scholarly journals Illuminating glycoscience: synthetic strategies for FRET-enabled carbohydrate active enzyme probes

2020 ◽  
Vol 1 (5) ◽  
pp. 352-368
Author(s):  
Meenakshi Singh ◽  
Michael Watkinson ◽  
Eoin M. Scanlan ◽  
Gavin J. Miller
Keyword(s):  
Active Enzyme ◽  
Carbohydrate Active Enzymes ◽  
Drug Candidates ◽  
Carbohydrate Active Enzyme ◽  
New Drug ◽  
Enzyme Probes

Carbohydrates are synthesised, refined and degraded by carbohydrate active enzymes. FRET is emerging as a powerful tool to monitor and quantify their activity as well as to test inhibitors as new drug candidates and monitor disease.

Synthetic Strategies for FRET-Enabled Carbohydrate Active Enzyme Probes

2021 ◽  
pp. 237-264
Author(s):  
Meenakshi Singh ◽  
Michael Watkinson ◽  
Eoin M. Scanlan ◽  
Gavin J. Miller
Keyword(s):  
Active Enzyme ◽  
Carbohydrate Active Enzyme ◽  
Enzyme Probes

Antitubercular Marine Natural Products

2018 ◽  
Vol 25 (20) ◽  
pp. 2304-2328 ◽  
Author(s):  
Lishu Wang ◽  
Jungfeng Wang ◽  
Juan Liu ◽  
Yonghong Liu
Keyword(s):  
Natural Products ◽  
Marine Natural Products ◽  
Antitubercular Activity ◽  
Marine Resources ◽  
Drug Candidates ◽  
New Drug ◽  
Chemical Constitution

Due to the importance of nature as a source of new drug candidates, the purpose of this article is to emphasize the marine natural products, which exhibit antitubercular activity, published between January 2000 and May 2016, with 138 quotations to 250 compounds obtained from marine resources. These metabolites are organized by chemical constitution and named as simple alkyl lipids derivatives, aromatics derivatives, peptides, alkaloids, terpenoids, steroids, macrolides, and polycyclic polyketides.

Current Approaches to Drug Discovery for Chagas Disease: Methodological Advances

2019 ◽  
Vol 22 (8) ◽  
pp. 509-520
Author(s):  
Cauê B. Scarim ◽  
Chung M. Chin
Keyword(s):  
Drug Discovery ◽  
Chagas Disease ◽  
Drug Candidates ◽  
Lead Compounds ◽  
New Drug ◽  
Compound Libraries ◽  
Screening Assays ◽  
Cruzi Infection

Background: In recent years, there has been an improvement in the in vitro and in vivo methodology for the screening of anti-chagasic compounds. Millions of compounds can now have their activity evaluated (in large compound libraries) by means of high throughput in vitro screening assays. Objective: Current approaches to drug discovery for Chagas disease. Method: This review article examines the contribution of these methodological advances in medicinal chemistry in the last four years, focusing on Trypanosoma cruzi infection, obtained from the PubMed, Web of Science, and Scopus databases. Results: Here, we have shown that the promise is increasing each year for more lead compounds for the development of a new drug against Chagas disease. Conclusion: There is increased optimism among those working with the objective to find new drug candidates for optimal treatments against Chagas disease.

Molecular Topological Properties of Alkylating Agents Based Anticancer Drug Candidates Via Some Ve-degree Topological Indices

2020 ◽  
Vol 16 (2) ◽  
pp. 190-195 ◽  
Author(s):  
Süleyman Ediz ◽  
Murat Cancan
Keyword(s):  
Anticancer Drugs ◽  
Anticancer Drug ◽  
Alkylating Agents ◽  
Topological Indices ◽  
Pharmacological Properties ◽  
Topological Properties ◽  
Drug Candidates ◽  
New Drug ◽  
Atom Bond ◽  
Dual Target

Background: Reckoning molecular topological indices of drug structures gives the data about the underlying topology of these drug structures. Novel anticancer drugs have been leading by researchers to produce ideal drugs. Materials and Methods: Pharmacological properties of these new drug agents explored by utilizing simulation strategies. Topological indices additionally have been utilized to research pharmacological properties of some drug structures. Novel alkylating agents based anticancer drug candidates and ve-degree molecular topological indices have been introduced recently. Results and Conclusion: In this study we calculate ve-degree atom-bond connectivity, harmonic, geometric-arithmetic and sum-connectivity molecular topological indices for the newly defined alkylating agents based dual-target anticancer drug candidates.

