Synonym |
Met-Enkephalin-RGL |
Species |
Human |
Protein Accession |
P01210 |
Purity |
Greater than 95% |
Endotoxin Level |
Less than 1 EU/µg |
Biological Activity |
The ED50 of ≤0.5ng/ml |
Expression System |
E. coli |
Fusion Tag |
None |
Predicted Molecular Mass |
5557 Da |
Formulation |
Lyophilized from a 0.2 μm filtered solution of 20mM PB,150mM NaCl, pH7.2. |
Reconstitution |
It is recommended to reconstitute the lyophilized Met-Enkephalin-RGL in sterile 18MΩ-cm H2O not
less than 100µg/ml, which can then be further diluted to other aqueous solutions. |
Storage & Stability |
Store lyophilized protein at -20°C. Aliquot the product after reconstitution to avoid repeated
freezing/thawing cycles. Reconstituted protein can be stored at 4°C for a limited period of
time. The lyophilized protein remains stable until the expiry date when stored at -20°C. |
FAQ
What is Met-Enkephalin-RGL and how does it work in the body?
Met-Enkephalin-RGL is a synthetic
analog of the naturally occurring peptide Met-enkephalin, which is one of the endogenous opioids found
in the body. Enkephalins are part of a broader group of peptides known as endorphins, which play key
roles in modulating pain and producing analgesia. Met-Enkephalin specifically binds to the delta and
mu-opioid receptors in the central nervous system. This binding alters the perception of pain by
inhibiting the release of neurotransmitters involved in the transmission of pain signals, effectively
reducing the sensation of pain. Its potency and specificity for opioid receptors make it an important
peptide for research into pain management and potential therapeutic applications. The addition of RGL, a
modified amino acid sequence, is designed to enhance the peptide’s stability and resistance to enzymatic
degradation. This modification allows it to remain active longer in the body, potentially increasing its
therapeutic benefits and making it more suitable for clinical applications. The improved stability and
activity duration mean that Met-Enkephalin-RGL can be administered less frequently while providing
sustained effects.
In addition to pain modulation, Met-Enkephalin-RGL is also being explored for
its potential effects on the immune system. Research suggests that opioids have immunomodulatory
properties, and Met-Enkephalin-RGL might influence the activity of immune cells, thereby affecting
inflammation and immune response. This dual action on pain and the immune system presents a significant
opportunity for treating conditions that involve chronic pain and inflammation. Furthermore, the
peptide’s potential applications extend beyond just analgesia, including areas such as mood disorders,
stress response, and potentially neurodegenerative diseases, because of its interaction with
neurotransmitter systems in the brain. Although still under investigation, Met-Enkephalin-RGL signifies
a promising pathway in developing advanced therapeutic agents that harness the multifaceted roles of
enkephalins within the physiological and neurological framework.
What are the potential benefits
of using Met-Enkephalin-RGL over traditional pain management methods?
Met-Enkephalin-RGL offers a
variety of potential benefits compared to traditional pain management techniques, primarily due to its
mechanism of action and the nature of its composition. One of the most notable advantages is its
specificity and targeted action on opioid receptors, allowing for more precise modulation of pain
pathways. Traditional pain management often relies on non-steroidal anti-inflammatory drugs (NSAIDs) or
non-specific opioids. While effective, these medications can bring about significant side effects such
as gastrointestinal issues, potential for addiction, or liver toxicity with long-term use.
Met-Enkephalin-RGL, due to its selective activity, may reduce these side effects and offer a safer
profile for long-term management of chronic pain.
Furthermore, Met-Enkephalin-RGL’s modified
structure—enhanced by the RGL sequence—gives it improved stability over time, meaning it can remain
active in the body far longer than naturally occurring enkephalins. By resisting enzymatic breakdown,
this synthetic analog sustains its analgesic effects with less frequent dosing. This increased duration
not only is more convenient for patients but may also lead to better adherence to treatment protocols
with improved overall outcomes. Moreover, unlike common narcotic painkillers, Met-Enkephalin-RGL is
being developed and studied with the aim of minimizing or even avoiding the development of tolerance and
physical dependence. This could be of particular importance when addressing the challenges associated
with opioid addiction and abuse, a significant concern with current opioid use.
