Peptides that are composed of an alternating pattern of α- and γ-amino acids are potentially valuable as metabolism-resistant bioactive agents. For optimal function, some kind of conformational restriction is usually required to either stabilize the dominant 12-helix, or else to divert the peptide away from this conformation in a controlled way. Herein, we explore stereoselective fluorination as a method for controlling the conformations of α/γ-hybrid peptides. We show through a combination of X-ray, NMR and CD analyses that fluorination can either stabilize or disrupt the 12-helix, depending on the fluorine stereochemistry. These findings could inform the ongoing development of diverse functional hybrid peptides.
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http://dx.doi.org/10.1039/d3ob02016a | DOI Listing |
Ann Rheum Dis
January 2025
Division of Rheumatology, Department of Internal Medicine, Keio University School of Medicine, Tokyo, Japan. Electronic address:
Objectives: The usefulness of methotrexate-polyglutamates (MTX-PGs) concentration for management of rheumatoid arthritis has been debated. We aimed to clarify the association of MTX-PGs concentration with efficacy and safety in MTX-naïve patients initiating MTX in a prospective interventional clinical trial.
Methods: The MIRACLE trial enrolled 300 MTX-naïve patients.
Biopolymers
March 2025
Departmento de Química Inorgánica y Orgánica, Universidad Jaume I, Castellón, Spain.
We report the reversible redox-controlled DNA condensation using a simple dicationic diphenylalanine derivative which contains a disulfide unit as linker. Despite the conventional belief that DNA condensing agents require a charge of +3 or higher, this dicationic molecule functions below its critical aggregation concentration, representing a non-canonical DNA condensing agent. The interaction with DNA of the studied compound combines electrostatic effects with hydrophobic/stacking interactions provided with the diphenylalanine moiety.
View Article and Find Full Text PDFFront Immunol
January 2025
Department of Dermatology, Jacobs School of Medicine and Biomedical Sciences, University at Buffalo, Buffalo, NY, United States.
Autoimmune diseases (AID) are defined by immune dysregulation characterized by specific humoral and/or cell mediated responses directed against the body's own tissues. Cytokines in particular play a pivotal role in the pathogenesis of AID, with proinflammatory cytokines contributing to the initiation and propagation of autoimmune inflammation, whereas anti-inflammatory cytokines facilitate regression of inflammation and recovery from acute phases of the disease. Parallel work by our group evaluating a comprehensive set of pro- and anti-inflammatory serum cytokines in Pemphigus vulgaris (PV) as well as Alopecia areata (AA) uncovered a similar pattern of inheritance specific immune dysregulation in these two distinct autoimmune skin diseases.
View Article and Find Full Text PDFChemistryOpen
January 2025
Central Department of Physics, Tribhuvan University, Kathmandu, Nepal.
Thermodynamic properties of amino acids explore the ideas about the energetic contribution in biomolecular interfaces. In our work, we have estimated the solvation free energy of leucine and isoleucine peptides with the variation of chain length or residues of different monomer units (n=1, 2, 4, 8 & 16) using molecular dynamic simulation. We modeled our system using OPLS-AA force field and TIP3P water model at 310 K temperature.
View Article and Find Full Text PDFBackground: Insulinoma is a neuroendocrine tumor, the main manifestation of which is hypoglycemia. However, the symptoms of hypoglycemia can be non-specific for a long time, especially outside provocative conditions, and quite often the tumor manifests from a life-threatening condition - hypoglycemic coma. In this regard, timely laboratory diagnosis of insulinoma and determination of its aggressive course is one of the priorities in modern researches.
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