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Introduction to Vaccination
Published in Mesut Karahan, Synthetic Peptide Vaccine Models, 2021
Nezih Pişkinpaşa, Ömer Faruk Karasakal
In this book synthetic peptide vaccines are explained in detail. Peptide is a word that is of Greek origin. Peptides are found naturally in the body, plants, animals, or it is synthesized in laboratories. The body can produce ribosomal and non-ribosomal peptides. Peptides can be synthesized by more than one method. Peptide synthesis depends on bonding the amino acids with peptide bonds. They are also known as amide bonds. The biological process of producing long peptides is known as protein biosynthesis. Peptides play an important role in biological and physiological processes. They can be synthesized in natural objects via genetic and bioengineering principles, or by using chemical synthesis methods. The greatest advantage of using chemical synthesis methods in vaccine studies is the elimination of the infection-induced factors caused by the antigen. This provides a more stable and specific response to the intended vaccine (Özcan et al. 2019). Peptide-based vaccination usually takes place by using an immunoadjuvant (nanoparticles or biopolymers) to induce T cell and sometimes B cell immunity. It can also be said that peptide-based vaccines have the ability to play a role in inducing innate and adaptive immunity, but without the peptide, biopolymer, or nanoparticle system, they show weakness in immune responses. (Özcan et al. 2019). Strong targeted immune responses with a specific phenotype of many dimensions are required for a strong immunogenic trait, including T cells and B cell phebotypes, antigen-presenting cells, and phenotypes of other immune cells given in Chapter 1.
Cell Components and Function
Published in Peter Kam, Ian Power, Michael J. Cousins, Philip J. Siddal, Principles of Physiology for the Anaesthetist, 2020
Peter Kam, Ian Power, Michael J. Cousins, Philip J. Siddal
Tetrodotoxin and saxitoxin block the mouth of sodium channels from the outside. Sodium channel function is reduced by a high hydrogen concentration. Ester and amide local anaesthetics block the channel after diffusing through the membrane. Quaternary ammonium ions may block the channel at the same site, but they are not lipid soluble and only work when applied internally. Some peptide toxins from scorpions and sea anemones prevent the inactivation of sodium channels, producing hyperexcitation and pain.
Cationic Surfactants and Quaternary Derivatives for Hair and Skin Care
Published in Randy Schueller, Perry Romanowski, Conditioning Agents for Hair and Skin, 2020
Matthew F. Jurczyk, David T. Floyd, Burghard H. Grüning
Amidoamines are an interesting class of substances characterized by the presence of one or more amide groups coupled with one or more amine functions. When compared to alkyl amines and their derivatives, amidoamines are generally more compatible with anionic surfactants, easier to formulate with, and function as better foaming aids (9), Representative amidoamine compounds and related derivatives are displayed in Figure 5.
Design, synthesis and in vitro and in vivo biological evaluation of flurbiprofen amides as new fatty acid amide hydrolase/cyclooxygenase-2 dual inhibitory potential analgesic agents
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Alessandro Deplano, Jessica Karlsson, Federica Moraca, Mona Svensson, Claudia Cristiano, Carmine Marco Morgillo, Christopher J. Fowler, Roberto Russo, Bruno Catalanotti, Valentina Onnis
The obtained halogenated amides (Flu-AM3, 4 and 6), along with the reference compound Flu-AM1 were evaluated for their ability to inhibit FAAH. The inhibition assays were performed using 0.5 µM [3H]AEA as substrate and rat or mouse brain homogenates as the enzyme source. The results of these primary assays are shown in Table 1 and Figure 1(A). The results revealed that the introduction of a halogenated moiety at 3-position of pyridine ring resulted in an increased ability to inhibit FAAH as compared to the reference Flu-AM1. All the new amides showed enhanced activity as compared with the reference. The replacement of the methyl on the pyridine ring of Flu-AM1 with a trifluoromethyl group led to about 4-fold increase in activity (Flu-AM3 IC50 0.11 µM). The introduction in the same position of chlorine or bromine atom produced further increase in activity being amides Flu-AM6 and Flu-AM4 with nanomolar potency (IC50 19 and 21 nM respectively, i.e. more than three orders of magnitude greater than flurbiprofen) and approximately 20-fold more potent than Flu-AM1.
Mechanistic and biological characterisation of novel N 5-substituted paullones targeting the biosynthesis of trypanothione in Leishmania
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Andrea Medeiros, Diego Benítez, Ricarda S. Korn, Vinicius C. Ferreira, Exequiel Barrera, Federico Carrión, Otto Pritsch, Sergio Pantano, Conrad Kunick, Camila I. de Oliveira, Oliver C. F. Orban, Marcelo A. Comini
These data suggest that the enzyme binding pocket for the N5-substituent of paullones allows the accommodation of an acetamide linker with either smaller and apolar groups (e.g. methyl: 9 and 10, ethyl: 11, pyrrolidine: 25) or larger (a)polar groups (e.g. piperazine: 20 or 4-methylpiperazine: 21). Overall, compounds bearing tertiary amides (N,N-dimethyl: 10 and N,N-diethyl: 12) were more potent than those with secondary (9, 11, 13–19) or primary (7) amides. In addition, the apolar nature of relatively smaller substituents appears to be important because derivatives containing groups with H-bond donors or acceptors (e.g. a terminal primary alcohol, 1,3,4-thiadiazole, 4,5-dihydro-1,3-thiazole or 1,3-oxazole: 13, 14, 16, 17 and 18, all with µM IC50) were less active than those lacking them (e.g. N-methyl, N-ethyl, N,N-dimethyl, N,N-diethyl and pyrrolidine: 9, 11, 10, 12 and 25, all with nM IC50).
Characterization of the phosphotransacetylase-acetate kinase pathway for ATP production in Porphyromonas gingivalis
Published in Journal of Oral Microbiology, 2019
Yasuo Yoshida, Mitsunari Sato, Takamasa Nonaka, Yoshiaki Hasegawa, Yuichiro Kezuka
Structural analysis revealed an acetyl-CoA molecule bound to each subunit (Figure 5(a)), with seven direct hydrogen bonds or electrostatic interactions between the bound acetyl-CoA and subunit B (Figure 5(b)). The adenine base is recognized by two hydrogen bonds with the main-chain amide and carbonyl groups of Val150. The 3´-phosphate interacts with the side chains of Arg89 and Lys92 in subunit B. Arg135 forms an electrostatic interaction with the β-phosphate. The second amide nitrogen is hydrogen-bonded to the carbonyl group of Ala175. The interactions provided from Lys92 and Ala175 are missing in subunit A due to differences in χ angles of side chains and/or the bound acetyl-CoA. This results in higher B-factor values for acetyl-CoA in subunit A (74 Å2) than subunit B (52 Å2).