63,184 research outputs found
Preparation of 'side-chain-to-side-chain' cyclic peptides by Allyl and Alloc strategy: Potential for library synthesis
No full textAutomated and manual deprotection methods for allyl/allyloxycarbonyl (Allyl/Alloc) were evaluated for the prepn. of side-chain-to-side-chain cyclic peptides. Using a std. Allyl/Alloc deprotection method, a small library of cyclic peptides with lactam bridges (with seven amino acids) was prepd. on an automatic peptide synthesizer. We demonstrate that the Guibe method for removing Allyl/Alloc protecting groups under specific neutral conditions [Pd(PPh3)4/PhSiH3/DCM] can be a useful, efficient and reliable method for prepg. long cyclic peptides on a resin. We have also manually synthesized a cyclic glucagon analog contg. 24 amino acid residues. These results demonstrated that properly controlled palladium-mediated deprotection of Allyl/Alloc protecting groups can be used to prep. cyclic peptides on the resin using an automated peptide synthesizer and cyclic peptides with a long chain
J. N. Aletti, L. beirnaert, J. Calloud, M. Carrez, G. Combet, J. Delorme, A. George, P. Grelot, K. Hruby, P. Lamarche, s. Legasse, X. Léon-Dufour (éd.), Les miracles de Jésus, Parole de Dieu, 1977
No full textC. C. J. N. Aletti, L. beirnaert, J. Calloud, M. Carrez, G. Combet, J. Delorme, A. George, P. Grelot, K. Hruby, P. Lamarche, s. Legasse, X. Léon-Dufour (éd.), Les miracles de Jésus, Parole de Dieu, 1977. In: Revue des Sciences Religieuses, tome 54, fascicule 1, 1980. p. 92
Structure-Activity Relationships of Novel Cyclic alpha-MSH/gamma-MSH Hybrid Analogues which Lead to Potent and Selective Ligands for the Human MC3R and Human MC5R
No full textStructure-Activity Relationships of Novel Cyclic alpha-MSH/gamma-MSH Hybrid Analogues which Lead to Potent and Selective Ligands for the Human MC3R and Human MC5R
No full textStructure-Activity Relationships of alpha-MSH Analogues at the Human Melanocortin MC3, MC4, and MC5 Receptors. Discovery of Highly Selective hMC3R, hMC4R, and hMC5R Analogues.
No full textIt has been shown by extensive studies that melanotropin bioactivities are critically dependent
on the core or central tetrapeptide sequence, His-Phe-Arg-Trp, and in R-MSH it has been
demonstrated further that a reverse-turn type conformation exists at this pharmacophore. To
probe the receptor active conformation of the pharmacophore His-Phe-Arg-Trp in ç-MSH, two
different series of ç-MSH analogues have been designed and synthesized and their biological
activities determined at hMC3R, hMC4R, and hMC5R. The 1st series consists of a cyclic scan
using different disulfides or lactam bridges. It was found that cyclization of the native ç-MSH
around the highly conserved sequence can lead to shifts in affinity and selectivity for hMC4R
instead of the hMC3R as seen in the native peptide. Furthermore, a 23-membered ring is
desirable for potency (e.g., analogues 6 and 10) whereas a 26-membered ring (analogue 1, H-Tyr-
Val-c[Cys-Gly-His-Phe-Arg-Trp-Cys]-Arg-Phe-Gly-NH2 with Gly4) is more important for selectivity.
