FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2886033858> ?p ?o ?g. }

• W2886033858 endingPage "67" @default.
• W2886033858 startingPage "58" @default.
• W2886033858 abstract "Insect kinins modulate aspects of diuresis, digestion, development, and sugar taste perception in tarsi and labellar sensilla in mosquitoes. They are, however, subject to rapid biological degradation by endogenous invertebrate peptidases. A series of α-aminoisobutyric (Aib) acid-containing insect kinin analogs incorporating sequences native to the Aedes aegypti mosquito aedeskinins were evaluated on two recombinant kinin invertebrate receptors stably expressed in cell lines, discovering a number of highly potent and biostable insect kinin mimics. On the Ae. aegypti mosquito kinin receptor, three highly potent, biostable Aib analogs matched the activity of the Aib-containing biostable insect kinin analog 1728, which previously showed disruptive and/or aversive activity in aphid, mosquito and kissing bug. These three analogs are IK-Aib-19 ([Aib]FY[Aib]WGa, EC50 = 18 nM), IK-Aib-12 (pQKFY[Aib]WGa, EC50 = 23 nM) and IK-Aib-20 ([Aib]FH[Aib]WGa, EC50 = 28 nM). On the Rhipicephalus (Boophilus) microplus tick receptor, IK-Aib-20 ([Aib]FH[Aib]WGa, EC50 = 2 nM) is more potent than 1728 by a factor of 3. Seven other potentially biostable analogs exhibited an EC50 range of 5–10 nM, all of which match the potency of 1728. Among the multi-Aib hexapeptide kinin analogs tested the tick receptor has a preference for the positively-charged, aromatic H over the aromatic residues Y and F in the X1 variable position ([Aib]FX1[Aib]WGa), whereas the mosquito receptor does not distinguish between them. In contrast, in a mono-Aib pentapeptide analog framework (FX1[Aib]WGa), both receptors exhibit a preference for Y over H in the variable position. Among analogs incorporating polyethylene glycol (PEG) polymer attachments at the N-terminus that can confer enhanced bioavailability and biostability, three matched or surpassed the potency of a positive control peptide. On the tick receptor IK-PEG-9 (P8-R[Aib]FF[Aib]WGa) was the most potent. Two others, IK-PEG-8 (P8-RFFPWGa) and IK-PEG-6 (P4-RFFPWGa), were most potent on the mosquito receptor, with the first surpassing the activity of the positive control peptide. These analogs and others in the IK-Aib series expand the toolbox of potent analogs accessible to invertebrate endocrinologists studying the structural requirements for bioactivity and the as yet unknown role of the insect kinins in ticks. They may contribute to the development of selective, environmentally friendly pest arthropod control agents." @default.
• W2886033858 created "2018-08-22" @default.
• W2886033858 creator A5031752704 @default.
• W2886033858 creator A5033725536 @default.
• W2886033858 creator A5042422062 @default.
• W2886033858 creator A5061213234 @default.
• W2886033858 creator A5087146368 @default.
• W2886033858 date "2019-07-01" @default.
• W2886033858 modified "2023-09-27" @default.
• W2886033858 title "Evaluation of Aib and PEG-polymer insect kinin analogs on mosquito and tick GPCRs identifies potent new pest management tools with potentially enhanced biostability and bioavailability" @default.
• W2886033858 cites W1521815313 @default.
• W2886033858 cites W1922119015 @default.
• W2886033858 cites W1970793109 @default.
• W2886033858 cites W1971081299 @default.
• W2886033858 cites W1972255915 @default.
• W2886033858 cites W1985046771 @default.
• W2886033858 cites W1985409672 @default.
• W2886033858 cites W1993243416 @default.
• W2886033858 cites W1997371351 @default.
• W2886033858 cites W1998957810 @default.
• W2886033858 cites W2000864903 @default.
• W2886033858 cites W2030026428 @default.
• W2886033858 cites W2048873687 @default.
• W2886033858 cites W2051319674 @default.
• W2886033858 cites W2056393701 @default.
• W2886033858 cites W2057681109 @default.
