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What Are Peptides - Their Functions, Advantages & Where Are They Used?

May 16, 2024

What are peptides?

Peptides are short chains of amino acids, which are the fundamental building blocks of proteins. Amino acids are organic molecules characterized by the presence of an amino group (-NH2) and a carboxyl group (-COOH), as well as a distinctive side chain unique to each amino acid. When amino acids link together through peptide bonds, they form peptides. Peptides are smaller than proteins and typically consist of fewer than 50 amino acids, whereas proteins are longer chains with more than 50 amino acids.

What are different types of peptides?

Peptides exhibit a diverse array of types delineated by their origins, functions, and lengths. Here’s an in-depth exploration of the various categories of peptides:

Endogenous Peptides: Exogenous peptides refer to those that are either artificially synthesized or sourced naturally, which may involve processes such as enzymatic protein degradation, biosynthesis, or organic synthesis methods.

Exogenous Peptides: Exogenous peptides are either synthetically manufactured or derived from natural sources such as enzymatic hydrolysis of proteins, biosynthesis, or organic synthesis. They manifest in different amino acid chain lengths and can stem from botanical or zoological origins.

 

Classification by Length:

Dipeptides: Comprising two amino acids, dipeptides represent a fundamental building block in peptide structures.

Oligopeptides: Consisting of a modest number of amino acids, oligopeptides encompass a varied spectrum of sequences.

Polypeptides: Ranging between 20 to 50 amino acids, polypeptides represent an intermediate length within the peptide hierarchy.

Functional Peptides:

Skin-Repairing Peptides: These peptides specialize in rejuvenating and repairing the skin’s integrity, aiding in wound healing and promoting overall skin health.

Signaling Peptides: Tasked with regulating protein synthesis within the skin, signaling peptides can either stimulate or inhibit specific protein formations crucial for skin vitality.

Carrier Peptides: Facilitating the transportation of essential trace elements pivotal for wound healing, carrier peptides play a vital role in nurturing skin health.

Enzyme-Inhibiting Peptides: These peptides serve as inhibitors against enzymes like tyrosinase and matrix metalloproteinase, effectively mitigating skin darkening and preventing tissue degradation.

Neurotransmitter-Inhibiting Peptides: By acting on neurotransmitter pathways, these peptides help modulate neuronal activity and influence various physiological processes.

Antimicrobial Peptides: Exhibiting potent antimicrobial properties, these peptides combat microbial proliferation on the skin’s surface, contributing to overall skin health and hygiene.

Where Are Peptides Used?

Peptide Therapy: Peptides find application in modifying or augmenting specific bodily functions. For instance, athletes utilize growth hormone-releasing peptides to expedite recovery post intense training sessions.

Peptide Supplements: Peptides are available in the form of dietary supplements, including pills or protein shakes. These supplements offer benefits such as muscle augmentation, skin enhancement, and weight management.

Peptides in Food: Naturally occurring peptides abound in foods rich in amino acids. They play indispensable roles in various bodily functions, contributing to skin health, muscle development, and weight regulation.

Peptide Drugs: With over 100 peptide drugs FDA-approved, conditions like prostate cancer, HIV, multiple myeloma, and diabetes find effective treatments. These drugs, synthesized artificially, stand as potent remedies for an array of disorders.

What are the functions of Peptides?

Hormones and Growth Factors: Peptide hormones, exemplified by vasopressin, play pivotal roles in regulating blood pressure and inducing aldosterone release from the adrenal cortex, facilitating sodium retention.

Antioxidants: Peptides exhibit antioxidant properties, effectively scavenging free radicals and safeguarding cells against oxidative stress-induced damage.

Antibacterial Activity: Certain peptides demonstrate antibacterial efficacy, aiding in the eradication of microbial populations on the skin and promoting skin health.

Structural Integrity: Elongated peptide chains contribute to the formation of structural proteins, offering crucial support and stability to bodily tissues.

Hypersecretion as Diagnostic Marker: Excessive peptide secretion in urine serves as an indicator for specific mental health disorders, such as schizophrenia and depression, aiding in diagnostic procedures.

Nutritional Supplements: Peptides are integral components of health and fitness supplements, notably collagen supplements that target skin health and anti-aging effects.

Dietary Additives: Collagen peptides, incorporated into dietary supplements, bolster skin elasticity and hydration, offering holistic skincare benefits.

What are the potential therapeutic applications of peptides?

Peptides have emerged as invaluable therapeutic agents, offering a myriad of medical and biotechnological applications. Here are key insights gleaned from the provided research findings:

Medical Utilizations: Peptides find applications across a diverse array of therapeutic domains, spanning urology, respiratory medicine, pain management, oncology, metabolic disorders, cardiovascular ailments, and antimicrobial interventions. With over 170 peptides currently undergoing clinical development, their expansive therapeutic potential is evident.

