Target General Information
Target ID T67849
Target Name PI3-kinase delta
Synonyms P110delta; PI3-kinase p110 subunit delta; PI3K; Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit, delta isoform; Phosphoinositide 3-kinase delta; PtdIns-3-kinase p110; PIK3CD
Target Type Successful
Gene Name PIK3CD
Biochemical Class Kinase
UniProt ID PK3CD_HUMAN
Target Gene Expression Profiles in the Disease-Relevant Drug Targeted Tissue of the Patients and Healthy Individuals
Disease Breast cancer
Example drug Buparlisib Phase 3 [523929], [542804], [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: -0.08
Z-score: -0.28
P-value: 1.03E-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: 0.07
Z-score: 0.18
P-value: 4.06E-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 [532543], [542746], [1572592]
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: -0.39
Z-score: -1.39
P-value: 3.63E-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
Disease Acute myelocytic leukemia
Example drug AMG 319 Phase 1 [523366], [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: -0.37
Z-score: -0.91
P-value: 4.31E-16
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 Gene Expression Profiles in Other Tissues of Healthy Individuals
Reference
Ref 542746(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 542804(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 532543PI3K-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 523366ClinicalTrials.gov (NCT01300026) AMG 319 Lymphoid Malignancy FIH. U.S. National Institutes of Health.
Ref 523929ClinicalTrials.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 1572592NCBI GEO: archive for functional genomics data sets--update.

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