Target Information

Target General Infomation
Target ID
T69085
Former ID
TTDC00119
Target Name
Transcription factor AP-1
Gene Name
JUN
Synonyms
AP-1 transcription factor; AP1; Activator protein 1; Activator protein-1; C-jun proto-oncogene; P39; Proto-oncogene c-jun; V-jun avian sarcoma virus 17 oncogene homolog; JUN
Target Type
Discontinued
Disease Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06]
Function
Transcription factor that recognizes and binds to the enhancer heptamer motif 5'-TGA[CG]TCA-3'. Promotes activity of NR5A1 when phosphorylated by HIPK3 leading to increased steroidogenic gene expression upon cAMP signaling pathway stimulation.
Target Validation
T69085
UniProt ID
P05412
Sequence
MTAKMETTFYDDALNASFLPSESGPYGYSNPKILKQSMTLNLADPVGSLKPHLRAKNSDL
LTSPDVGLLKLASPELERLIIQSSNGHITTTPTPTQFLCPKNVTDEQEGFAEGFVRALAE
LHSQNTLPSVTSAAQPVNGAGMVAPAVASVAGGSGSGGFSASLHSEPPVYANLSNFNPGA
LSSGGGAPSYGAAGLAFPAQPQQQQQPPHHLPQQMPVQHPRLQALKEEPQTVPEMPGETP
PLSPIDMESQERIKAERKRMRNRIAASKCRKRKLERIARLEEKVKTLKAQNSELASTANM
LREQVAQLKQKVMNHVNSGCQLMLTQQLQTF
Structure
1A02; 1FOS; 1JNM; 1JUN; 1S9K; 1T2K
Drugs and Mode of Action
Drug(s) T-5224 Drug Info Discontinued in Phase 2 Rheumatoid arthritis [547484]
Inhibitor PNRI-299 Drug Info [535686]
T-5224 Drug Info [550543]
TAM-67 Drug Info [535196]
TWS-119 Drug Info [527964]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway MAPK signaling pathway
ErbB signaling pathway
cAMP signaling pathway
Wnt signaling pathway
Osteoclast differentiation
Focal adhesion
Toll-like receptor signaling pathway
T cell receptor signaling pathway
B cell receptor signaling pathway
TNF signaling pathway
Neurotrophin signaling pathway
GnRH signaling pathway
Estrogen signaling pathway
Oxytocin signaling pathway
Non-alcoholic fatty liver disease (NAFLD)
Cocaine addiction
Amphetamine addiction
Epithelial cell signaling in Helicobacter pylori infection
Salmonella infection
Pertussis
Leishmaniasis
Chagas disease (American trypanosomiasis)
Hepatitis B
Influenza A
HTLV-I infection
Herpes simplex infection
Epstein-Barr virus infection
Pathways in cancer
Viral carcinogenesis
Colorectal cancer
Renal cell carcinoma
Choline metabolism in cancer
Inflammatory bowel disease (IBD)
Rheumatoid arthritis
NetPath Pathway IL-7 Signaling Pathway
IL1 Signaling Pathway
TCR Signaling Pathway
IL2 Signaling Pathway
IL4 Signaling Pathway
TSH Signaling Pathway
TGF_beta_Receptor Signaling Pathway
AndrogenReceptor Signaling Pathway
RANKL Signaling Pathway
PANTHER Pathway Angiogenesis
Apoptosis signaling pathway
B cell activation
FAS signaling pathway
Huntington disease
Inflammation mediated by chemokine and cytokine signaling pathway
Oxidative stress response
PDGF signaling pathway
TGF-beta signaling pathway
T cell activation
Toll receptor signaling pathway
Ras Pathway
CCKR signaling map ST
Pathway Interaction Database Regulation of nuclear SMAD2/3 signaling
Fc-epsilon receptor I signaling in mast cells
Endothelins
BCR signaling pathway
RhoA signaling pathway
LPA receptor mediated events
CD40/CD40L signaling
Signaling events mediated by Hepatocyte Growth Factor Receptor (c-Met)
Calcineurin-regulated NFAT-dependent transcription in lymphocytes
Osteopontin-mediated events
Validated transcriptional targets of AP1 family members Fra1 and Fra2
Presenilin action in Notch and Wnt signaling
Integrin-linked kinase signaling
CDC42 signaling events
Signaling events regulated by Ret tyrosine kinase
Regulation of Telomerase
IL1-mediated signaling events
Glucocorticoid receptor regulatory network