The 2nd series is made of D-2-naphthylalanine (D-Nal(2¢)) scan of the ç-MSH sequence at
position 6 and 8 and the replacement of His5 with Pro (analogue 13). Analogue 12, H-Tyr-Val-
Nle-Gly-His-Phe-Arg-D-Nal(2¢)-Asp-Arg-Phe-Gly-NH2, is a potent and selective antagonist at
the hMC4R, and analogue 15, H-Tyr-Val-Nle-Gly-Aib-Phe-Arg-D-Nal(2¢)-Asp-Arg-Phe-Gly-NH2,
is a highly selective and potent agonist of the hMC5R. A most promising analogue is 13, H-Tyr-
Val-Nle-Gly-Pro-D-Nal(2¢)-Arg-Trp-Asp-Arg-Phe-Gly-NH2, which is a very potent agonist of the
hMC4R, and this analogue can be further evaluated for feeding behavior and the regulation of
fat stores
A 2 h periodic variation in the low-mass X-ray binary Ser X-1
No full textSpectroscopy of the low-mass X-ray binary Ser X-1 using the Gran Telescopio Canarias have revealed a ?2 h periodic variability that is present in the three strongest emission lines. We tentatively interpret this variability as due to orbital motion, making it the first indication of the orbital period of Ser X-1. Together with the fact that the emission lines are remarkably narrow, but still resolved, we show that a main-sequence K dwarf together with a canonical 1.4 M? neutron star gives a good description of the system. In this scenario, the most likely place for the emission lines to arise is the accretion disc, instead of a localized region in the binary (such as the irradiated surface or the stream-impact point), and their narrowness is due instead to the low inclination (?10°) of Ser X-1
H. Gazelles, A. Gélin, B. Botte, G. Vermès, R. Bloch, A. Descamps, P. Démann, R.-M. Tonneau, J. Daniélou, A. Luneau, J. Châtillon, K. Hruby, J. Blanc, J. Leroy, Y. Moubarac, L. Gardet, Moïse l'homme de l'alliance (« Cahiers Sioniens», nos 2, 3, 4, de 1954, réunis en un volume spécial). Tournai, Desclée et Cie, 1955
No full textPiccard Denise. H. Gazelles, A. Gélin, B. Botte, G. Vermès, R. Bloch, A. Descamps, P. Démann, R.-M. Tonneau, J. Daniélou, A. Luneau, J. Châtillon, K. Hruby, J. Blanc, J. Leroy, Y. Moubarac, L. Gardet, Moïse l'homme de l'alliance (« Cahiers Sioniens», nos 2, 3, 4, de 1954, réunis en un volume spécial). Tournai, Desclée et Cie, 1955. In: Revue d'histoire et de philosophie religieuses, 37e année n°3,1957. pp. 268-269
H. Gazelles, A. Gélin, B. Botte, G. Vermès, R. Bloch, A. Descamps, P. Démann, R.-M. Tonneau, J. Daniélou, A. Luneau, J. Châtillon, K. Hruby, J. Blanc, J. Leroy, Y. Moubarac, L. Gardet, Moïse l'homme de l'alliance (« Cahiers Sioniens», nos 2, 3, 4, de 1954, réunis en un volume spécial). Tournai, Desclée et Cie, 1955
No full textPiccard Denise. H. Gazelles, A. Gélin, B. Botte, G. Vermès, R. Bloch, A. Descamps, P. Démann, R.-M. Tonneau, J. Daniélou, A. Luneau, J. Châtillon, K. Hruby, J. Blanc, J. Leroy, Y. Moubarac, L. Gardet, Moïse l'homme de l'alliance (« Cahiers Sioniens», nos 2, 3, 4, de 1954, réunis en un volume spécial). Tournai, Desclée et Cie, 1955. In: Revue d'histoire et de philosophie religieuses, 37e année n°3,1957. pp. 268-269
Stable voters in an unstable party environment : continuity and change in Italian electoral behaviour
No full textM.24981-1999 Paolo Segatti, Paolo Bellucci and Marco Maraffi. 30 cm. A previous version of this paper was presented at a symposium on Political Parties : Changing Roles in Contemporary Democracies, held at the Center for Advanced Study in the Social Sciences of the Juan March Institute, Madrid, December 15-17, 1994. -- P.1. Includes bibliographical references (p. 56-59
De Maiestate / Praeside M. Jacobo Thomasio, Moralis Philosoph. P. P., publice disputabit Johannes Dunte, R. L. Author & Respon: ad diem 9. Septembr. H L. Q. C.
No full textDE MAIESTATE / PRAESIDE M. JACOBO THOMASIO, MORALIS PHILOSOPH. P. P., PUBLICE DISPUTABIT JOHANNES DUNTE, R. L. AUTHOR & RESPON: AD DIEM 9. SEPTEMBR. H L. Q. C.
De Maiestate / Praeside M. Jacobo Thomasio, Moralis Philosoph. P. P., publice disputabit Johannes Dunte, R. L. Author & Respon: ad diem 9. Septembr. H L. Q. C. (1)
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