In addition to
its role in pain relief, the immunomodulatory effects of Met-Enkephalin-RGL suggest it may concurrently
manage both pain and inflammation, which is not typically achievable with conventional analgesic
treatments. This dual functionality can be particularly valuable in managing conditions such as
rheumatoid arthritis, where both pain and inflammation are constant issues. The combined pain relief and
modulation of the immune response also hold promise for synergistic effects that enhance patient quality
of life. Ongoing research continues to explore these multifaceted benefits, potentially propelling
Met-Enkephalin-RGL toward more widespread clinical application. Ultimately, while requiring further
trials and studies to fully understand and validate its benefits, the peptide's promising profile offers
a glimpse into next-generation pain management solutions.
How does the modification in
Met-Enkephalin-RGL result in enhanced stability compared to natural Met-Enkephalin?
The modification
in Met-Enkephalin-RGL is designed specifically to enhance the peptide's stability, making it a powerful
candidate in therapeutic development. Naturally occurring Met-enkephalin, like many other peptides, is
susceptible to rapid enzymatic degradation in the bloodstream, which can significantly limit its
clinical efficacy. This degradation is primarily carried out by peptidases that break down peptide
bonds, thus inactivating the therapeutic agent. The addition of the RGL sequence in Met-Enkephalin-RGL
is a strategic modification aiming to overcome such limitations and prolong the bioactive lifespan of
the peptide.
The RGL sequence is thought to confer resistance against these enzyme activities,
allowing Met-Enkephalin-RGL to evade premature breakdown. This is achieved through structural
alterations that cause steric hindrance or alter the secondary structure of the peptide, making it a
less suitable substrate for peptidases. Consequently, this modification helps maintain the integrity of
Met-Enkephalin-RGL in the circulatory system, providing a longer duration of action which is highly
beneficial in clinical settings where reduced frequency of dosing is advantageous.
Another aspect
of the enhanced stability is related to improved binding affinity and specificity for opioid receptors.
The modification may simultaneously facilitate better interaction with the target receptors, implying
more pronounced and sustained pharmacological effects. The ability to remain bonded to these receptors
longer means enhanced signal transduction, which translates to more effective alleviation of pain and
modulation of neurological responses. Moreover, this improved receptor interaction contributes to
reduced off-target effects, minimizing potential adverse reactions commonly associated with traditional
opioids and offering a cleaner safety profile.
Additionally, the prolonged bioavailability
derived from enhanced stability does not only improve patient convenience but also potentiates
engagement with downstream signaling pathways linked to opioid receptor activation. This could result in
robust therapeutic outcomes such as sustained analgesia without reaching toxic levels that could
initiate tolerance or dependence. The structural integration provided by modifications like that of the
RGL sequence represents a frontier in peptide drug design, unlocking new possibilities for enhancing the
functionality and therapeutic potential of peptide-based drugs like Met-Enkephalin-RGL beyond what is
feasible with their natural counterparts.
Can Met-Enkephalin-RGL be used for conditions other
than pain management, and if so, how?
Met-Enkephalin-RGL is primarily studied for its analgesic
properties, but its biological activities suggest it could be applicable in a range of other therapeutic
contexts beyond traditional pain management. One area under investigation is its potential role in
managing mood disorders and stress-related conditions, such as depression and anxiety. Endogenous opioid
peptides, including enkephalins, play an intrinsic role in regulating mood and emotional states by
interacting with the neurotransmitter systems in the brain. By modulating these systems,
Met-Enkephalin-RGL may help balance mood levels and alleviate symptoms associated with mood disorders,
offering a novel approach compared to standard treatments like SSRIs.
Additionally, the
immunomodulatory properties of Met-Enkephalin-RGL open the door to its use in managing inflammatory and
autoimmune conditions. By influencing immune cell activity and cytokine production, this peptide could
help regulate inflammatory responses and ameliorate symptoms of autoimmune diseases such as rheumatoid
arthritis and multiple sclerosis. This capacity to modulate the immune system highlights its dual-action
potential, making it a candidate for combined anti-inflammatory and analgesic therapy, a layered
approach often required in complex chronic conditions.
