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• W2078902341 endingPage "948" @default.
• W2078902341 startingPage "936" @default.
• W2078902341 abstract "There is increased interest in the Bn-receptor family because they are frequently over/ectopically expressed by tumors and thus useful as targets for imaging or receptor-targeted-cytotoxicity. The synthetic Bn-analog, [D-Tyr(6), β-Ala(11), Phe(13), Nle(14)]Bn(6-14) [Univ.Lig] has the unique property of having high affinity for all three human BNRs (GRPR, NMBR, BRS-3), and thus could be especially useful for this approach. However, the molecular basis of this property is unclear and is the subject of this study. To accomplish this, site-directed mutagenesis was used after identifying potentially important amino acids using sequence homology analysis of all BnRs with high affinity for Univ.Lig compared to the Cholecystokinin-receptor (CCK(A)R), which has low affinity. Using various criteria 74 amino acids were identified and 101 mutations made in GRPR by changing each to those of CCK(A)R or to alanine. 22 GRPR mutations showed a significant decrease in affinity for Univ.Lig (>2-fold) with 2 in EC2[D97N, G112V], 1 in UTM6[Y284A], 2 in EC4[R287N, H300S] showing >10-fold decrease in Univ.Lig affinity. Additional mutations were made to explore the molecular basis for these changes. Our results show that high affinity for Univ.Lig by human Bn-receptors requires positively charged amino acids in extracellular (EC)-domain 4 and to a lesser extent EC2 and EC3 suggesting charge-charge interactions may be particularly important for determining the general high affinity of this ligand. Furthermore, transmembrane amino acids particularly in UTM6 are important contributing both charge-charge interactions as well as interaction with a tyrosine residue in close proximity suggesting possible receptor-peptide cation-π or H-bonding interactions are also important for determining its high affinity." @default.
• W2078902341 created "2016-06-24" @default.
• W2078902341 creator A5000480842 @default.
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• W2078902341 creator A5090559830 @default.
• W2078902341 date "2012-10-01" @default.
• W2078902341 modified "2023-09-30" @default.
• W2078902341 title "The molecular basis for high affinity of a universal ligand for human bombesin receptor (BnR) family members" @default.
• W2078902341 cites W104793819 @default.
• W2078902341 cites W1537449868 @default.
• W2078902341 cites W1540718768 @default.
• W2078902341 cites W1545856647 @default.
• W2078902341 cites W1548350321 @default.
• W2078902341 cites W1553706088 @default.
• W2078902341 cites W1573917099 @default.
• W2078902341 cites W1580662746 @default.
• W2078902341 cites W1607867087 @default.
• W2078902341 cites W1836431516 @default.
• W2078902341 cites W1903466722 @default.
• W2078902341 cites W1951669519 @default.
• W2078902341 cites W1968585499 @default.
• W2078902341 cites W1973596141 @default.
• W2078902341 cites W1974390948 @default.
• W2078902341 cites W1978349701 @default.
• W2078902341 cites W1981770260 @default.
• W2078902341 cites W1994147646 @default.
• W2078902341 cites W1996012668 @default.
• W2078902341 cites W1997527683 @default.
• W2078902341 cites W2001180937 @default.
• W2078902341 cites W2003266876 @default.
• W2078902341 cites W2005017658 @default.
• W2078902341 cites W2005688520 @default.
• W2078902341 cites W2014580615 @default.
• W2078902341 cites W2015642465 @default.
• W2078902341 cites W2021243510 @default.
• W2078902341 cites W2023063407 @default.
• W2078902341 cites W2026184136 @default.
• W2078902341 cites W2027699869 @default.
• W2078902341 cites W2029982856 @default.
• W2078902341 cites W2035167131 @default.
• W2078902341 cites W2048167560 @default.
• W2078902341 cites W2048962471 @default.
• W2078902341 cites W2049782036 @default.
• W2078902341 cites W2053627817 @default.
• W2078902341 cites W2054525948 @default.
• W2078902341 cites W2057139574 @default.
• W2078902341 cites W2062293719 @default.
• W2078902341 cites W2067219399 @default.
• W2078902341 cites W2072064360 @default.
• W2078902341 cites W2073008732 @default.
• W2078902341 cites W2074256753 @default.
• W2078902341 cites W2075033703 @default.
• W2078902341 cites W2075830220 @default.
• W2078902341 cites W2078535400 @default.
• W2078902341 cites W2079604571 @default.
• W2078902341 cites W2082344712 @default.
• W2078902341 cites W2083905313 @default.
• W2078902341 cites W2084840139 @default.
• W2078902341 cites W2086990011 @default.
• W2078902341 cites W2088080090 @default.
• W2078902341 cites W2088771797 @default.
• W2078902341 cites W2090457292 @default.
• W2078902341 cites W2090854342 @default.
• W2078902341 cites W2107282691 @default.
• W2078902341 cites W2111563843 @default.
• W2078902341 cites W2114082871 @default.
• W2078902341 cites W2119392173 @default.
• W2078902341 cites W2120137104 @default.
• W2078902341 cites W2122147571 @default.
• W2078902341 cites W2127739127 @default.
• W2078902341 cites W2137848795 @default.
• W2078902341 cites W2137852913 @default.
• W2078902341 cites W2145661651 @default.
• W2078902341 cites W2148559897 @default.
• W2078902341 cites W2148617171 @default.
• W2078902341 cites W2148624282 @default.
• W2078902341 cites W2152791137 @default.
• W2078902341 cites W2189201950 @default.
• W2078902341 cites W2189598040 @default.
• W2078902341 cites W2333970776 @default.
• W2078902341 cites W2342367813 @default.
• W2078902341 cites W2409997741 @default.
• W2078902341 cites W2418900977 @default.
• W2078902341 cites W2431380225 @default.
• W2078902341 cites W2435274822 @default.
• W2078902341 cites W4244479781 @default.
• W2078902341 doi "https://doi.org/10.1016/j.bcp.2012.07.010" @default.
• W2078902341 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3433740" @default.
• W2078902341 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/22828605" @default.
• W2078902341 hasPublicationYear "2012" @default.
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