0000000000194599
AUTHOR
R. Tejero
showing 3 related works from this author
Solution NMR structure of aD,L-alternating oligonorleucine as a model of ?-helix
2001
beta-Helix structures are of particular interest due to their capacity to form transmembrane channels with different transport properties. However, the relatively large number of beta-helices configurations does not allow a direct conformational analysis of beta-helical oligopeptides. A synthetic alternating D,L-oligopeptide with twelve norleucines (XIIMe) has been used as a model to get insight in the conformational features of beta-helix structures. The spatial configuration of XIIMe in solution has been determined by NMR. An extensive set of distances (nuclear Overhauser effect) and dihedral (J coupling constants) constraints have been included in molecular dynamics calculations. The NMR…
Influence of Several Effectors on the Structure-Activity Relationship of Spleen Phosphodiesterase
1993
The influence of Mg(II) and organic solvents on the structure-activity relationship of spleen phosphodiesterase II was analyzed using UV and fluorescence spectroscopies. An increase in the RNase activity found in the presence of Mg(II) was related to the enzyme-Mg(II) interaction detected by UV spectroscopy. In the fluorescence spectra of phosphodiesterase strong hypochromic and bathochromic effects were observed when RNA was present at a concentration (52 μg ml−1) of the same magnitude as the concentration that inhibits the activity (Ki = 40 μg ml−1). The strong quenching observed in the presence of RNA shows the importance of large dynamic and static quenching of the Trp residues of the e…
Novel, potent calmodulin antagonists derived from an all-dhexapeptide combinatorial library that inhibitin vivocell proliferation: activity and struc…
2000
: Calmodulin is known to bind to various amphipathic helical peptide sequences, and the calmodulin–peptide binding surface has been shown to be remarkably tolerant sterically. d-Amino acid peptides, therefore, represent potential non-hydrolysable intracellular antagonists of calmodulin. In the present study, synthetic combinatorial libraries have been used to develop novel d-amino acid hexapeptide antagonists to calmodulin-regulated phosphodiesterase activity. Five hexapeptides were identified from a library containing over 52 million sequences. These peptides inhibited cell proliferation both in cell culture using normal rat kidney cells and by injection via the femoral vein following part…