Target General Information
Target ID T99840
Target Name Gamma-secretase
Synonyms APH; Aph-1beta; PSFL; Presenilin-stabilization factor-like
Target Type Clinical Trial
Gene Name APH1A
Biochemical Class APH-1 family
UniProt ID APH1A_HUMAN||APH1B_HUMAN||NICA_HUMAN||PEN2_HUMAN||PSN1_HUMAN
Target Gene Expression Profiles in the Disease-Relevant Drug Targeted Tissue of the Patients and Healthy Individuals
Disease Alzheimer's disease
Example drug PF-03084014 Phase 2 [525008], [542711], [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: -0.09
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 [531882], [542361], [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: 0.81
Z-score: 0.65
P-value: 1.90E-10
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: 0.42
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 Gene Expression Profiles in Other Tissues of Healthy Individuals
Reference
Ref
Ref 542361(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 542711(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 531882Phase 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.
Ref 525008ClinicalTrials.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 1572592NCBI GEO: archive for functional genomics data sets--update.

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