Insulin-like growth factor receptor
From Proteopedia
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| - | <StructureSection load=' | + | <StructureSection load='' size='450' side='right' scene='Journal:JBSD:38/Cv/1' caption=''> |
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'''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. | '''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. | ||
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| + | === Memory-Enhancement by Traditional Chinese Medicine? <ref>doi 10.1080/07391102.2012.741052</ref>=== | ||
| + | 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. <scene name='Journal:JBSD:38/Cv/3'>IGF receptor </scene> (IGF-IR, PDB ID: [[3i81]], <font color='darkmagenta'><b>colored in darkmagenta</b></font>) activation is critical for IGF-I to elicit desirable cognitive functions. Traditional Chinese medicine (TCM) ligands <scene name='Journal:JBSD:38/Cv/2'>3-(2-carboxyphenyl)-4(3H)-quinazolinone</scene> (orgin: ''Isatisin digotica'', <span style="color:lime;background-color:black;font-weight:bold;">colored in green</span>), <scene name='Journal:JBSD:38/Cv/4'>(+)-N-methyllaurotetanine</scene> (origin: ''Lindera aggregate'', <span style="color:deeppink;background-color:black;font-weight:bold;">colored in deeppink</span>), and <scene name='Journal:JBSD:38/Cv/5'>(+)-1(R)-Coclaurine</scene> (origin: ''Nelumbonucifera Gaertn'', <span style="color:salmon;background-color:black;font-weight:bold;">colored in salmon</span>) 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. <scene name='Journal:JBSD:38/Cv/7'>3-(2-carboxyphenyl)-4(3H)-quinazolinone</scene> was stabilized by <scene name='Journal:JBSD:38/Cv/8'>Asp1056</scene>, <scene name='Journal:JBSD:38/Cv/9'>(+)-N-methyllaurotetanine</scene> was stabilized by <scene name='Journal:JBSD:38/Cv/10'>Leu975 and Asp1056</scene>, and <scene name='Journal:JBSD:38/Cv/11'>(+)-1(R)-Coclaurine</scene> was stabilized by <scene name='Journal:JBSD:38/Cv/12'>Leu975 and Gly1055</scene> (<span style="color:yellow;background-color:black;font-weight:bold;">key residues are colored in yellow</span>). 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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| + | __NOTOC__ | ||
===3D structures of insulin-like growth factor receptor=== | ===3D structures of insulin-like growth factor receptor=== | ||
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[[1syo]], [[1sz0]] - bIGFR II domains 1-3 + mannose-6-phosphate<BR /> | [[1syo]], [[1sz0]] - bIGFR II domains 1-3 + mannose-6-phosphate<BR /> | ||
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| + | == References == | ||
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| + | <references/> | ||
[[Category:Topic Page]] | [[Category:Topic Page]] | ||
Revision as of 09:31, 20 November 2013
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3D structures of insulin-like growth factor receptor
Updated on 20-November-2013
IGFR 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 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
References
- ↑ 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
