Novel Synthetic Polyamines Have Potent Antimalarial Activities in vitro and in vivo by Decreasing Intracellular Spermidine and Spermine Concentrations

Bissati, Kamal El; Redel, Henry; Ting, Li Min; Lykins, Joseph; McPhillie, Martin J.; Upadhya, Rajendra; Woster, Patrick M.; Yarlett, Nigel; Kim, Kami; Weiss, Louis M.

doi:10.3389/fcimb.2019.00009

Cited by 18 publications

(14 citation statements)

References 47 publications

(53 reference statements)

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“…This is likely due to the Fc-mediated mechanism of action found to be a large contributor to protection in many stalk-directed strategies, as these mechanisms are not neutralizing but rather contribute to viral clearance after infection [ 26 ]. This indicates that although the breadth of reactivity is increased with these stalk-directed approaches, the robustness of the protection is diminished [ 66 ].…”

Section: Stalk-directed Strategiesmentioning

confidence: 99%

Strategies Targeting Hemagglutinin as a Universal Influenza Vaccine

Bullard

Weaver

2021

Vaccines

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Influenza virus has significant viral diversity, both through antigenic drift and shift, which makes development of a vaccine challenging. Current influenza vaccines are updated yearly to include strains predicted to circulate in the upcoming influenza season, however this can lead to a mismatch which reduces vaccine efficacy. Several strategies targeting the most abundant and immunogenic surface protein of influenza, the hemagglutinin (HA) protein, have been explored. These strategies include stalk-directed, consensus-based, and computationally derived HA immunogens. In this review, we explore vaccine strategies which utilize novel antigen design of the HA protein to improve cross-reactive immunity for development of a universal influenza vaccine.

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Section: Stalk-directed Strategiesmentioning

confidence: 99%

Strategies Targeting Hemagglutinin as a Universal Influenza Vaccine

Bullard

Weaver

2021

Vaccines

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“…В общем случае, противопаразитное действие аналогов полиаминов имеет химиотерапевтический характер. Нарушение обменных процессов, вызванное ингибированием ферментов биосинтеза/катаболизма полиаминов, а также взаимодействие с ДНК/РНК вызывает гибель патогенных организмов [82].…”

Section: противопаразитарная активностьunclassified

Structure and biological action of analogs and derivatives of biogenic polyamines

Egorov

Borisova

et al. 2021

Fine Chem. Technol.

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Objectives. Biogenic polyamines are widely present in nature. They are characteristic of both protozoan cells and multicellular organisms. These compounds have a wide range of biological functions and are necessary for normal growth and development of cells. Violation of polyamine homeostasis can cause significant abnormalities in cell functioning, provoking various pathological processes, including oncological and neuropsychiatric diseases. The impact on the “polyamine pathway” is an attractive basis for the creation of many pharmacological agents with a diverse spectrum of action. The purpose of this review is to summarize the results of the studies devoted to understanding the biological activity of compounds of the polyamine series, comparing their biological action with action on certain molecular targets. Due to the structural diversity of this group of substances, it is impossible to fully reflect the currently available data in one review. Therefore, in this work, the main attention is paid to the derivatives, acyclic saturated polyamines.Results. The following aspects are considered: biological functionality, biosynthesis and catabolism, cell transport, and localization of biogenic polyamines in the living systems. Structural analogs and derivatives of biogenic polyamines with antitumor, neuroprotective, antiarrhythmic, antiparasitic, antibacterial, and other biological activities are represented; the relationship between biological activity and the target of exposure is reflected. It was found that the nature of the substituent, the number of cationic centers, and the length of the polyamine chain have a great influence on the nature of the effect.Conclusions. At present, the use of polyamine structures is restrained by cytotoxicity and nonspecific toxic effects on the central nervous system. Further research in the field of biochemistry, cell transport, and a deeper understanding of receptor interaction mechanisms will help making polyamines as the basis for potential drug formulation.

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“…In the last decades, thiourea derivatives have received considerable attention owing to their effective biological activities, including the antibacterial [1][2][3][4][5][6], antitubercular [7,8], antimalarial [9][10][11], antileishmanial [12], antifungal [13][14][15][16], or antiviral effects [17][18][19][20][21][22][23].…”

Section: Introductionmentioning

confidence: 99%

New Substituted Benzoylthiourea Derivatives: From Design to Antimicrobial Applications

et al. 2020

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The increasing threat of antimicrobial resistance to all currently available therapeutic agents has urged the development of novel antimicrobials. In this context, a series of new benzoylthiourea derivatives substituted with one or more fluorine atoms and with the trifluoromethyl group have been tested, synthesized, and characterized by IR, NMR, CHNS and crystal X-ray diffraction. The molecular docking has provided information regarding the binding affinity and the orientation of the new compounds to Escherichia coli DNA gyrase B. The docking score predicted the antimicrobial activity of the studied compounds, especially against E. coli, which was further demonstrated experimentally against planktonic and biofilm embedded bacterial and fungal cells. The compounds bearing one fluorine atom on the phenyl ring have shown the best antibacterial effect, while those with three fluorine atoms exhibited the most intensive antifungal activity. All tested compounds exhibited antibiofilm activity, correlated with the trifluoromethyl substituent, most favorable in para position.

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Novel Synthetic Polyamines Have Potent Antimalarial Activities in vitro and in vivo by Decreasing Intracellular Spermidine and Spermine Concentrations

Cited by 18 publications

References 47 publications

Strategies Targeting Hemagglutinin as a Universal Influenza Vaccine

Strategies Targeting Hemagglutinin as a Universal Influenza Vaccine

Structure and biological action of analogs and derivatives of biogenic polyamines

New Substituted Benzoylthiourea Derivatives: From Design to Antimicrobial Applications

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