Matches in SemOpenAlex for { <https://semopenalex.org/work/W2005017658> ?p ?o ?g. }
- W2005017658 endingPage "593" @default.
- W2005017658 startingPage "579" @default.
- W2005017658 abstract "The bombesin (Bn) receptor family includes the gastrin-releasing peptide (GRPR) and neuromedin B (NMBR) receptors, Bn receptor subtype 3 (BRS-3) and Bn receptor subtype 4 (BB(4)). They share 50% homology, yet their affinities for gastrin-releasing peptide (GRP) differ. The determinants of GRP high affinity for GRPR and BB(4), and low affinity for BRS-3 are largely unknown. To address this question we made an analysis of structural homologies in Bn receptor members correlated with their affinities for GRP to develop criteria to identify amino acids important for GRP selectivity. Fourteen differences were identified and each was mutated singly in GRPR to that found in hBRS-3. Eleven mutants had a loss of GRP affinity. Furthermore, three of four amino acids in the GRPR selected used a similar approach and previously reported to be important for high affinity Bn binding, were important for GRP affinity. Some GRPR mutants containing combinations of these mutations had greater decreases in GRP affinity than any single mutation. Particularly important for GRP selectivity were K101, Q121, A198, P199, S293, R288, T297 in GRPR. These results were confirmed by making the reverse mutations in BRS-3 to make GRP gain of affinity mutants. Modeling studies demonstrated a number of the important amino acids had side-chains oriented inward and within 6A of the binding pocket. These results demonstrated this approach could identify amino acids needed for GRP affinity and complemented results from chimera/mutagenesis studies by identifying which differences in the extracellular domains of Bn receptors were important for GRP affinity." @default.
- W2005017658 created "2016-06-24" @default.
- W2005017658 creator A5000480842 @default.
- W2005017658 creator A5005161415 @default.
- W2005017658 creator A5015646615 @default.
- W2005017658 creator A5018253779 @default.
- W2005017658 creator A5021831733 @default.
- W2005017658 creator A5069852269 @default.
- W2005017658 creator A5073688431 @default.
- W2005017658 creator A5089930328 @default.
- W2005017658 creator A5090559830 @default.
- W2005017658 date "2005-02-01" @default.
- W2005017658 modified "2023-10-18" @default.
- W2005017658 title "Identification of key amino acids in the gastrin-releasing peptide receptor (GRPR) responsible for high affinity binding of gastrin-releasing peptide (GRP)" @default.
- W2005017658 cites W1537449868 @default.
- W2005017658 cites W1541400111 @default.
- W2005017658 cites W1556149078 @default.
- W2005017658 cites W1573917099 @default.
- W2005017658 cites W1580662746 @default.
- W2005017658 cites W1921735617 @default.
- W2005017658 cites W1924799369 @default.
- W2005017658 cites W1966937360 @default.
- W2005017658 cites W1967534234 @default.
- W2005017658 cites W1967591064 @default.
- W2005017658 cites W1968585499 @default.
- W2005017658 cites W1974390948 @default.
- W2005017658 cites W1974777098 @default.
- W2005017658 cites W1996955964 @default.
- W2005017658 cites W2005688520 @default.
- W2005017658 cites W2015179997 @default.
- W2005017658 cites W2015642465 @default.
- W2005017658 cites W2015939711 @default.
- W2005017658 cites W2023660643 @default.
- W2005017658 cites W2027699869 @default.
- W2005017658 cites W2029982856 @default.
- W2005017658 cites W2035979242 @default.
- W2005017658 cites W2043343372 @default.
- W2005017658 cites W2045394542 @default.
- W2005017658 cites W2046459625 @default.
- W2005017658 cites W2047349833 @default.
- W2005017658 cites W2049782036 @default.
- W2005017658 cites W2052973557 @default.
- W2005017658 cites W2053174683 @default.
- W2005017658 cites W2063844010 @default.
- W2005017658 cites W2072064360 @default.
- W2005017658 cites W2073008732 @default.
- W2005017658 cites W2075033703 @default.
- W2005017658 cites W2077808319 @default.
- W2005017658 cites W2078535400 @default.
- W2005017658 cites W2080049180 @default.
- W2005017658 cites W2082344712 @default.
- W2005017658 cites W2090457292 @default.
- W2005017658 cites W2093732282 @default.
- W2005017658 cites W2094031081 @default.
- W2005017658 cites W2114082871 @default.
- W2005017658 cites W2137848795 @default.
- W2005017658 cites W2139996880 @default.
- W2005017658 cites W2149963584 @default.
- W2005017658 cites W2155524113 @default.
- W2005017658 cites W2155694817 @default.
- W2005017658 cites W2157681798 @default.
- W2005017658 cites W2167549601 @default.
- W2005017658 cites W2189598040 @default.
- W2005017658 cites W2190031288 @default.
- W2005017658 cites W4244479781 @default.
- W2005017658 doi "https://doi.org/10.1016/j.bcp.2004.11.003" @default.
- W2005017658 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/15670577" @default.
- W2005017658 hasPublicationYear "2005" @default.
- W2005017658 type Work @default.
- W2005017658 sameAs 2005017658 @default.
- W2005017658 citedByCount "22" @default.
- W2005017658 countsByYear W20050176582012 @default.
- W2005017658 countsByYear W20050176582013 @default.
- W2005017658 countsByYear W20050176582014 @default.
- W2005017658 countsByYear W20050176582016 @default.
- W2005017658 countsByYear W20050176582019 @default.
- W2005017658 countsByYear W20050176582020 @default.
- W2005017658 countsByYear W20050176582021 @default.
- W2005017658 countsByYear W20050176582022 @default.
- W2005017658 countsByYear W20050176582023 @default.
- W2005017658 crossrefType "journal-article" @default.
- W2005017658 hasAuthorship W2005017658A5000480842 @default.
- W2005017658 hasAuthorship W2005017658A5005161415 @default.
- W2005017658 hasAuthorship W2005017658A5015646615 @default.
- W2005017658 hasAuthorship W2005017658A5018253779 @default.
- W2005017658 hasAuthorship W2005017658A5021831733 @default.
- W2005017658 hasAuthorship W2005017658A5069852269 @default.
- W2005017658 hasAuthorship W2005017658A5073688431 @default.
- W2005017658 hasAuthorship W2005017658A5089930328 @default.
- W2005017658 hasAuthorship W2005017658A5090559830 @default.
- W2005017658 hasConcept C104317684 @default.
- W2005017658 hasConcept C118303440 @default.
- W2005017658 hasConcept C143065580 @default.
- W2005017658 hasConcept C16318435 @default.
- W2005017658 hasConcept C170493617 @default.
- W2005017658 hasConcept C185592680 @default.
- W2005017658 hasConcept C2776998989 @default.
- W2005017658 hasConcept C2778448772 @default.