Insulin-like growth factor receptor
Insulin-like growth factor receptors (IGFR) are transmembrane receptors which are stimulated by insulin-like growth factors (IGF). IGFR contains 2 extracellular α chains and 2 transmembranal β chains. Upon binding of IGF, a tyrosine in the β chain becomes autophosphorylated and triggers a cascade of intracellular signaling. Memory-Enhancement by Traditional Chinese Medicine? [1]Cognitive impairment is an emerging issue and increasing research points to the significant role of insulin-like growth factor I (IGF-I) in cognitive brain functions. (IGF-IR, PDB ID: 3i81, colored in darkmagenta) activation is critical for IGF-I to elicit desirable cognitive functions. Traditional Chinese medicine (TCM) ligands (orgin: Isatisin digotica, colored in green), (origin: Lindera aggregate, colored in deeppink), and (origin: Nelumbonucifera Gaertn, colored in salmon) showed high binding affinity towards IGF-IR at the binding site defined by the control in PDB ID: 3i81. Molecular dynamics simulation revealed that the TCM ligands were secured at the opening of the IGF-IR binding site for the duration of the MD. was stabilized by , was stabilized by , and was stabilized by (key residues are colored in yellow). Four different quantitative-structure activity relationship models consistently predicted bioactivity of the TCM ligands towards IGF-IR. In summary, the TCM candidates exhibit drug-like potential in both structural-based and ligand-based properties and may have potential for further applications in enhancing cognition. |
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3D structures of insulin-like growth factor receptor3D structures of insulin-like growth factor receptor
Updated on 18-March-2014
IGFR IIGFR I
1igr – hIGFR I domains 1-3 – human
1jqh, 1p4o - hIGFR I kinase domain (mutant)
1m7n - hIGFR I kinase domain
1k3a - hIGFR I kinase domain + insulin receptor substrate peptide
2oj9, 2zm3, 3d94, 3f5p, 3i81, 3lvp, 3nw5, 3nw6, 3nw7, 3lw0, 3qqu, 3o23 - hIGFR I kinase domain + inhibitor
IGFR IIIGFR II
1gqb - hIGFR II
2kva - hIGFR II domain 5 – NMR
2cnj - hIGFR II domain 11 - NMR
2l2a - hIGFR II domains 11 (mutant) - NMR
2kvb - hIGFR II domain 5 + inhibitor – NMR
2v5n - hIGFR II domains 11-12
2v5o - hIGFR II domains 11-14
2v5p - hIGFR II domains 11-13 + IGF II
2l29 - hIGFR II domain 11 + IGF II - NMR
1gp0, 1gp3, 1e6f - hIGFR II IGF II-binding domain
1q25 - bIGFR II domains 1-3 – bovine
1syo, 1sz0 - bIGFR II domains 1-3 + mannose-6-phosphate
2lla - IGFR II domain 11 – short-beaked echidna - NMR
ReferencesReferences
- ↑ Hung IC, Chang SS, Chang PC, Lee CC, Chen CY. Memory enhancement by traditional Chinese medicine? J Biomol Struct Dyn. 2012 Dec 19. PMID:23249175 doi:10.1080/07391102.2012.741052