 2013 Nov 21;20(11):1364-74.
REF 8 URL: 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: 7936).
REF 9 ClinicalTrials.gov (NCT01430585) Pre-Operative Study of PF-4691502 With Letrozole Compared To Letrozole Alone In Patients With Early Breast Cancer. U.S. National Institutes of Health.

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