Another promising application lies in the
area of neuroprotection and neurodegenerative diseases. Through its interaction with opioid receptors,
Met-Enkephalin-RGL could exert neuroprotective effects that help slow the progression of
neurodegenerative disorders like Parkinson's or Alzheimer's disease. This potential is based on the
peptide’s ability to mitigate cellular stress responses and modulate pathways related to cellular
survival and apoptosis. While clinical validation is still pending, the incorporation of such peptides
in comprehensive treatment regimens could signal a shift in tackling the multifactorial nature of
neurodegenerative diseases.
Moreover, there is interest in exploring Met-Enkephalin-RGL's role in
addiction therapy. Its design aims to reduce the development of tolerance and dependency, making it a
potentially safer alternative for those seeking relief from substance addiction. By possibly modulating
reward pathways without the same addictive potential as conventional opioids, Met-Enkephalin-RGL could
contribute to strategies aimed at reducing opioid dependence. The development of treatments capable of
addressing withdrawal symptoms and reducing cravings without perpetuating addiction could be a
significant breakthrough.
Met-Enkephalin-RGL's versatility exemplifies the potential of
peptide-based treatments to address a spectrum of conditions, thanks to their specificity, efficacy, and
lower side-effect profiles. Continued research is crucial to fully elucidate its capabilities and pave
the way for innovative therapeutic strategies that leverage its unique properties. While further
clinical trials are needed for these alternative applications, the prospects they represent could
redefine our approach to managing complex and multi-faceted health challenges.
What makes
Met-Enkephalin-RGL a promising candidate for future pharmaceuticals?
Met-Enkephalin-RGL stands out
as a promising candidate in the pharmaceutical landscape due to several intrinsic factors attributed to
its unique composition and mode of action. The peptide leverage on its specificity and potency makes it
a powerful tool in the emerging field of peptide-based therapeutics. Unlike small molecule drugs,
peptides like Met-Enkephalin-RGL offer a high degree of specificity in targeting biological processes.
They can engage with receptors or enzymes with precision, leading to fewer off-target effects and
consequently a lower incidence of adverse reactions. This characteristic is incredibly appealing in drug
development as it aligns with the ongoing demand for safer and more targeted therapies.
Moreover,
Met-Enkephalin-RGL’s enhanced stability and prolonged duration of action represent a significant
advancement in peptide therapeutics. Traditional peptides often suffer from rapid degradation in vivo,
limiting their therapeutic potential. However, by incorporating modifications that confer resistance to
enzymatic breakdown, Met-Enkephalin-RGL overcomes these conventional barriers, offering a sustainable
and effective means of achieving therapeutic effects. The ability to maintain its bioactivity over
extended periods elevates its clinical utility by enabling less frequent dosing schedules, enhancing
patient compliance, and delivering sustained results that improve overall treatment
outcomes.
Another compelling feature of Met-Enkephalin-RGL is its inherent dual-action ability.
As a peptide with effects on both pain and immune response, it encompasses a broad therapeutic window.
The capacity to address multiple pathways or conditions with a single compound is highly sought after in
medicine, particularly for comorbid conditions that commonly require complex treatment regimens. This
attribute positions Met-Enkephalin-RGL as a versatile therapeutic candidate with the potential to
simplify approaches to complex health issues and improve patient quality of life.
Beyond its
current scope, Met-Enkephalin-RGL also reflects a major trend toward personalized medicine. Its design
facilitates adjustment or refinement, allowing custom tailoring to fit specific patient needs or to
enhance its interaction with biological targets. As precision medicine becomes more prevalent, the
adaptability and specificity of peptides like Met-Enkephalin-RGL will play an instrumental role in
creating customized and effective patient-centric therapies.
What's equally fascinating is the
broad potential market that Met-Enkephalin-RGL presents. From pain management to autoimmune conditions,
mood disorders, and potentially neurodegenerative diseases, Met-Enkephalin-RGL could serve a wide array
of medical sectors. Such versatility means it could significantly influence the pharmaceutical industry
by offering a strategic solution that is both effective and economical. Furthermore, given the ongoing
opioid crisis and the urgent need for safer pain management solutions, Met-Enkephalin-RGL could fulfill
a critical gap by providing alternative strategies that target pain without the high risk of
addiction.
The evolution of Met-Enkephalin-RGL outlines a remarkable trajectory in the role of
peptides within modern medicine. As further research and clinical trials unveil its full potential, it
is poised to redefine therapeutic strategies, leading to safer, more effective, and personalized
approaches to a wide range of health challenges.