Target's General Information
Target ID T99840
Target Name Gamma-secretase (GS)
Synonyms Presenilin-stabilization factor-like; PSFL; Aph-1beta
Target Type Successful
Gene Name APH1A; APH1B; NCSTN; PSENEN; PSEN1
UniProt ID APH1A_HUMAN||APH1B_HUMAN||NICA_HUMAN||PEN2_HUMAN||PSN1_HUMAN
Target's Expression Profile in Disease Related Tissue between Patients and Normal People
Disease Alzheimer's disease
Example drug PF-03084014 Phase 2 [1], [2], [3], [4]
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: -0.09
Z-score: -0.37
P-value: 1.47E-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 Breast cancer
Example drug RO-4929097 Phase 2 [3], [4], [5], [6]
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: 0.81
Z-score: 0.65
P-value: 1.90E-10
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: 0.42
Z-score: 0.36
P-value: 8.51E-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 Parkinson's disease
Tissue Substantia nigra tissue
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: -0.27
Z-score: -0.71
P-value: 4.02E-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
Target's Expression Profile across Various Tissues of Healthy Individual
References
REF 1 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: 7746).
REF 2 ClinicalTrials.gov (NCT02299635) A Study Evaluating PF-03084014 In Patients With Advanced Breast Cancer With Or Without Notch Alterations. U.S. National Institutes of Health.
REF 3 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
REF 4 NCBI GEO: archive for functional genomics data sets--update. Nucleic Acids Res. 2013 Jan;41(Database issue):D991-5.
REF 5 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: 7338).
REF 6 Phase I study of RO4929097, a gamma secretase inhibitor of Notch signaling, in patients with refractory metastatic or locally advanced solid tumors. J Clin Oncol. 2012 Jul 1;30(19):2348-53.

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