Target Information
Target General Information | Top | |||||
---|---|---|---|---|---|---|
Target ID |
T69085
(Former ID: TTDC00119)
|
|||||
Target Name |
Transcription factor AP-1 (JUN)
|
|||||
Synonyms |
V-jun avian sarcoma virus 17 oncogene homolog; Proto-oncogene c-jun; P39; C-jun proto-oncogene; Activator protein-1; Activator protein 1; AP1; AP-1 transcription factor
|
|||||
Gene Name |
JUN
|
|||||
Target Type |
Discontinued target
|
[1] | ||||
Disease | [+] 1 Target-related Diseases | + | ||||
1 | Rheumatoid arthritis [ICD-11: FA20] | |||||
Function |
Promotes activity of NR5A1 when phosphorylated by HIPK3 leading to increased steroidogenic gene expression upon cAMP signaling pathway stimulation. Involved in activated KRAS-mediated transcriptional activation of USP28 in colorectal cancer (CRC) cells. Binds to the USP28 promoter in colorectal cancer (CRC) cells. Transcription factor that recognizes and binds to the enhancer heptamer motif 5'-TGA[CG]TCA-3'.
Click to Show/Hide
|
|||||
BioChemical Class |
Basic leucine zipper bZIP
|
|||||
UniProt ID | ||||||
Sequence |
MTAKMETTFYDDALNASFLPSESGPYGYSNPKILKQSMTLNLADPVGSLKPHLRAKNSDL
LTSPDVGLLKLASPELERLIIQSSNGHITTTPTPTQFLCPKNVTDEQEGFAEGFVRALAE LHSQNTLPSVTSAAQPVNGAGMVAPAVASVAGGSGSGGFSASLHSEPPVYANLSNFNPGA LSSGGGAPSYGAAGLAFPAQPQQQQQPPHHLPQQMPVQHPRLQALKEEPQTVPEMPGETP PLSPIDMESQERIKAERKRMRNRIAASKCRKRKLERIARLEEKVKTLKAQNSELASTANM LREQVAQLKQKVMNHVNSGCQLMLTQQLQTF Click to Show/Hide
|
|||||
3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
ADReCS ID | BADD_A02053 ; BADD_A02756 ; BADD_A05675 ; BADD_A06250 ; BADD_A06356 ; BADD_A08298 | |||||
HIT2.0 ID | T26KIE |
Drugs and Modes of Action | Top | |||||
---|---|---|---|---|---|---|
Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
1 | T-5224 | Drug Info | Discontinued in Phase 2 | Rheumatoid arthritis | [2] | |
Mode of Action | [+] 1 Modes of Action | + | ||||
Inhibitor | [+] 4 Inhibitor drugs | + | ||||
1 | T-5224 | Drug Info | [1] | |||
2 | PNRI-299 | Drug Info | [3] | |||
3 | TAM-67 | Drug Info | [4] | |||
4 | TWS-119 | Drug Info | [5] |
Chemical Structure based Activity Landscape of Target | Top |
---|---|
Drug Property Profile of Target | Top | |
---|---|---|
(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
|
||
(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
|
||
(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
|
||
"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Target Poor or Non Binders | Top | |||||
---|---|---|---|---|---|---|
Target Poor or Non Binders |
Target Regulators | Top | |||||
---|---|---|---|---|---|---|
Target-regulating microRNAs | ||||||
Target-regulating Transcription Factors | ||||||
Target-interacting Proteins |
Target Profiles in Patients | Top | |||||
---|---|---|---|---|---|---|
Target Expression Profile (TEP) |
Target-Related Models and Studies | Top | |||||
---|---|---|---|---|---|---|
Target Validation |
References | Top | |||||
---|---|---|---|---|---|---|
REF 1 | CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008. | |||||
REF 2 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016746) | |||||
REF 3 | Chemogenomic 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. | |||||
REF 4 | AP-1 blockade inhibits the growth of normal and malignant breast cells. Oncogene. 2001 May 17;20(22):2771-80. | |||||
REF 5 | Diversity-oriented synthesis: exploring the intersections between chemistry and biology. Nat Chem Biol. 2005 Jul;1(2):74-84. |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.