Investigations on T cell transmigration in a human skin-on-chip (SoC) model

Lab on a Chip ◽  
2021 ◽  
Vol 21 (8) ◽  
pp. 1527-1539
Author(s):  
Xiaoou Ren ◽  
Anthony E. Getschman ◽  
Samuel Hwang ◽  
Brian F. Volkman ◽  
Thomas Klonisch ◽  
...  
Keyword(s):  
T Cell ◽  
T Lymphocytes ◽  
Human Skin ◽  
Drug Candidates ◽  
New Drug ◽  
Human T Lymphocytes ◽  
Quantitative Studies ◽  
Inflammatory Skin ◽  
Skin Conditions ◽  
On Chip

Our skin-on-chip (SoC) model uniquely enabled quantitative studies of transendothelial and transepithelial migration of human T lymphocytes under mimicked inflammatory skin conditions and was used to test new drug candidates.

scholarly journals 3-Phenylcoumarins as a Privileged Scaffold in Medicinal Chemistry: The Landmarks of the Past Decade

Molecules ◽  
2021 ◽  
Vol 26 (21) ◽  
pp. 6755
Author(s):  
Maria J. Matos ◽  
Eugenio Uriarte ◽  
Lourdes Santana
Keyword(s):  
Medicinal Chemistry ◽  
Review Paper ◽  
Relevant Literature ◽  
Natural Origin ◽  
Drug Candidates ◽  
Heterocyclic Molecules ◽  
The Past ◽  
New Drug ◽  
Privileged Scaffold

3-Phenylcoumarins are a family of heterocyclic molecules that are widely used in both organic and medicinal chemistry. In this overview, research on this scaffold, since 2010, is included and discussed, focusing on aspects related to its natural origin, synthetic procedures and pharmacological applications. This review paper is based on the most relevant literature related to the role of 3-phenylcoumarins in the design of new drug candidates. The references presented in this review have been collected from multiple electronic databases, including SciFinder, Pubmed and Mendeley.

scholarly journals A Novel Triple-Fluorescent HCMV Strain Reveals Gene Expression Dynamics and Anti-Herpesviral Drug Mechanisms

2021 ◽  
Vol 10 ◽  
Author(s):  
Ulfert Rand ◽  
Tobias Kubsch ◽  
Bahram Kasmapour ◽  
Luka Cicin-Sain
Keyword(s):  
Gene Expression ◽  
Hcmv Infection ◽  
Viral Fitness ◽  
High Temporal Resolution ◽  
Detection Techniques ◽  
Drug Candidates ◽  
New Drug ◽  
Gene Expression Dynamics ◽  
Identification And Characterization

Human Cytomegalovirus (HCMV) infection may result in severe outcomes in immunocompromised individuals such as AIDS patients, transplant recipients, and neonates. To date, no vaccines are available and there are only few drugs for anti-HCMV therapy. Adverse effects and the continuous emergence of drug-resistance strains require the identification of new drug candidates in the near future. Identification and characterization of such compounds and biological factors requires sensitive and reliable detection techniques of HCMV infection, gene expression and spread. In this work, we present and validate a novel concept for multi-reporter herpesviruses, identified through iterative testing of minimally invasive mutations. We integrated up to three fluorescence reporter genes into replication-competent HCMV strains, generating reporter HCMVs that allow the visualization of replication cycle stages of HCMV, namely the immediate early (IE), early (E), and late (L) phase. Fluorescent proteins with clearly distinguishable emission spectra were linked by 2A peptides to essential viral genes, allowing bicistronic expression of the viral and the fluorescent protein without major effects on viral fitness. By using this triple color reporter HCMV, we monitored gene expression dynamics of the IE, E, and L genes by measuring the fluorescent signal of the viral gene-associated fluorophores within infected cell populations and at high temporal resolution. We demonstrate distinct inhibitory profiles of foscarnet, fomivirsen, phosphonoacetic acid, ganciclovir, and letermovir reflecting their mode-of-action. In conclusion, our data argues that this experimental approach allows the identification and characterization of new drug candidates in a single step.

Synthesis of Hydroxylated Biphenyls Derivatives Bearing an α,β‐Unsaturated Ketone as Lead Structure for the Development of New Drug Candidates Against Malignant Melanoma

ChemMedChem ◽  
2020 ◽  
Author(s):  
Maria Antonietta Dettori ◽  
Davide Fabbri ◽  
Marina Pisano ◽  
Carla Rozzo ◽  
Giovanna Delogu
Keyword(s):  
Malignant Melanoma ◽  
Unsaturated Ketone ◽  
Lead Structure ◽  
Drug Candidates ◽  
New Drug
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