Synthetic strategy for organometallic complexes of rhenium with exceptionally high affinity for the oestradiol receptor; their potential use as imaging and therapeutic agents

1994 ◽  
pp. 453-454 ◽  
Author(s):  
Siden Top ◽  
Anne Vessières ◽  
Gérard Jaouen
Keyword(s):  
Therapeutic Agents ◽  
Organometallic Complexes ◽  
High Affinity ◽  
Synthetic Strategy ◽  
Potential Use

Bio-organometallic Peptide Conjugates: Recent Advances in Their Synthesis and Prospects for Biomedical Application

2020 ◽  
Vol 24 (21) ◽  
pp. 2508-2523
Author(s):  
Johana Gómez ◽  
Diego Sierra ◽  
Constanza Cárdenas ◽  
Fanny Guzmán
Keyword(s):  
Amino Acids ◽  
Biomedical Application ◽  
Structural Diversity ◽  
Biological Properties ◽  
Therapeutic Agents ◽  
Organometallic Complexes ◽  
Chemical Behavior ◽  
Metal Compounds ◽  
Bioorganometallic Chemistry ◽  
Pharmacological Control

One area of organometallic chemistry that has attracted great interest in recent years is the syntheses, characterization and study of organometallic complexes conjugated to biomolecules with different steric and electronic properties as potential therapeutic agents against cancer and malaria, as antibiotics and as radiopharmaceuticals. This minireview focuses on the unique structural diversity that has recently been discovered in α- amino acids and the reactions of metallocene complexes with peptides having different chemical behavior and potential medical applications. Replacing α-amino acids with metallocene fragments is an effective way of selectively influencing the physicochemical, structural, electrochemical and biological properties of the peptides. Consequently, research in the field of bioorganometallic chemistry offers the opportunity to develop bioactive metal compounds as an innovative and promising approach in the search for pharmacological control of different diseases.

Novel inhibitors of the high-affinity l-proline transporter as potential therapeutic agents for the treatment of cognitive disorders

2014 ◽  
Vol 24 (16) ◽  
pp. 3886-3890 ◽  
Author(s):  
G. Greg Zipp ◽  
Joseph Barbosa ◽  
Michael A. Green ◽  
Kristen M. Terranova ◽  
Cynthia Fink ◽  
...  
Keyword(s):  
Cognitive Disorders ◽  
Therapeutic Agents ◽  
High Affinity

scholarly journals In VitroActivities of Hexaazatrinaphthylenes against Leishmania spp.

2015 ◽  
Vol 59 (5) ◽  
pp. 2867-2874 ◽  
Author(s):  
Atteneri López-Arencibia ◽  
Daniel García-Velázquez ◽  
Carmen M. Martín-Navarro ◽  
Ines Sifaoui ◽  
María Reyes-Batlle ◽  
...  
Keyword(s):  
Therapeutic Agents ◽  
Content Type ◽  
Inhibition Effect ◽  
Intracellular Amastigotes ◽  
Dependent Inhibition ◽  
Leishmania Spp ◽  
Dose Dependent Inhibition ◽  
Dose Dependent ◽  
Potential Use

ABSTRACTThein vitroactivity of a novel group of compounds, hexaazatrinaphthylene derivatives, against two species ofLeishmaniais described in this study. These compounds showed a significant dose-dependent inhibition effect on the proliferation of the parasites, with 50% inhibitory concentrations (IC50s) ranging from 1.23 to 25.05 μM against the promastigote stage and 0.5 to 0.7 μM against intracellular amastigotes. Also, a cytotoxicity assay was carried out to in order to evaluate the possible toxic effects of these compounds. Moreover, different assays were performed to determine the type of cell death induced after incubation with these compounds. The obtained results highlight the potential use of hexaazatrinaphthylene derivatives againstLeishmaniaspecies, and further studies should be undertaken to establish them as novel leishmanicidal therapeutic agents.

scholarly journals Brain-specific inhibition of mTORC1 eliminates side effects resulting from mTORC1 blockade in the periphery and reduces alcohol intake in mice

