Locmi-AKH-I, cycloAKH (cyclo[LNFTPNWG]
![Locmi-AKH-I, cycloAKH (cyclo[LNFTPNWG]](https://cpcscientific.com/wp-content/uploads/2022/05/cyclo-LNFTPNWG-v2-1500sm.png "cyclo-LNFTPNWG-v2-1500sm")
Abstract
Arteriolar vasodilation and the resultant increase in blood flow are characteristic vascular responses to tissue injury. The dilatory mediators signaling these responses are incompletely understood. We show that integrin-binding peptides containing the Arg-Gly-Asp (RGD) tripeptide sequence cause immediate and, in some instances, sustained vasodilation when applied to isolated rat cremaster arterioles. The vasodilation is dependent on interaction of the soluble RGD sequence with the αvβ3 integrin expressed by smooth muscle cells in the arteriolar wall. Possible in vivo sources of soluble RGD sequences are fragments of extracellular matrix proteins that are generated after tissue injury. Indeed, protease-generated fragments of denatured collagen type I (a major source of RGD sequences) also cause cremaster arteriolar vasodilation through the αvβ3 integrin. Thus, extracellular matrix protein fragments containing the RGD sequence may act as vascular wound recognition signals to regulate blood flow to injured tissue.
SOCIAL MEDIA
Connect with us and stay updated by following our social media channels.
Latest Briefings from our Knowledge Center
Press Releases, Industry News, Articles, and Technical Content
Gavathiotis, E., Albert Einstein College of Medicine, 2017. U.S. Patent Application 15/311,861.
"Hydrocarbon-stapled peptide corresponding to the BH3 domain of BIM, BIM SAHBA2: N-acetylated 145EIWIAQELRS5IGDS5FNAYYA164-CONH2 (SEQ ID NO:2), where S5 represents the non-natural amino acid inserted for olefin metathesis, was synthesized, purified and characterized as previously described by CPC Scientific (11)."
Kwon, Ester J., Jaideep S. Dudani, and Sangeeta N. Bhatia. Nature Biomedical Engineering 1 (2017): 0054.
[..] MMP substrate, 5-FAM–GGPLGVRGKK(CPQ2)–PEG2–C; thrombin substrate, 5-FAM–GGfPRSGGGK(CPQ2)–PEG2–C; where 5-FAM is the 5-carboxyfluorescein fluorophore, CPQ2 is the quencher, PEG2 is the linker polyethylene glycol, [..] dye for urinary detection (biotin–CGPLGVRGKK(Cy7)eGvndneeGffsar; Cy7 is cyanine7). Targeting peptides were [..] cyclized: LyP1, C–K(5-FAM)–C6–CGNKRTRGC; iRGD, C–PEG2–CRGDKGPDC; where C6 is the 6-aminohexanoic acid linker [..]
Weaver, Clarissa L., et al. Biochemistry 56.15 (2017): 2071-2075.
"The peptide, NCysRepA50mer (C MNQSFISDIL YADIESKAKE LTVNSNNTVQ PVALMRLGVF VPKPSKSKGE), was synthesized by CPC Scientific (Sunnyvale, CA). "
Wang, X., Kurowski, S., Wu, W., Castriota, G.A., Zhou, X., Chu, L., Ellsworth, K.P., Chu, D., Edmondson, S., Ali, A. and Andre, P. Journal of Pharmacology and Experimental Therapeutics 360, no. 3 (2017): 476-483.
- Departments of Cardiometabolic Disease Biology, Discovery Pharmaceutical Sciences, In Vitro Pharmacology, and Discovery Chemistry, Merck Research Laboratories, Kenilworth, New Jersey.
- Lead Optimization Chemistry, Merck Research Laboratories, Rahway, New Jersey.
The 7-amido-4-thifluoromethylcoumarin (AFC) containing fluorescence substrate, CH3SO2-cyclohexyl-Gly-Gly-Arg-AFC (cyclohexyl-G-G-R-AFC) was custom synthesized by CPC Scientific (Sunnyvale, CA, USA)..
Barbieri, Christopher M., et al. Journal of Pharmacology and Experimental Therapeutics 360.3 (2017): 466-475.
- In Vitro Pharmacology and Cardiometabolic Diseases, Merck & Co., Inc., Kenilworth, New Jersey
"The 7-amido-4-thifluoromethylcoumarin (AFC) containing fluorescence substrate, CH3SO2-cyclohexyl-Gly-Gly-Arg-AFC (cyclohexylG-G-R-AFC) was custom synthesized by CPC Scientific (Sunnyvale, CA, USA)"
Joshi, Bishnu P., et al. Endoscopy 48.02 (2016): A1-A13
"ASY*-FITC was synthesized using good manufacturing practice (GMP) methods (CPC Scientific, Inc.). Stability was evaluated on high-performance liquid chromatography (HPLC) and mass spectrometry.”
Chatterjee, Samit, et al. Biochemical and Biophysical Research Communications 483.1 (2017): 258-263.
PD-L1 binding peptide, WL12, was custom synthesized by CPC Scientific (Sunnyvale, CA) with >95% purity.
Novel theranostic nanoporphyrins for photodynamic diagnosis and trimodal therapy for bladder cancer.
Lin, Tzu-Yin, et al. Biomaterials 104 (2016): 339-351.
"Our previously reported PLZ4-PEG 5k -CA 8 telodendrimer was synthesized by the conjugation of alkyne-derivatized bladder cancer targeting ligand PLZ4 (CPC Scientific, Sunnyvale, CA)"