Synonym |
Boc-Met-Enkephalin-t-butyl ester |
Species |
Human |
Protein Accession |
NA |
Purity |
95% |
Endotoxin Level |
<1.0 EU per 1 µg of protein |
Biological Activity |
NA |
Expression System |
Chemical synthesis |
Fusion Tag |
NA |
Predicted Molecular Mass |
NA |
Formulation |
Supplied as a lyophilized powder |
Reconstitution |
Centrifuge the vial prior to opening. Reconstitute in sterile ddH2O to a concentration of
0.1-1.0 mg/ml. |
Storage & Stability |
Store at -20°C. After reconstitution, store at -20°C or -80°C for long term storage. |
FAQ
What is Boc-Met-Enkephalin-t-butyl ester, and what are its primary applications in
research?
Boc-Met-Enkephalin-t-butyl ester is a synthetic peptide that serves as a biochemical
tool for various research applications, particularly in neuroscience and pharmacology. Structurally, it
is an enkephalin analog, where enkephalins are endogenous peptides with a known role in modulating pain,
stress, and immune responses through their action as agonists for opioid receptors. Enkephalins
influence neurotransmission and can impact mood, making them important for research into conditions like
depression, anxiety, and drug addiction. The Boc (tert-butyloxycarbonyl) group in its name refers to a
protective group often used in peptide synthesis to prevent side reactions, while the "t-butyl ester"
suffix indicates a modification for enhancing the molecule's stability and solubility, facilitating its
use in various experimental conditions.
Research involving Boc-Met-Enkephalin-t-butyl ester spans
multiple areas. In neuroscience, it is frequently used in the study of pain pathways, given its capacity
to mimic natural enkephalins and interact with receptor sites involved in pain perception and
management. Understanding these pathways can lead to the development of new analgesics and treatments
for chronic pain conditions. In pharmacology, using such a synthetic peptide can clarify the effects of
opioid receptor activation and help describe the pharmacodynamics of other opioid-related agents.
Additionally, because opioid receptors are also involved in reward pathways, there is potential for this
compound to contribute to addiction research, offering insights into how addictive behaviors can be
mitigated through biochemical intervention.
Besides direct applications, this peptide is valuable
in assay development. Variations in binding affinities, receptor subtype selectivity, and downstream
signaling pathways can all be analyzed using Boc-Met-Enkephalin-t-butyl ester, providing a clearer
understanding of these molecular interactions. Finally, beyond neuroscience, this peptide's modification
and stability features promote its use in structural biology, enabling researchers to elucidate the
three-dimensional structures of receptor-peptide complexes through techniques like X-ray crystallography
or NMR spectroscopy, potentially identifying new therapeutic targets or advancing drug design
processes.
How does Boc-Met-Enkephalin-t-butyl ester contribute to opioid receptor
studies?
Boc-Met-Enkephalin-t-butyl ester plays a critical role in investigating opioid
receptors' function due to its structure as an enkephalin analog. Opioid receptors, which include mu,
delta, and kappa subtypes, are G-protein-coupled receptors (GPCRs) that mediate diverse physiological
effects like pain modulation, mood alteration, and reward mechanisms. The ability of researchers to
study these receptors is key to advancing our understanding of how drugs like morphine and other opioids
exert their effects, providing insight into more effective and safer therapeutic options.
Boc-Met-Enkephalin-t-butyl ester is particularly useful because it can selectively interact with these
receptors, reproducing the activity of naturally occurring enkephalins.
One major contribution of
this peptide to opioid receptor studies is its use in binding assays. By acting as a ligand that binds
to opioid receptors, Boc-Met-Enkephalin-t-butyl ester can help determine binding affinities and specific
activities of receptor subtypes, ultimately clarifying receptor-ligand interactions. This information is
crucial for distinguishing the various effects elicited by different opioid receptor subtypes, guiding
the development of receptor-selective drugs that may offer therapeutic benefits with reduced adverse
effects.
Additionally, the compound is valuable for signal transduction analyses. When
Boc-Met-Enkephalin-t-butyl ester binds to an opioid receptor, it triggers a cascade of intracellular
signaling events, primarily through G-protein pathways. Understanding these pathways provides insights
into how opioid receptors regulate physiological processes and how different ligands may influence these
pathways variously. This can be important for identifying molecular mechanisms responsible for the
diverse effects of drugs targeting these receptors, enabling the design of compounds with enhanced
efficacy and safety profiles.
