FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2752273098> ?p ?o ?g. }

• W2752273098 endingPage "17112" @default.
• W2752273098 startingPage "17101" @default.
• W2752273098 abstract "Conotoxin GeXIVA inhibits the α9α10 nicotinic acetylcholine receptor (nAChR) and is analgesic in animal models of pain. α-Conotoxins have four cysteines that can have three possible disulfide connectivities: globular (CysI–CysIII and CysII–CysIV), ribbon (CysI–CysIV and CysII–CysIII), or bead (CysI–CysII and CysIII–CysIV). Native α-conotoxins preferably adopt the globular connectivity, and previous studies of α-conotoxins have focused on the globular isomers as the ribbon and bead isomers typically have lower potency at nAChRs than the globular form. A recent report showed that the bead and ribbon isomers of GeXIVA are more potent than the globular isomer, with low nanomolar half-maximal inhibitory concentrations (IC50). Despite this high potency, the therapeutic potential of GeXIVA is limited, because like most peptides, it is susceptible to proteolytic degradation and is challenging to synthesize in high yield. Here we used backbone cyclization as a strategy to improve the folding yield as well as increase the serum stability of ribbon GeXIVA while preserving activity at the α9α10 nAChR. Specifically, cyclization of ribbon GeXIVA with a two-residue linker maintained the biological activity at the human α9α10 nAChR and improved stability in human serum. Short linkers led to selective formation of the ribbon disulfide isomer without requiring orthogonal protection. Overall, this study highlights the value of backbone cyclization in directing folding, improving yields, and stabilizing conotoxins with therapeutic potential." @default.
• W2752273098 created "2017-09-15" @default.
• W2752273098 creator A5014444837 @default.
• W2752273098 creator A5015410355 @default.
• W2752273098 creator A5023919017 @default.
• W2752273098 creator A5025386235 @default.
• W2752273098 creator A5040937753 @default.
• W2752273098 creator A5048792248 @default.
• W2752273098 creator A5063128380 @default.
• W2752273098 creator A5079308758 @default.
• W2752273098 date "2017-10-01" @default.
• W2752273098 modified "2023-10-12" @default.
• W2752273098 title "Backbone cyclization of analgesic conotoxin GeXIVA facilitates direct folding of the ribbon isomer" @default.
• W2752273098 cites W1491301840 @default.
• W2752273098 cites W1515799994 @default.
• W2752273098 cites W1581758663 @default.
• W2752273098 cites W1824721868 @default.
• W2752273098 cites W1860382351 @default.
• W2752273098 cites W1889703234 @default.
• W2752273098 cites W1932102690 @default.
• W2752273098 cites W1964673525 @default.
• W2752273098 cites W1967903536 @default.
• W2752273098 cites W1970898345 @default.
• W2752273098 cites W1974043792 @default.
• W2752273098 cites W1974175820 @default.
• W2752273098 cites W1975383593 @default.
• W2752273098 cites W1976233924 @default.
• W2752273098 cites W1983093761 @default.
• W2752273098 cites W1986070483 @default.
• W2752273098 cites W1986397265 @default.
• W2752273098 cites W1992242607 @default.
• W2752273098 cites W1992556352 @default.
• W2752273098 cites W1992696950 @default.
• W2752273098 cites W1994656998 @default.
• W2752273098 cites W1995390287 @default.
• W2752273098 cites W1997843197 @default.
• W2752273098 cites W2009809547 @default.
• W2752273098 cites W2011253696 @default.
• W2752273098 cites W201400539 @default.
• W2752273098 cites W2015211105 @default.
• W2752273098 cites W2015769091 @default.
• W2752273098 cites W2019025856 @default.
• W2752273098 cites W2020708235 @default.
• W2752273098 cites W2021190011 @default.
• W2752273098 cites W2028533826 @default.
• W2752273098 cites W2028638910 @default.
• W2752273098 cites W2030622814 @default.
• W2752273098 cites W2040106038 @default.
• W2752273098 cites W2044342670 @default.
• W2752273098 cites W2049885807 @default.
• W2752273098 cites W2052956415 @default.
• W2752273098 cites W2057492677 @default.
• W2752273098 cites W2065283382 @default.
• W2752273098 cites W2075127809 @default.
• W2752273098 cites W2079145821 @default.
• W2752273098 cites W2085269882 @default.
• W2752273098 cites W2088848851 @default.
• W2752273098 cites W2092424786 @default.
• W2752273098 cites W2094310013 @default.
• W2752273098 cites W2098879522 @default.
• W2752273098 cites W2104838343 @default.
• W2752273098 cites W2112418305 @default.
• W2752273098 cites W2113369993 @default.
• W2752273098 cites W2119873953 @default.
• W2752273098 cites W2127525984 @default.
• W2752273098 cites W2128779418 @default.
• W2752273098 cites W2134261418 @default.
• W2752273098 cites W2134571618 @default.
• W2752273098 cites W2147285542 @default.
• W2752273098 cites W2154714625 @default.
• W2752273098 cites W2156900111 @default.
• W2752273098 cites W2160386479 @default.
• W2752273098 cites W2162291204 @default.
• W2752273098 cites W2163545771 @default.
• W2752273098 cites W2170725577 @default.
• W2752273098 cites W2205164763 @default.
• W2752273098 cites W2207824372 @default.
• W2752273098 cites W2280118389 @default.
• W2752273098 cites W2295245722 @default.
• W2752273098 cites W2312248593 @default.
• W2752273098 cites W2327873630 @default.
• W2752273098 cites W2343381229 @default.
• W2752273098 cites W2417255443 @default.
• W2752273098 cites W2460876812 @default.
• W2752273098 cites W2474591621 @default.
• W2752273098 cites W4211119836 @default.
• W2752273098 cites W4249037006 @default.
• W2752273098 cites W4323517667 @default.
• W2752273098 doi "https://doi.org/10.1074/jbc.m117.808386" @default.
• W2752273098 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/5641895" @default.
• W2752273098 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/28851841" @default.
• W2752273098 hasPublicationYear "2017" @default.
• W2752273098 type Work @default.
• W2752273098 sameAs 2752273098 @default.
• W2752273098 citedByCount "13" @default.
• W2752273098 countsByYear W27522730982018 @default.
• W2752273098 countsByYear W27522730982019 @default.
• W2752273098 countsByYear W27522730982020 @default.

• next