Site-Selective C–H Amination of Phenol-Containing Biomolecules DOI Creative Commons
Carlota Girón-Elola, Ibon Sasiain, Rosalía Sánchez‐Fernández

et al.

Organic Letters, Journal Year: 2023, Volume and Issue: 25(23), P. 4383 - 4387

Published: June 7, 2023

A C-N bond-forming cross-dehydrogenative coupling of a collection Tyr-containing peptides and estrogens with heteroarenes is described. This oxidative distinguished by its scalability, operational simplicity, air tolerance enables the appendance phenothiazines phenoxazines in phenol-like compounds. When incorporated into Tb(III) metallopeptide, Tyr-phenothiazine moiety acts as sensitizer for ion, providing new tool design luminescent probes.

Language: Английский

Peptides as Therapeutic Agents: Challenges and Opportunities in the Green Transition Era DOI Creative Commons
Giacomo Rossino, Emanuela Marchese, Giovanni Galli

et al.

Molecules, Journal Year: 2023, Volume and Issue: 28(20), P. 7165 - 7165

Published: Oct. 19, 2023

Peptides are at the cutting edge of contemporary research for new potent, selective, and safe therapeutical agents. Their rise has reshaped pharmaceutical landscape, providing solutions to challenges that traditional small molecules often cannot address. A wide variety natural modified peptides have been obtained studied, many others advancing in clinical trials, covering multiple therapeutic areas. As demand peptide-based therapies grows, so does need sustainable environmentally friendly synthesis methods. Traditional peptide synthesis, while effective, involves draining processes, generating significant waste consuming vast resources. The integration green chemistry offers alternatives, prioritizing eco-friendly reduction, energy conservation. This review delves into transformative potential applying principles by discussing relevant examples application such approaches production active ingredients (APIs) with a structure how these efforts critical an effective transition era field.

Language: Английский

Citations

103

Advances in microbial exoenzymes bioengineering for improvement of bioplastics degradation DOI Creative Commons
Farzad Rahmati, Debadatta Sethi, Weixi Shu

et al.

Chemosphere, Journal Year: 2024, Volume and Issue: 355, P. 141749 - 141749

Published: March 21, 2024

Plastic pollution has become a major global concern, posing numerous challenges for the environment and wildlife. Most conventional ways of plastics degradation are inefficient cause great damage to ecosystems. The development biodegradable offers promising solution waste management. These designed break down under various conditions, opening up new possibilities mitigate negative impact traditional plastics. Microbes, including bacteria fungi, play crucial role in bioplastics by producing secreting extracellular enzymes, such as cutinase, lipases, proteases. However, these microbial enzymes sensitive extreme environmental temperature acidity, affecting their functions stability. To address challenges, scientists have employed protein engineering immobilization techniques enhance enzyme stability predict structures. Strategies improving substrate interaction, increasing thermostability, reinforcing bonding between active site substrate, refining activity being utilized boost functionality. Recently, bioengineering through gene cloning expression potential microorganisms, revolutionized biodegradation bioplastics. This review aimed discuss most recent strategies modifying bioplastic-degrading terms functionality, thermostability enhancement, binding site, with other improvement surface action. Additionally, discovered exoenzymes metagenomics were emphasized.

Language: Английский

Citations

26

In pursuit of next-generation therapeutics: Antimicrobial peptides against superbugs, their sources, mechanism of action, nanotechnology-based delivery, and clinical applications DOI

Akshita Thakur,

Akanksha Sharma, Hema Kumari Alajangi

et al.

International Journal of Biological Macromolecules, Journal Year: 2022, Volume and Issue: 218, P. 135 - 156

Published: July 20, 2022

Language: Английский

Citations

55

Recent Scaffold Hopping Applications in Central Nervous System Drug Discovery DOI

Timothy B. Callis,

Taylor R. Garrett, Andrew P. Montgomery

et al.

Journal of Medicinal Chemistry, Journal Year: 2022, Volume and Issue: 65(20), P. 13483 - 13504

Published: Oct. 7, 2022

The concept of bioisosterism and the implementation bioisosteric replacement is fundamental to medicinal chemistry. exploration bioisosteres often used probe key structural features candidate pharmacophores enhance pharmacokinetic properties. As understanding has evolved, capabilities undertake more ambitious replacements have emerged. Scaffold hopping a broadly term in literature referring variety different strategies, ranging from simple heterocyclic topological overhauls. In this work, we highlighted recent applications scaffold central nervous system drug discovery space. While benefits using approaches discovery, these are also widely applicable other chemistry fields. We recommend shift toward use refined meaningful terminology within realm hopping.

Language: Английский

Citations

45

Antimicrobial Peptides and Small Molecules Targeting the Cell Membrane of Staphylococcus aureus DOI

Narchonai Ganesan,

Biswajit Mishra,

Felix LewisOscar

et al.

Microbiology and Molecular Biology Reviews, Journal Year: 2023, Volume and Issue: 87(2)

Published: April 27, 2023

Clinical management of Staphylococcus aureus infections presents a challenge due to the high incidence, considerable virulence, and emergence drug resistance mechanisms.