Boc-Met-Enkephalin-t-butyl ester also supports research into
receptor dimerization, where two receptor units interact to alter functionality. Such dimerizations can
influence the pharmacology and signaling properties of opioid receptors. Using specific enkephalin
analogs like Boc-Met-Enkephalin-t-butyl ester helps illuminate these interactions, providing
foundational knowledge for novel approaches in drug development. Overall, the peptide stands as a
valuable tool in the precise characterization of opioid receptor activity, which is indispensable for
drug discovery and development efforts targeting receptor-mediated conditions.
What are the
benefits of using a modified enkephalin like Boc-Met-Enkephalin-t-butyl ester in experimental
settings?
The use of modified enkephalins, such as Boc-Met-Enkephalin-t-butyl ester, offers
numerous benefits in experimental settings, particularly within the fields of biochemistry,
pharmacology, and neuroscience. Modifying enkephalins with protective groups and esterification enhances
certain properties of the peptide, providing significant advantages for research
applications.
Firstly, one of the primary benefits is improved stability. Naturally occurring
peptides are often susceptible to enzymatic degradation, which can limit their effectiveness and
consistency in experiments. The modification in Boc-Met-Enkephalin-t-butyl ester, particularly the Boc
protective group and the t-butyl ester, enhances its resistance to proteolytic enzymes, thereby
prolonging its half-life in biological assays and allowing for more extended observation periods. This
stability is crucial for accurately assessing the peptide’s biological effects and avoiding artifacts
that may arise from rapid degradation.
Secondly, solubility improvements are another significant
advantage. Modified peptides like Boc-Met-Enkephalin-t-butyl ester often exhibit better solubility in
various solvents, facilitating their use in diverse experimental conditions. Enhanced solubility can
ensure more uniform distribution in biological systems, reducing the potential for aggregation and
promoting reliable outcomes in kinetic studies and binding assays.
Furthermore, the inclusion of
protective groups such as Boc allows for the targeted delivery of the peptide within organisms. This
capability can enhance the compound’s selectivity and efficacy at its intended receptor targets, often
resulting in more precise data regarding receptor-ligand interactions and pharmacodynamic properties.
Consequently, researchers can discern subtle differences in receptor functionality that may lead to
innovations in therapeutic development.
Additionally, chemical modifications can enhance these
peptides' selective binding affinity and receptor activation profiles. By tailoring enkephalin analogs,
researchers can create compounds capable of preferentially interacting with specific opioid receptor
subtypes. This selectivity helps delineate the distinct physiological roles and signaling pathways
associated with each receptor subtype, enhancing our understanding of receptor-mediated processes and
leading to safer analgesics and other therapeutic agents.
Finally, using a modified enkephalin
like Boc-Met-Enkephalin-t-butyl ester allows for versatility in its applications. It can be employed in
biochemical assays, animal models, and even structural studies. Its robustness and versatility make it
an attractive choice for academic research and industrial applications, underscoring its importance in
the pursuit of scientific advancement and drug innovation.
How does Boc-Met-Enkephalin-t-butyl
ester facilitate structural biology studies?
Boc-Met-Enkephalin-t-butyl ester is a key compound
in the field of structural biology due to its potential in elucidating the structures of complex
biomolecules such as proteins and receptors. Structural biology aims to understand the molecular
architecture of biomolecules, which is critical for determining their function, interactions, and
therapeutic potential. The structural insights gained using compounds like Boc-Met-Enkephalin-t-butyl
ester are invaluable for advancing drug discovery and biomedical research.
One of the essential
contributions of Boc-Met-Enkephalin-t-butyl ester to structural biology is its ability to stabilize
proteins and receptor complexes during structural analyses. The protective Boc group and ester
modification enhance the peptide's stability, help maintain the integrity of the receptor-peptide
complexes during experiments, and enable detailed structural characterization. Techniques such as X-ray
crystallography, nuclear magnetic resonance (NMR) spectroscopy, and cryo-electron microscopy (cryo-EM)
often rely on such stabilized peptides to generate high-resolution structures.
When used in X-ray
crystallography, Boc-Met-Enkephalin-t-butyl ester can serve as a useful ligand that interacts with
target receptors, aiding in the crystallization process. Successful crystallization of a receptor-ligand
complex is a critical step in obtaining detailed structural information about the receptor's active or
inactive conformations, helping researchers understand how the peptides bind and exert their biological
effects. This knowledge can also highlight potential sites for therapeutic intervention, influencing the
design of more effective drugs with improved affinity and specificity.
NMR spectroscopy benefits
similarly, where Boc-Met-Enkephalin-t-butyl ester's stable interaction with receptor targets provides an
opportunity to study the dynamics and conformational changes within the receptor-ligand complex. By
understanding these dynamic processes, researchers gain insights into the flexibility and allosteric
modulation of receptors, shedding light on the fundamental aspects of receptor functionality and
signaling.
