We have examined the effect of C alpha-methyl groups on the conformational ensemble of GnRH analog peptides by comparing 1H 2D NMR data from two analogs, Ac-D-Nal1-D-4-Cl-C alpha-Me-Phe2-D-Pal3-Ser4-Tyr5-D-Arg6-Leu7-Arg8-Pro9-D-Al a10- NH2 (1) and Ac-D-Nal1-D-4-Cl-C alpha-Me-Phe2-D-Pal3-Ser4-C alpha-Me-Tyr5-D-Arg6- Leu7-C alpha-Me-Arg8-Pro9-D-Ala10-NH2 (2). The two additional C alpha-methyl groups in residues 5 and 8 of 2 do not influence significantly the pattern of the observable main chain NOE intensities, or of the backbone HN proton chemical shifts, which indicates that they do not produce global changes in the conformational ensemble of the peptide. A local change induced by the substitution was observed in the conformation at D-Arg8-Pro9.
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http://dx.doi.org/10.1111/j.1399-3011.1994.tb00546.x | DOI Listing |
J Inflamm Res
January 2025
Department of Gastroenterology, The National Key Clinical Specialty, Zhongshan Hospital of Xiamen University, School of Medicine, Xiamen University, Xiamen, Fujian, 361004, People's Republic of China.
Introduction: Crohn's disease (CD) is a chronic inflammatory condition of the intestines with a rising global incidence. Traditional diagnostic and therapeutic methods have limitations, necessitating the exploration of more effective strategies.
Methods: In this study, we employed the Gene Expression Omnibus database to identify genes that are differentially expressed in CD.
Int J Mol Sci
November 2024
Institute for Radiation Sciences, Osaka University, 2-4 Yamadaoka, Suita, Osaka 565-0871, Japan.
We investigated nuclear medicine therapeutics targeting the L-type amino acid transporter 1 (LAT1). We previously reported that a nuclear medicine therapeutic drug using astatine 211 (At), an alpha-emitting nuclide that can be produced in an accelerator and targets LAT1 as a molecular target, is effective. The seed compound was 3-[At] Astato-α-methyl-L-tyrosine (At-AAMT-OH-L).
View Article and Find Full Text PDFChemistry
January 2025
Department of Chemistry, Brock University, 1812 Sir Isaac Brock Way, L2S 3A1, St. Catharines, Ontario, Canada.
A high-nuclearity {Ni} complex (1) with a unique 'flying saucer' motif has been prepared from the organic chelate, α-methyl-2-pyridine-methanol (mpmH), in conjunction with bridging azido (N ) and peroxido (O ) ligands. Magnetic susceptibility measurements revealed the presence of both ferro- and antiferromagnetic exchange interactions between the metal centres in 1, and the stabilization of spin states with appreciable S values at two different temperature regimes. The end-on bridging azido and alkoxido groups are in all likelihood the ferromagnetic mediators, while the η:η:μ-bridging peroxides most likely promote the antiparallel alignment of the metals' spin vectors, yielding an overall non-zero spin ground state for the centrosymmetric compound 1.
View Article and Find Full Text PDFRSC Med Chem
October 2024
School of Chemistry and Chemical Engineering, Queen's University Belfast David Keir Building, Stranmillis Road Belfast BT9 5AG UK
Cyclic lipopeptides (CLiPs) are a highly diverse class of secondary metabolites produced by bacteria and fungi. Examples of CLiPs have been found that possess potent antimicrobial activity against multidrug-resistant Gram-negative bacteria. Globomycin is a 19-membered CLiP that kills both Gram-positive and Gram-negative bacteria through inhibition of lipoprotein signal peptidase II (Lsp).
View Article and Find Full Text PDFDomest Anim Endocrinol
January 2025
Melbourne Veterinary School, The University of Melbourne, Parkville, Victoria, Australia. Electronic address:
The role of dopamine in the regulation of insulin secretion in horses is poorly understood and requires further investigation. Pituitary pars intermedia dysfunction (PPID) is associated with decreased activity of dopaminergic neurons which normally suppress peptide hormone secretion from the pituitary pars intermedia. A high proportion of horses with PPID also have insulin dysregulation (ID), characterised by post-prandial hyperinsulinaemia and/or tissue insulin resistance, which are risk factors for the development of laminitis.
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