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Advances in Fmoc solid‐phase peptide synthesis

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TLDR
The number of synthetic peptides entering clinical trials has grown continuously over the last decade, and recent advances in the Fmoc SPPS technology are a response to the growing demand from medicinal chemistry and pharmacology.
Abstract
Today, Fmoc SPPS is the method of choice for peptide synthesis. Very-high-quality Fmoc building blocks are available at low cost because of the economies of scale arising from current multiton production of therapeutic peptides by Fmoc SPPS. Many modified derivatives are commercially available as Fmoc building blocks, making synthetic access to a broad range of peptide derivatives straightforward. The number of synthetic peptides entering clinical trials has grown continuously over the last decade, and recent advances in the Fmoc SPPS technology are a response to the growing demand from medicinal chemistry and pharmacology. Improvements are being continually reported for peptide quality, synthesis time and novel synthetic targets. Topical peptide research has contributed to a continuous improvement and expansion of Fmoc SPPS applications.

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Journal ArticleDOI

Therapeutic peptides: Historical perspectives, current development trends, and future directions.

TL;DR: An overview of the peptide therapeutic landscape is provided, including historical perspectives, molecular characteristics, regulatory benchmarks, and a therapeutic area breakdown, which includes over 150 peptides in active development today.
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The Current State of Peptide Drug Discovery: Back to the Future?

TL;DR: An emphasis is placed on describing research efforts to overcome the inherent weaknesses of peptide drugs, in particular their poor pharmacokinetic properties, and how these efforts have been critical to the discovery, design, and subsequent development of novel therapeutics.
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Native Chemical Ligation and Extended Methods: Mechanisms, Catalysis, Scope, and Limitations

TL;DR: The most relevant properties of peptide thioesters, Cys peptides, and common solvents, reagents, additives, and catalysts used for these ligations are presented and the various thiol-based auxiliaries and thiol or selenol amino acid surrogates that have been developed so far are discussed.
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Sustainability Challenges in Peptide Synthesis and Purification: From R&D to Production

TL;DR: The current challenges of peptide synthesis and purification in terms of sustainability are summarized, possible solutions are highlighted, and synergies between academia, the pharmaceutical industry, and contract research organizations/contract manufacturing organizations are encouraged.
Journal ArticleDOI

Therapeutic peptides: current applications and future directions

TL;DR: This review summarizes the efforts and achievements in peptide drug discovery, production, and modification, and their current applications and discusses the value and challenges associated with future developments in therapeutic peptides.
References
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TL;DR: The surface of nucleosomes is studded with a multiplicity of modifications that can dictate the higher-order chromatin structure in which DNA is packaged and can orchestrate the ordered recruitment of enzyme complexes to manipulate DNA.
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Protein Misfolding, Functional Amyloid, and Human Disease

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Solid phase peptide synthesis utilizing 9‐fluorenylmethoxycarbonyl amino acids

TL;DR: The great variety of conditions under which Fmoc solid phase peptide synthesis may be carried out represents a truly "orthogonal" scheme, and thus offers many unique opportunities for bioorganic chemistry.
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Peptide therapeutics: current status and future directions.

TL;DR: The current status, strengths, and weaknesses of peptides as medicines and the emerging new opportunities in peptide drug design and development are discussed.
Journal ArticleDOI

The diverse functions of histone lysine methylation.

TL;DR: Recent advances in understanding of how lysine methylation functions in these diverse biological processes are summarized, and questions that need to be addressed in the future are raised.