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.
journal_name
Gen Comp Endocrinoljournal_title
General and comparative endocrinologyauthors
Xiong C,Kaczmarek K,Zabrocki J,Pietrantonio PV,Nachman RJdoi
10.1016/j.ygcen.2018.08.002subject
Has Abstractpub_date
2019-07-01 00:00:00pages
58-67eissn
0016-6480issn
1095-6840pii
S0016-6480(18)30324-1journal_volume
278pub_type
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journal_title:General and comparative endocrinology
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journal_title:General and comparative endocrinology
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journal_title:General and comparative endocrinology
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journal_title:General and comparative endocrinology
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journal_title:General and comparative endocrinology
pub_type: 杂志文章
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journal_title:General and comparative endocrinology
pub_type: 杂志文章
doi:10.1016/j.ygcen.2008.09.003
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journal_title:General and comparative endocrinology
pub_type: 杂志文章
doi:10.1016/j.ygcen.2005.02.010
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journal_title:General and comparative endocrinology
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journal_title:General and comparative endocrinology
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journal_title:General and comparative endocrinology
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journal_title:General and comparative endocrinology
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journal_title:General and comparative endocrinology
pub_type: 杂志文章
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journal_title:General and comparative endocrinology
pub_type: 杂志文章,评审
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journal_title:General and comparative endocrinology
pub_type: 杂志文章
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journal_title:General and comparative endocrinology
pub_type: 杂志文章
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更新日期:2015-12-01 00:00:00
abstract::Two types of cDNAs (GTH-I beta and -II beta) that encode the beta subunit of goldfish gonadotropin were cloned from a goldfish pituitary cDNA library. The nucleotide sequence of GTH-I beta cDNA was 616 bp long, encoding 130 amino acids, and that of GTH-II beta was 552 bp long, encoding 140 amino acids. These two types...
journal_title:General and comparative endocrinology
pub_type: 杂志文章
doi:10.1006/gcen.1996.6839
更新日期:1997-03-01 00:00:00
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journal_title:General and comparative endocrinology
pub_type: 杂志文章
doi:10.1016/j.ygcen.2005.05.001
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abstract::The cell types within the endocrine pancreatic tissue and anterior intestine of larvae and juveniles of representatives of the two southern-hemisphere families (Mordaciidae and Geotriidae) were compared, using immunohistochemistry and antisera against insulin (lamprey, bovine), two somatostatins (SST-14, -34), two PP-...
journal_title:General and comparative endocrinology
pub_type: 杂志文章
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