FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2025383208> ?p ?o ?g. }

• W2025383208 endingPage "795" @default.
• W2025383208 startingPage "788" @default.
• W2025383208 abstract "There is some evidence to suggest that inducible kinin B1 receptors (B1R) may play beneficial and protecting roles in cardiovascular-related pathologies such as hypertension, diabetes, and ischemic organ diseases. Peptide B1R agonists bearing optimized pharmacological features (high potency, selectivity and stability toward proteolysis) hold promise as valuable therapeutic agents in the treatment of these diseases. In the present study, we used solid-phase methodology to synthesize a series of novel peptide analogues based on the sequence of Sar[dPhe8]desArg9-bradykinin, a relatively stable peptide agonist with moderate affinity for the human B1R. We evaluated the pharmacological properties of these peptides using (1) in vitro competitive binding experiments on recombinant human B1R and B2R (for index of selectivity determination) in transiently transfected human embryonic kidney 293 cells (HEK-293T cells), (2) ex vivo vasomotor assays on isolated human umbilical veins expressing endogenous human B1R, and (3) in vivo blood pressure tests using anesthetized lipopolysaccharide-immunostimulated rabbits. Key chemical modifications at the N-terminus, the positions 3 and 5 on Sar[dPhe8]desArg9-bradykinin led to potent analogues. For example, peptides 18 (SarLys[Hyp3,Cha5, dPhe8]desArg9-bradykinin) and 20 (SarLys[Hyp3,Igl5, dPhe8]desArg9-bradykinin) outperformed the parental molecule in terms of affinity, functional potency and duration of action in vitro and in vivo. These selective agonists should be valuable in future animal and human studies to investigate the potential benefits of B1R activation." @default.
• W2025383208 created "2016-06-24" @default.
• W2025383208 creator A5013008851 @default.
• W2025383208 creator A5041000550 @default.
• W2025383208 creator A5042349914 @default.
• W2025383208 creator A5047901224 @default.
• W2025383208 creator A5054475023 @default.
• W2025383208 creator A5065437733 @default.
• W2025383208 creator A5070536251 @default.
• W2025383208 creator A5075346906 @default.
• W2025383208 creator A5079454902 @default.
• W2025383208 date "2009-04-01" @default.
• W2025383208 modified "2023-10-18" @default.
• W2025383208 title "Novel kinin B1 receptor agonists with improved pharmacological profiles" @default.
• W2025383208 cites W1505408758 @default.
• W2025383208 cites W1777223861 @default.
• W2025383208 cites W1889139395 @default.
• W2025383208 cites W1970222518 @default.
• W2025383208 cites W1980861089 @default.
• W2025383208 cites W1983360201 @default.
• W2025383208 cites W1988659390 @default.
• W2025383208 cites W1988725357 @default.
• W2025383208 cites W1993757656 @default.
• W2025383208 cites W1998381401 @default.
• W2025383208 cites W2000605942 @default.
• W2025383208 cites W2001180937 @default.
• W2025383208 cites W2001639445 @default.
• W2025383208 cites W2001854026 @default.
• W2025383208 cites W2021460711 @default.
• W2025383208 cites W2026368662 @default.
• W2025383208 cites W2026514186 @default.
• W2025383208 cites W2028746669 @default.
• W2025383208 cites W2028799468 @default.
• W2025383208 cites W2030039568 @default.
• W2025383208 cites W2032895641 @default.
• W2025383208 cites W2033691230 @default.
• W2025383208 cites W2034292992 @default.
• W2025383208 cites W2043077654 @default.
• W2025383208 cites W2053635170 @default.
• W2025383208 cites W2060860123 @default.
• W2025383208 cites W2067753910 @default.
• W2025383208 cites W2073108733 @default.
• W2025383208 cites W2075209136 @default.
• W2025383208 cites W2080260121 @default.
• W2025383208 cites W2080549818 @default.
• W2025383208 cites W2084552526 @default.
• W2025383208 cites W2084713066 @default.
• W2025383208 cites W2087868822 @default.
• W2025383208 cites W2088800801 @default.
• W2025383208 cites W2089582460 @default.
• W2025383208 cites W2091977844 @default.
• W2025383208 cites W2093198207 @default.
• W2025383208 cites W2100512546 @default.
• W2025383208 cites W2107898589 @default.
• W2025383208 cites W2112133857 @default.
• W2025383208 cites W2115565372 @default.
• W2025383208 cites W2119748083 @default.
• W2025383208 cites W2121044482 @default.
• W2025383208 cites W2123814639 @default.
• W2025383208 cites W2125483282 @default.
• W2025383208 cites W2128652266 @default.
• W2025383208 cites W2135756973 @default.
• W2025383208 cites W2144018405 @default.
• W2025383208 cites W2150446284 @default.
• W2025383208 cites W2152839247 @default.
• W2025383208 cites W2169526581 @default.
• W2025383208 cites W2220177972 @default.
• W2025383208 cites W2332391599 @default.
• W2025383208 cites W4238197563 @default.
• W2025383208 cites W4253097613 @default.
• W2025383208 doi "https://doi.org/10.1016/j.peptides.2008.12.018" @default.
• W2025383208 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/19150636" @default.
• W2025383208 hasPublicationYear "2009" @default.
• W2025383208 type Work @default.
• W2025383208 sameAs 2025383208 @default.
• W2025383208 citedByCount "24" @default.
• W2025383208 countsByYear W20253832082012 @default.
• W2025383208 countsByYear W20253832082013 @default.
• W2025383208 countsByYear W20253832082014 @default.
• W2025383208 countsByYear W20253832082015 @default.
• W2025383208 countsByYear W20253832082016 @default.
• W2025383208 countsByYear W20253832082017 @default.
• W2025383208 countsByYear W20253832082018 @default.
• W2025383208 countsByYear W20253832082019 @default.
• W2025383208 countsByYear W20253832082020 @default.
• W2025383208 countsByYear W20253832082021 @default.
• W2025383208 countsByYear W20253832082022 @default.
• W2025383208 crossrefType "journal-article" @default.
• W2025383208 hasAuthorship W2025383208A5013008851 @default.
• W2025383208 hasAuthorship W2025383208A5041000550 @default.
• W2025383208 hasAuthorship W2025383208A5042349914 @default.
• W2025383208 hasAuthorship W2025383208A5047901224 @default.
• W2025383208 hasAuthorship W2025383208A5054475023 @default.
• W2025383208 hasAuthorship W2025383208A5065437733 @default.
• W2025383208 hasAuthorship W2025383208A5070536251 @default.
• W2025383208 hasAuthorship W2025383208A5075346906 @default.
• W2025383208 hasAuthorship W2025383208A5079454902 @default.
• W2025383208 hasConcept C150903083 @default.

• next