• W2886033858 cites W2059289447 @default.
• W2886033858 cites W2067923085 @default.
• W2886033858 cites W2078779436 @default.
• W2886033858 cites W2083652994 @default.
• W2886033858 cites W2085345221 @default.
• W2886033858 cites W2104835532 @default.
• W2886033858 cites W210754388 @default.
• W2886033858 cites W2135519314 @default.
• W2886033858 cites W2136844377 @default.
• W2886033858 cites W2137266759 @default.
• W2886033858 cites W2139626288 @default.
• W2886033858 cites W2146910069 @default.
• W2886033858 cites W2147634623 @default.
• W2886033858 cites W2152989766 @default.
• W2886033858 cites W2417700665 @default.
• W2886033858 cites W2792841892 @default.
• W2886033858 cites W4250704915 @default.
• W2886033858 doi "https://doi.org/10.1016/j.ygcen.2018.08.002" @default.
• W2886033858 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30107140" @default.
• W2886033858 hasPublicationYear "2019" @default.
• W2886033858 type Work @default.
• W2886033858 sameAs 2886033858 @default.
• W2886033858 citedByCount "7" @default.
• W2886033858 countsByYear W28860338582019 @default.
• W2886033858 countsByYear W28860338582020 @default.
• W2886033858 countsByYear W28860338582021 @default.
• W2886033858 crossrefType "journal-article" @default.
• W2886033858 hasAuthorship W2886033858A5031752704 @default.
• W2886033858 hasAuthorship W2886033858A5033725536 @default.
• W2886033858 hasAuthorship W2886033858A5042422062 @default.
• W2886033858 hasAuthorship W2886033858A5061213234 @default.
• W2886033858 hasAuthorship W2886033858A5087146368 @default.
• W2886033858 hasBestOaLocation W28860338581 @default.
• W2886033858 hasConcept C170493617 @default.
• W2886033858 hasConcept C173758957 @default.
• W2886033858 hasConcept C2776246183 @default.
• W2886033858 hasConcept C2777775583 @default.
• W2886033858 hasConcept C2779591629 @default.
• W2886033858 hasConcept C55493867 @default.
• W2886033858 hasConcept C59822182 @default.
• W2886033858 hasConcept C86803240 @default.
• W2886033858 hasConcept C98274493 @default.
• W2886033858 hasConceptScore W2886033858C170493617 @default.
• W2886033858 hasConceptScore W2886033858C173758957 @default.
• W2886033858 hasConceptScore W2886033858C2776246183 @default.
• W2886033858 hasConceptScore W2886033858C2777775583 @default.
• W2886033858 hasConceptScore W2886033858C2779591629 @default.
• W2886033858 hasConceptScore W2886033858C55493867 @default.
• W2886033858 hasConceptScore W2886033858C59822182 @default.
• W2886033858 hasConceptScore W2886033858C86803240 @default.
• W2886033858 hasConceptScore W2886033858C98274493 @default.
• W2886033858 hasFunder F4320306114 @default.
• W2886033858 hasLocation W28860338581 @default.
• W2886033858 hasLocation W28860338582 @default.
• W2886033858 hasOpenAccess W2886033858 @default.
• W2886033858 hasPrimaryLocation W28860338581 @default.
• W2886033858 hasRelatedWork W1972212321 @default.
• W2886033858 hasRelatedWork W1982434144 @default.
• W2886033858 hasRelatedWork W2030881267 @default.
• W2886033858 hasRelatedWork W2038665504 @default.
• W2886033858 hasRelatedWork W2248045933 @default.
• W2886033858 hasRelatedWork W2318162828 @default.
• W2886033858 hasRelatedWork W2319664552 @default.
• W2886033858 hasRelatedWork W2528798348 @default.
• W2886033858 hasRelatedWork W3130200169 @default.
• W2886033858 hasRelatedWork W4230390215 @default.
• W2886033858 hasVolume "278" @default.
• W2886033858 isParatext "false" @default.
• W2886033858 isRetracted "false" @default.
• W2886033858 magId "2886033858" @default.
• W2886033858 workType "article" @default.