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Yann Ehinger ◽  
Ziyang Zhang ◽  
Khanhky Phamluong ◽  
Drishti Soneja ◽  
Kevan M. Shokat ◽  
...  
Keyword(s):  
Side Effects ◽  
Inhibitory Action ◽  
Alcohol Use Disorder ◽  
Alcohol Intake ◽  
Therapeutic Agents ◽  
Adverse Side Effects ◽  
Mtorc1 Activation ◽  
Potential Use ◽  
Heavy Alcohol Intake ◽  
Alcohol Dependent

AbstractAlcohol Use Disorder (AUD) affects a large portion of the population. Unfortunately, efficacious medications to treat the disease are limited. Studies in rodents suggest that mTORC1 plays a crucial role in mechanisms underlying phenotypes such as heavy alcohol intake, habit, and relapse. Thus, mTORC1 inhibitors, which are used in the clinic, are promising therapeutic agents to treat AUD. However, chronic inhibition of mTORC1 in the periphery produces undesirable side effects, which limit their potential use for the treatment of AUD. To overcome these limitations, we designed a binary drug strategy in which male mice were treated with the mTORC1 inhibitor RapaLink-1 together with a small molecule (RapaBlock) to protect mTORC1 activity in the periphery. We show that whereas RapaLink-1 administration blocked mTORC1 activation in the liver, RapaBlock abolished the inhibitory action of Rapalink-1. RapaBlock also prevented the adverse side effects produced by chronic inhibition of mTORC1. Importantly, co-administration of RapaLink-1 and RapaBlock inhibited alcohol-dependent mTORC1 activation in the nucleus accumbens and attenuated alcohol seeking and drinking.

scholarly journals Is There Potential for Repurposing Statins as Novel Antimicrobials?

2016 ◽  
Vol 60 (9) ◽  
pp. 5111-5121 ◽  
Author(s):  
Emma Hennessy ◽  
Claire Adams ◽  
F. Jerry Reen ◽  
Fergal O'Gara
Keyword(s):  
Serum Cholesterol ◽  
Bacterial Growth ◽  
Bacterial Infections ◽  
Statin Treatment ◽  
Therapeutic Agents ◽  
Pleiotropic Effects ◽  
Current Information ◽  
Potential Use

ABSTRACTStatins are members of a class of pharmaceutical widely used to reduce high levels of serum cholesterol. In addition, statins have so-called “pleiotropic effects,” which include inflammation reduction, immunomodulation, and antimicrobial effects. An increasing number of studies are emerging which detail the attenuation of bacterial growth andin vitroandin vivovirulence by statin treatment. In this review, we describe the current information available concerning the effects of statins on bacterial infections and provide insight regarding the potential use of these compounds as antimicrobial therapeutic agents.

scholarly journals Extracellular Vesicles as Biological Shuttles for Targeted Therapies

2019 ◽  
Vol 20 (8) ◽  
pp. 1848 ◽  
Author(s):  
Stefania Raimondo ◽  
Gianluca Giavaresi ◽  
Aurelio Lorico ◽  
Riccardo Alessandro
Keyword(s):  
Extracellular Vesicles ◽  
Therapeutic Agents ◽  
Bioactive Molecules ◽  
Target Cells ◽  
Special Focus ◽  
Pathological Conditions ◽  
Critical Issues ◽  
Membrane Bound ◽  
And Function ◽  
Potential Use

The development of effective nanosystems for drug delivery represents a key challenge for the improvement of most current anticancer therapies. Recent progress in the understanding of structure and function of extracellular vesicles (EVs)—specialized membrane-bound nanocarriers for intercellular communication—suggests that they might also serve as optimal delivery systems of therapeutics. In addition to carrying proteins, lipids, DNA and different forms of RNAs, EVs can be engineered to deliver specific bioactive molecules to target cells. Exploitation of their molecular composition and physical properties, together with improvement in bio-techniques to modify their content are critical issues to target them to specific cells/tissues/organs. Here, we will discuss the current developments in the field of animal and plant-derived EVs toward their potential use for delivery of therapeutic agents in different pathological conditions, with a special focus on cancer.

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