Language: Английский

Citations

37

Plant antimicrobial peptides: a comprehensive review of their classification, production, mode of action, functions, applications, and challenges DOI

Fanglei Zou,

Chunming Tan, Tharushi S. Shinali

et al.

Food & Function, Journal Year: 2023, Volume and Issue: 14(12), P. 5492 - 5515

Published: Jan. 1, 2023

The emergence of pathogens resistant to conventional antibiotics and the growing interest in developing alternative natural antimicrobial agents have prompted a search for plant-derived peptides (PAMPs) recent years.

Language: Английский

Citations

27

Inhibitors of SARS-CoV-2 Main Protease (Mpro) as Anti-Coronavirus Agents DOI Creative Commons
Agnieszka Zagórska, Anna Czopek,

Monika Fryc

et al.

Biomolecules, Journal Year: 2024, Volume and Issue: 14(7), P. 797 - 797

Published: July 4, 2024

The main protease (Mpro) of SARS-CoV-2 is an essential enzyme that plays a critical part in the virus’s life cycle, making it significant target for developing antiviral drugs. inhibition Mpro has emerged as promising approach therapeutic agents to treat COVID-19. This review explores structure protein and analyzes progress made understanding protein–ligand interactions inhibitors. It focuses on binding kinetics, origin, chemical these provides in-depth analysis recent clinical trials involving covalent non-covalent inhibitors emerging dual targeting Mpro. By integrating findings from literature ongoing trials, this captures current state research into inhibitors, offering comprehensive challenges directions their future development anti-coronavirus agents. information new insights inspiration medicinal chemists, paving way more effective novel COVID-19 therapies.

Language: Английский

Citations

11

Recent Advances on Targeting Proteases for Antiviral Development DOI Creative Commons
Pedro Henrique Oliveira Borges, Sabrina Baptista Ferreira, Floriano Paes Silva

et al.

Viruses, Journal Year: 2024, Volume and Issue: 16(3), P. 366 - 366

Published: Feb. 27, 2024

Viral proteases are an important target for drug development, since they can modulate vital pathways in viral replication, maturation, assembly and cell entry. With the (re)appearance of several new viruses responsible causing diseases humans, like West Nile virus (WNV) recent severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), understanding mechanisms behind blocking protease’s function is pivotal development antiviral drugs therapeutical strategies. Apart from directly inhibiting protease, usually by targeting its active site, have been explored to impair activity, such as inducing protein aggregation, allosteric sites or degradation cellular proteasomes, which be extremely valuable when considering emerging drug-resistant strains. In this review, we aim discuss advances on a broad range inhibitors, therapies molecular approaches inactivation degradation, giving insight different possible strategies against class target.

Language: Английский

Citations

10

Nature’s Arsenal: Uncovering Antibacterial Agents Against Antimicrobial Resistance DOI Creative Commons
Ina Gajić, Dušan Kekić, Marko Janković

et al.

Antibiotics, Journal Year: 2025, Volume and Issue: 14(3), P. 253 - 253

Published: March 1, 2025

Background/Objectives: Antimicrobial resistance (AMR) poses a significant public health threat, leading to increased mortality. The World Health Organization has established priority list highlighting critical multidrug-resistant (MDR) pathogens that demand urgent research on antimicrobial treatments. Considering this and the fact new antibiotics are only sporadically approved, natural antibacterial agents have seen resurgence in interest as potential alternatives conventional chemotherapeutics. Natural antibacterials, derived from microorganisms, higher fungi, plants, animals, minerals, food sources, offer diverse mechanisms of action against MDR pathogens. Here, we present comprehensive summary including brief history their application key strategies for using microorganisms (microbiopredators, such bacteriophages), plant extracts essential oils, minerals (e.g., silver copper), well compounds animal origin, milk or even venoms. review also addresses role prebiotics, probiotics, peptides, novel formulations nanoparticles. these compounds, terpenoids, alkaloids, phenolic explored alongside challenges application, e.g., extraction, formulation, pharmacokinetics. Conclusions: Future should focus developing eco-friendly, sustainable validating safety efficacy through clinical trials. Clear regulatory frameworks integrating into practice. Despite challenges, sources transformative combating AMR promoting solutions.

Language: Английский

Citations

2

Perspectives on Nuclear Magnetic Resonance Spectroscopy in Drug Discovery Research DOI
Janet Caceres‐Cortes, Bradley T. Falk, Luciano Mueller

et al.

Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 67(3), P. 1701 - 1733

Published: Jan. 30, 2024

The drug discovery landscape has undergone a significant transformation over the past decade, owing to research endeavors in wide range of areas leading strategies for pursuing new targets and emergence novel modalities. NMR spectroscopy been technology fundamental importance these pursuits seen its use expanded both within outside traditional medicinal chemistry applications. In this perspective, we will present advancement NMR-derived methods that have facilitated characterization small molecules modalities including macrocyclic peptides, cyclic dinucleotides, ligands protein degradation. We discuss innovations at biology interface broadened NMR's utility from hit identification through lead optimization activities. also promise emerging approaches bridging our understanding addressing challenges pursuit therapeutic agents future.

Language: Английский

Citations

9