The present invention relates to the field of regulating the activity of the purinergic receptors for the modulation of the vascular tone, particularly for the purpose of treatment of haemodynamic conditions by overriding of vasoconstriction activity, such as increases in sympathic vasoconstriction. Modulators, such as UTP analogues as described herein are preferably specific for P2Y2. Compounds capable of stimulating the P2Y2 receptor are suitable for the treatment or prevention wherein inhibition of vasoconstriction activity is desirable such as hypertension and hypertension relates disorders or diseases, whereas compound capable of counteracting the activity of the P2Y2 receptor are suitable for the treatment of or prevention wherein inhibition of vasodilatation is desirable.
Automated Maskless Photolithography System for Peptide Microarray Synthesis on a Chip
作者:Dong-Sik Shin、Kook-Nyung Lee、Byung-Wook Yoo、Jaehi Kim、Mira Kim、Yong-Kweon Kim、Yoon-Sik Lee
DOI:10.1021/cc100009g
日期:2010.7.12
Maskless photolithographic peptide synthesis was performed on a glass chip using an automated peptide array synthesizer system. The peptide array synthesizer was built in a closed box, which contained optical and fluidic systems. The conditions for peptide synthesis were fully controlled by a computer program. For the peptide synthesis on a glass chip, 20 NVOC-protected amino acids were synthesized. The coupling efficiencies of two model peptide sequences were examined on ACA/APTS and PEG/CHI/GPTS chips. PEG/CHI/GPIS chip gave higher average stepwise yields of GIYWHHY (94%) and YIYGSFK (98%) than those of ACA/APTS chip. To quantify peptide-protein binding affinity, HPQ- or HPM-containing pentapeptides were synthesized on a PEG/CHI/GPTS chip and the binding event of Cy3 labeled-streptavidin was quantified. The peptide sequence of IQHPQ showed highest binding affinity with Cy3 labeled-streptavidin. The results demonstrated that the photolithographic peptide array synthesis method efficiently quantified the binding activities of protein-peptide interactions and it can be used for additional biological assay applications.
Preparation of Translationally Competent tRNA by Direct Chemical Acylation
作者:Noah H. Duffy、Dennis A. Dougherty
DOI:10.1021/ol101408f
日期:2010.9.3
Nonsense codon suppression for unnatural amino acid incorporation requires the preparation of a suppressor aminoacyl-tRNA. Chemical acylation strategies are general but inefficient and arduous. A recent report (J. Am. Chem. Soc. 2007, 129, 15848) showed acylation of RNA mediated by lanthanum(III) using amino acid phosphate esters. The successful implementation of this methodology to full-length suppressor tRNA is described, and it is shown that the derived aminoacyl-tRNA is translationally competent in Xenopus oocytes.
COMPOUNDS THAT BIND P2Y sb 2 /sb OR P2Y sb 1 /sb RECEPTORS