Advantages Over Conventional Molecules: Peptides boast favorable pharmacological attributes, including heightened specificity, enhanced tolerability, and heightened efficacy in human subjects compared to traditional small molecules. Despite past challenges such as susceptibility to degradation and limited target specificity, ongoing advancements in processing methodologies have bolstered their therapeutic utility significantly.

Peptide Drug Innovation: Recent years have witnessed a notable surge in peptide drug development, driven by breakthroughs in structural biology, recombinant biologics, and synthetic methodologies. These technological advancements have streamlined the fabrication, customization, and assessment of peptides for therapeutic purposes.

Therapeutic Versatility: Peptides play pivotal roles in combatting aging, augmenting muscle growth and recuperation, fostering skin revitalization, enhancing sexual vitality and performance, and fortifying overall health and wellness. They offer a wide spectrum of health-enhancing benefits across diverse therapeutic realms.

What are the challenges in developing peptide drugs?

Proteolytic Instability: Peptides are inherently susceptible to proteolytic degradation, rendering them more prone to enzymatic breakdown compared to small molecules. This instability can compromise their bioavailability and therapeutic efficacy.

Bioavailability Limitations: Peptides often exhibit poor oral bioavailability due to their susceptibility to enzymatic degradation and limited ability to traverse biological membranes. These factors hinder their absorption into systemic circulation, constraining their therapeutic potential.

Pharmacokinetic Constraints: Peptides typically possess suboptimal pharmacokinetic properties characterized by rapid clearance from the body and short plasma half-lives. These pharmacokinetic limitations pose challenges in maintaining therapeutic concentrations of peptides within the body for extended durations.

Cost Considerations: The production costs associated with peptides can be relatively high compared to small molecule drugs, primarily due to the complexity of peptide synthesis and purification processes. This elevated cost of production may limit the economic viability of peptide-based therapeutics.

Delivery Challenges: Delivering peptides to the target site of action can be challenging owing to their large molecular size and susceptibility to enzymatic degradation. Overcoming these delivery hurdles while ensuring targeted delivery remains a significant challenge in peptide drug development.

Regulatory Complexity: Peptides are subject to stringent regulatory requirements, particularly in the United States, where they are regulated as drugs. Navigating the regulatory landscape adds complexity and cost to the development process, posing additional challenges to bringing peptide drugs to market.

How to overcome these challenges?

Chemical Synthesis: Employing chemical peptide synthesis methods or enzymatic synthesis to produce peptides as active pharmaceutical ingredients can improve their stability and bioavailability, mitigating issues associated with proteolytic degradation.

Solid-Phase Peptide Synthesis (SPPS): Implementing SPPS techniques, such as a catch-and-release strategy, enables the efficient synthesis of linear peptides with high purity. This method involves coupling a chemical linker to the free N-terminal amino group, facilitating the rapid removal of impurities and truncated sequences after peptide cleavage.

Optimization Strategies: Utilizing strategies to directly optimize peptide properties can enhance their therapeutic efficacy. This may involve chemical derivatization techniques like rigidification, substitution or shielding of labile moieties, and incorporation of non-natural amino acids to improve protease stability, circulation half-life, cellular permeability, and oral bioavailability.

Macrocyclic Peptides: Emphasizing the development of macrocyclic peptides has shown promise in overcoming challenges associated with traditional linear peptides. Macrocyclic peptides offer distinct advantages in targeting ‘undruggable’ proteins and broadening the scope of peptide-based therapeutics.

Delivery Enhancements: Exploring innovative drug formulation and delivery approaches can enhance the bioavailability and effectiveness of peptide drugs without altering their fundamental structure. Strategies such as conjugation with cell-penetrating peptides (CPPs) or prodrug approaches aim to improve membrane permeability.

Future Perspectives: Despite existing challenges like limited membrane permeability and oral bioavailability, extensive research is being carried out to surmount these barriers. Advances in understanding how to manipulate these parameters are driving the development of novel strategies that may pave the way for broader acceptance of peptide therapeutics in the future.

Conclusion:

The peptide therapeutics market and peptide manufacturing are on an upward trajectory, driven by increasing demand and innovative solutions to overcome production and delivery challenges.

It is witnessing robust growth and is expected to grow further due to advancements in purification processes, reduced waste generation, and the development of novel peptide synthesis technologies.

With ongoing investment in R&D, the future holds promise for the development of innovative drugs that deliver improved outcomes for patients.

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