IL2-mediated signaling events
Direct p53 effectors
Regulation of Androgen receptor activity
ErbB1 downstream signaling
ATF-2 transcription factor network
AP-1 transcription factor network
ErbB2/ErbB3 signaling events
IL6-mediated signaling events
PDGFR-beta signaling pathway
JNK signaling in the CD4+ TCR pathway
Nephrin/Neph1 signaling in the kidney podocyte
Validated nuclear estrogen receptor alpha network
PDGFR-alpha signaling pathway
Regulation of nuclear beta catenin signaling and target gene transcription
Signaling mediated by p38-alpha and p38-beta
Calcium signaling in the CD4+ TCR pathway
HIF-1-alpha transcription factor network
S1P2 pathway
Downstream signaling in na&amp
#xef
ve CD8+ T cells
FGF signaling pathway
RAC1 signaling pathway
Regulation of retinoblastoma protein
Signaling events mediated by focal adhesion kinase
FOXA1 transcription factor network
IL12 signaling mediated by STAT4
PathWhiz Pathway Intracellular Signalling Through Adenosine Receptor A2a and Adenosine
Intracellular Signalling Through Adenosine Receptor A2b and Adenosine
Reactome Pre-NOTCH Transcription and Translation
Oxidative Stress Induced Senescence
Senescence-Associated Secretory Phenotype (SASP)
FCERI mediated MAPK activation
Activation of the AP-1 family of transcription factors
MAPK6/MAPK4 signaling
WikiPathways Toll-like receptor signaling pathway
Estrogen signaling pathway
DNA Damage Response (only ATM dependent)
SIDS Susceptibility Pathways
TCR Signaling Pathway
ErbB Signaling Pathway
Senescence and Autophagy in Cancer
TGF Beta Signaling Pathway
IL-2 Signaling Pathway
Insulin Signaling
EGF/EGFR Signaling Pathway
Wnt Signaling Pathway
MAPK Cascade
Wnt Signaling Pathway and Pluripotency
MAPK Signaling Pathway
TGF beta Signaling Pathway
Copper homeostasis
FAS pathway and Stress induction of HSP regulation
Signaling of Hepatocyte Growth Factor Receptor
Focal Adhesion
Myometrial Relaxation and Contraction Pathways
Nuclear Receptors Meta-Pathway
Estrogen Receptor Pathway
Aryl Hydrocarbon Receptor Pathway
IL-3 Signaling Pathway
Cytodifferentiation (Part 3 of 3)
Selenium Metabolism and Selenoproteins
Pre-NOTCH Expression and Processing
Fc epsilon receptor (FCERI) signaling
Polycystic Kidney Disease Pathway
Apoptosis
PDGF Pathway
ATM Signaling Pathway
Quercetin and Nf-kB/ AP-1 Induced Cell Apoptosis
BDNF signaling pathway
Integrated Pancreatic Cancer Pathway
AGE/RAGE pathway
TNF alpha Signaling Pathway
B Cell Receptor Signaling Pathway
Prostate Cancer
Arylhydrocarbon receptor (AhR) signaling pathway
TWEAK Signaling Pathway
TSH signaling pathway
RANKL/RANK Signaling Pathway
Integrated Breast Cancer Pathway
IL-1 signaling pathway
MAPK targets/ Nuclear events mediated by MAP kinases
Apoptosis Modulation and Signaling
Physiological and Pathological Hypertrophy of the Heart
Regulation of toll-like receptor signaling pathway
Androgen receptor signaling pathway
IL-5 Signaling Pathway
References
Ref 547484Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016746)
Ref 527964Nat Chem Biol. 2005 Jul;1(2):74-84.Diversity-oriented synthesis: exploring the intersections between chemistry and biology.
Ref 535196AP-1 blockade inhibits the growth of normal and malignant breast cells. Oncogene. 2001 May 17;20(22):2771-80.
Ref 535686Chemogenomic identification of Ref-1/AP-1 as a therapeutic target for asthma. Proc Natl Acad Sci U S A. 2003 Feb 4;100(3):1169-73. Epub 2003 Jan 24.
Ref 550543CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008.

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