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Cyclic Peptides as Therapeutics: A New Frontier in Drug Development 作者:JS Choi·2019·被引用次数:126—Notable progress has been made in thetherapeuticand research applications ofcyclic peptidessince our previous review. Newdrugsbased oncyclic peptides

:Cyclic Peptides as Drugs

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Cyclic Peptide 作者:JS Choi·2019·被引用次数:126—Notable progress has been made in thetherapeuticand research applications ofcyclic peptidessince our previous review. Newdrugsbased oncyclic peptides

Cyclic peptides are emerging as a powerful and versatile class of molecules in the realm of drug development, offering significant advantages over traditional linear peptides and small molecules. Their unique structural characteristics, including enhanced stability and improved binding affinity, position them as promising therapeutic agents for a wide range of diseases. This article delves into the current status, future prospects, and key considerations for utilizing cyclic peptides in therapeutics.

The inherent nature of peptides, which are short chains of amino acids, often limits their effectiveness as drugs due to their susceptibility to enzymatic degradation and poor pharmacokinetic properties. However, the process of cyclization—where the linear peptide chain forms a ring structure—imparts crucial properties that make them highly attractive for drug discovery. This macrocycle formation can occur through various linkages, such as head-to-tail, side-chain to side-chain, or side-chain to terminus. These structural modifications significantly enhance the potency, stability, and pharmacokinetic properties of cyclic peptide drugs.

Numerous naturally derived cyclic peptides, or their synthetic derivatives, are already established as therapeutics. Prominent examples include hormones like oxytocin, which is a well-known peptide drug. Furthermore, octreotide, a synthetic analogue of somatostatin, is widely applied in the treatment of acromegaly and neuroendocrine tumors. These successes underscore the long-standing utility of cyclic peptides in therapy.

The appeal of cyclic peptides extends to their potential to target intracellular proteins and address diseases that have historically been challenging for conventional small-molecule drugs. Recent research highlights the development of de novo development of small cyclic peptides specifically designed to interact with intracellular targets, opening up new avenues for peptide therapeutic development. This represents a significant shift in how we approach treating complex diseases.

The field of cyclic peptides in drug development is experiencing rapid advancement. Several research groups and companies are actively engaged in discovering and developing novel cyclic peptide therapeutics across multiple therapeutic areas. This includes their application in cancer treatment, where cyclic peptides have demonstrated significant therapeutic abilities in both *in vitro* and *in vivo* studies. The ability to design cyclic peptides with specific structural features allows for tailored interactions with disease-specific targets, making them a versatile tool for oncological therapies.

Comparisons of cyclic peptide therapeutics with classical small molecules reveal distinct advantages. The inherent specificity and affinity of peptides, combined with the enhanced stability conferred by cyclization, can lead to more targeted and effective treatments with potentially fewer off-target effects. This makes them a powerful instrument for advancing medical science.

The journey of cyclic peptides in therapeutics spans from their past discoveries to their present applications and future potential. The continued evolution of peptide therapeutics promises a future where cyclic peptides play an even more central role in treating a wide array of conditions. Efforts are being made to develop synthetic cyclic peptides with improved properties, further expanding their therapeutic utility.

Emerging therapies utilizing cyclic peptides are also being explored for various conditions. The comparison of cyclic peptide therapeutics with other drug modalities consistently shows their unique strengths. The cyclization process itself enables peptides to gain properties that are highly beneficial in drug discovery and development.

In conclusion, cyclic peptides represent a transformative class of therapeutics with immense potential. Their structural advantages, proven efficacy in existing drugs, and ongoing innovation in their design and application position them at the forefront of therapeutic innovation. As research progresses, we can anticipate a future where cyclic peptide drugs become increasingly integral to modern medicine, offering novel solutions for unmet medical needs.

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Additionally, utilizing combination therapies with other drug classes may further elevate the efficacy ofcyclic Peptide Therapeutics. Tips: 
Cyclic Peptides as Therapeutic Agents and Biochemical Tools
Comparisons ofcyclic peptide therapeuticswith other drug modalities. Cyclisation enables peptides to gain properties that are beneficial in drug discovery.
作者:X Jing·2020·被引用次数:184—Over the past decades, more than 40cyclic peptide drugshave been clinically approved Peptides, Cyclic / therapeutic use*. Substances. Peptides, Cyclic.

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