Target Information
Target General Information | Top | |||||
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Target ID |
T02259
(Former ID: TTDI02413)
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Target Name |
Runt-related transcription factor 2 (RUNX2)
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Synonyms |
SL3/AKV core-binding factor alpha A subunit; SL3-3 enhancer factor 1 alpha A subunit; Polyomavirus enhancer-binding protein 2 alpha Asubunit; Polyomavirus enhancer-binding protein 2 alpha A subunit; PEBP2A; PEBP2-alpha A; PEA2-alpha A; Osteoblast-specific transcription factor 2; Oncogene AML-3; OSF2; OSF-2; Core-binding factor subunit alpha-1; CBFA1; CBF-alpha-1; Acute myeloid leukemia 3 protein; AML3
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Gene Name |
RUNX2
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Target Type |
Literature-reported target
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[1] | ||||
Function |
Essential for the maturation of osteoblasts and both intramembranous and endochondral ossification. CBF binds to the core site, 5'-PYGPYGGT-3', of a number of enhancers and promoters, including murine leukemia virus, polyomavirus enhancer, T-cell receptor enhancers, osteocalcin, osteopontin, bone sialoprotein, alpha 1(I) collagen, LCK, IL-3 and GM-CSF promoters. In osteoblasts, supports transcription activation: synergizes with SPEN/MINT to enhance FGFR2-mediated activation of the osteocalcin FGF-responsive element (OCFRE). Inhibits KAT6B-dependent transcriptional activation. Transcription factor involved in osteoblastic differentiation and skeletal morphogenesis.
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UniProt ID | ||||||
Sequence |
MASNSLFSTVTPCQQNFFWDPSTSRRFSPPSSSLQPGKMSDVSPVVAAQQQQQQQQQQQQ
QQQQQQQQQQQEAAAAAAAAAAAAAAAAAVPRLRPPHDNRTMVEIIADHPAELVRTDSPN FLCSVLPSHWRCNKTLPVAFKVVALGEVPDGTVVTVMAGNDENYSAELRNASAVMKNQVA RFNDLRFVGRSGRGKSFTLTITVFTNPPQVATYHRAIKVTVDGPREPRRHRQKLDDSKPS LFSDRLSDLGRIPHPSMRVGVPPQNPRPSLNSAPSPFNPQGQSQITDPRQAQSSPPWSYD QSYPSYLSQMTSPSIHSTTPLSSTRGTGLPAITDVPRRISDDDTATSDFCLWPSTLSKKS QAGASELGPFSDPRQFPSISSLTESRFSNPRMHYPATFTYTPPVTSGMSLGMSATTHYHT YLPPPYPGSSQSQSGPFQTSSTPYLYYGTSSGSYQFPMVPGGDRSPSRMLPPCTTTSNGS TLLNPNLPNQNDGVDADGSHSSSPTVLNSSGRMDESVWRPY Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
ADReCS ID | BADD_A01693 ; BADD_A04839 | |||||
HIT2.0 ID | T91MKC |
Cell-based Target Expression Variations | Top | |||||
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Cell-based Target Expression Variations |
Drug Binding Sites of Target | Top | |||||
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Ligand Name: Plicamycin | Ligand Info | |||||
Structure Description | Crystal structure of the DNA binding domains of human transcription factor ERG, human Runx2 bound to core binding factor beta (Cbfb), and mithramycin, in complex with 16mer DNA CAGAGGATGTGGCTTC | PDB:6VGG | ||||
Method | X-ray diffraction | Resolution | 4.31 Å | Mutation | No | [2] |
PDB Sequence |
AELVRTDSPN
120 FLCSVLPSHW130 RCNKTLPVAF140 KVVALGEVPD150 GTVVTVMAGN160 DENYSAELRN 170 ASAVMKNQVA180 RFNDLRFVGR190 SGRGKSFTLT200 ITVFTNPPQV210 ATYHRAIKVT 220 VDGPREP
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Click to View More Binding Site Information of This Target with Different Ligands |
Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Pathway Affiliation
Biological Network Descriptors
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There is no similarity protein (E value < 0.005) for this target
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KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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Parathyroid hormone synthesis, secretion and action | hsa04928 | Affiliated Target |
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Class: Organismal Systems => Endocrine system | Pathway Hierarchy |
Degree | 37 | Degree centrality | 3.98E-03 | Betweenness centrality | 4.88E-03 |
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Closeness centrality | 2.56E-01 | Radiality | 1.44E+01 | Clustering coefficient | 7.96E-02 |
Neighborhood connectivity | 4.06E+01 | Topological coefficient | 4.77E-02 | Eccentricity | 11 |
Download | Click to Download the Full PPI Network of This Target | ||||
Target Regulators | Top | |||||
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Target-regulating microRNAs | ||||||
Target-interacting Proteins |
References | Top | |||||
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REF 1 | RUNX2 and Osteosarcoma. Anticancer Agents Med Chem. 2015;15(7):881-7. | |||||
REF 2 | Allosteric interference in oncogenic FLI1 and ERG transactions by mithramycins. Structure. 2021 May 6;29(5):404-412.e4. |
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