Polyamine–Drug Conjugates: Do They Boost Drug Activity?

Basagni, Filippo; Marotta, Giambattista; Rosini, Michela; Minarini, Anna

doi:10.3390/molecules28114518

Cited by 2 publications

(2 citation statements)

References 122 publications

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“…Table 2 summarizes examples of using polyamine moiety and venom acylpolyamines as pharmacological leads, probes, potential insecticides, and molecular carriers. Delivery of bioactive payloads through the polyamine transporter system [102] Notes: Aliphatic polyamines (e.g., spermine and spermidine) and venom acylpolyamines were used as lead compounds for structural modification and application. Mygalin is not a component of the tarantula Acanthoscurria gomesiana spider, but is from the hemocytes.…”

Section: Pharmacological Leadsmentioning

confidence: 99%

“…The conjugation of polyamine backbones and various compounds improves the pharmacokinetics of hydrophobic drugs and biologically active groups for cellular de-livery through the polyamine transporter system [ 102 ]. In such a case, Ishii and col-leagues developed a polycationic redox-active injectable gel in which polyamines flanked a triblock copolymer to deliver exenatide, a peptide originally from the ven-omous Gila monster (Heloderma suspectum) saliva, to control diabetes [ 100 ].…”

Section: Spider and Wasp Acylpolyamines As Versatile Pharmacological ...mentioning

confidence: 99%

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Spider and Wasp Acylpolyamines: Venom Components and Versatile Pharmacological Leads, Probes, and Insecticidal Agents

Rádis-Baptista,

Konno

2024

Toxins

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Polyamines (PAs) are polycationic biogenic amines ubiquitously present in all life forms and are involved in molecular signaling and interaction, determining cell fate (e.g., cell proliferation, dif-ferentiation, and apoptosis). The intricate balance in the PAs’ levels in the tissues will determine whether beneficial or detrimental effects will affect homeostasis. It’s crucial to note that endoge-nous polyamines, like spermine and spermidine, play a pivotal role in our understanding of neu-rological disorders as they interact with membrane receptors and ion channels, modulating neuro-transmission. In spiders and wasps, monoamines (histamine, dopamine, serotonin, tryptamine) and polyamines (spermine, spermidine, acyl polyamines) comprise, with peptides and other sub-stances, the low molecular weight fraction of the venom. Acylpolyamines are venom components exclusively from spiders and a species of solitary wasp, which cause inhibition chiefly of iono-tropic glutamate receptors (AMPA, NMDA, and KA iGluRs) and nicotinic acetylcholine receptors (nAChRs). The first venom acylpolyamines ever discovered (argiopines, Joro and Nephila toxins, and philanthotoxins) have provided templates for the design and synthesis of numerous analogs. Thus far, analogs with high potency exert their effect at nanomolar concentrations, with high se-lectivity toward their ionotropic and ligand receptors. These potent and selective acylpolyamine analogs can serve biomedical purposes and pest control management. The structural modification of acylpolyamine with photolabile and fluorescent groups converted these venom toxins into use-ful molecular probes to discriminate iGluRs and nAchRs in cell populations. In various cases, the linear polyamines, like spermine and spermidine, constituting venom acyl polyamine backbones, have served as cargoes to deliver active molecules via a polyamine uptake system on diseased cells for targeted therapy. In this review, we examined examples of biogenic amines that play an essential role in neural homeostasis and cell signaling, contributing to human health and disease outcomes, which can be present in the venom of arachnids and hymenopterans. With an empha-sis on the spider and wasp venom acylpolyamines, we focused on the origin, structure, derivatiza-tion, and biomedical and biotechnological application of these pharmacologically attractive, chemically modular venom components.

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Section: Pharmacological Leadsmentioning

confidence: 99%

Section: Spider and Wasp Acylpolyamines As Versatile Pharmacological ...mentioning

confidence: 99%

Spider and Wasp Acylpolyamines: Venom Components and Versatile Pharmacological Leads, Probes, and Insecticidal Agents

Rádis-Baptista,

Konno

2024

Toxins

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Involvement of mammalian SoLute Carriers (SLC) in the traffic of polyamines

Pochini

2024

Front. Mol. Biosci.

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Polyamines interact with different molecular targets to regulate a vast range of cellular processes. A network of enzymes and transport systems is crucial for the maintenance of polyamine homeostasis. Indeed, polyamines after synthesis must be distributed to the various tissues and some intracellular organelles. Differently from the well characterized enzymes devoted to polyamine synthesis, the transport systems are not unequivocally identified or characterized. Besides some ATPases which have been identified as polyamine transporters, much less is known about solute carriers (SLC) involved in the transport of these compounds. Only two SLCs have been unequivocally identified as polyamine transporters: SLC18B1 (VPAT) and SLC22A4 (OCTN1). Transport studies have been performed with cells transfected with the cDNAs encoding the two and other SLCs or, in the case of OCTN1, also by in vitro assay using proteoliposomes harboring the recombinant human protein. According to the role proposed for OCTN1, polyamines have been associated with prolonged and quality of life. This review provides an update on the most recent findings concerning the polyamine transporters or the prediction of the putative ones.

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Polyamine–Drug Conjugates: Do They Boost Drug Activity?

Cited by 2 publications

References 122 publications

Spider and Wasp Acylpolyamines: Venom Components and Versatile Pharmacological Leads, Probes, and Insecticidal Agents

Spider and Wasp Acylpolyamines: Venom Components and Versatile Pharmacological Leads, Probes, and Insecticidal Agents

Involvement of mammalian SoLute Carriers (SLC) in the traffic of polyamines

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