Crystallographic and spectroscopic techniques rely heavily on the ability to isolate
specific interaction sites, which is made possible in part through the use of modified peptides like
Boc-Met-Enkephalin-t-butyl ester. These interactions can highlight residue-specific changes and binding
pockets, guiding the rational design of drugs that selectively alter these sites for therapeutic
benefits.
In summary, Boc-Met-Enkephalin-t-butyl ester serves as an invaluable tool in structural
biology, offering stability and specificity that enhance our capability to elucidate complex molecular
interactions at the atomic level, driving forward the understanding of biological function and drug
development.
What distinguishes Boc-Met-Enkephalin-t-butyl ester in pharmacological research when
compared to natural enkephalins?
In pharmacological research, Boc-Met-Enkephalin-t-butyl ester
distinguishes itself from natural enkephalins due to several critical modifications that enhance its
utility as an investigative tool. These modifications improve its suitability for experimental contexts,
allowing researchers to explore receptor-ligand interactions, physiological effects, and potential
therapeutic applications with greater precision and reliability.
The first and perhaps most
significant distinction is the chemical stability of Boc-Met-Enkephalin-t-butyl ester compared to
natural enkephalins. Natural enkephalins are rapidly degraded by peptidases in vivo, which limits their
effectiveness and makes sustained pharmacological interventions difficult. In contrast,
Boc-Met-Enkephalin-t-butyl ester, by incorporating protective groups like Boc and modifications such as
esterification, exhibits increased resistance to enzymatic breakdown. This added stability not only
makes it easier to handle within laboratory settings but also provides a longer duration of action when
used in various assay systems.
Another key differentiator is receptor selectivity and affinity.
Natural enkephalins interact with mu, delta, and kappa opioid receptor subtypes, but their non-selective
nature can complicate studies aimed at delineating specific receptor-mediated pathways.
Boc-Met-Enkephalin-t-butyl ester, developed as an enkephalin analog, is engineered to explore these
receptor interactions with greater selectivity. This characteristic is vital for studies focused on
understanding the distinct physiological effects mediated by each opioid receptor subtype, leading to
more targeted therapeutic interventions and reducing adverse effects typically associated with
non-selective agonists.
Moreover, the solubility profile of Boc-Met-Enkephalin-t-butyl ester is
enhanced relative to natural enkephalins. The increased solubility ensures it can be utilized in a
broader range of experimental conditions, both in vitro and in vivo. This characteristic is particularly
useful in drug screening and pharmacokinetic studies, where maintaining consistent compound
concentration and distribution is crucial for obtaining reliable data.
Additionally,
Boc-Met-Enkephalin-t-butyl ester can be used as a versatile tool in structural studies. Its enhanced
stability and specificity support the formation of receptor-ligand complexes essential for
high-resolution structural elucidation through techniques such as X-ray crystallography and NMR
spectroscopy. These structural insights are central to advancing our understanding of receptor
architecture and function, which informs rational drug design processes.
By providing a synthetic
derivative that maintains key characteristics of natural enkephalins while addressing their limitations,
Boc-Met-Enkephalin-t-butyl ester greatly enhances the scope and depth of pharmacological research into
opioid receptors and related physiological processes.
What are the safety considerations and
handling guidelines for Boc-Met-Enkephalin-t-butyl ester in a laboratory setting?
When working
with synthetic peptides such as Boc-Met-Enkephalin-t-butyl ester, adhering to safety guidelines and
proper handling protocols is paramount to ensuring researcher safety and experimental integrity.
Although Boc-Met-Enkephalin-t-butyl ester is typically handled in a laboratory context under controlled
conditions, it is vital to recognize potential risks and implement measures to mitigate them
effectively.
First and foremost, laboratory personnel should be thoroughly acquainted with the
material safety data sheet (MSDS) associated with Boc-Met-Enkephalin-t-butyl ester. The MSDS provides
detailed information about the peptide's physical and chemical properties, potential hazards, handling
and storage requirements, and first-aid procedures. It serves as an essential resource for understanding
how to manage risks associated with this compound.
Personal protective equipment (PPE) is a
crucial component in minimizing exposure to potentially hazardous substances. When handling
Boc-Met-Enkephalin-t-butyl ester, lab personnel should wear appropriate PPE, including gloves, lab
coats, and safety goggles, to prevent skin and eye contact. Always ensure that materials such as gloves
are rated for chemical resistance against the solvent or buffer systems used in conjunction with the
peptide.
Proper storage of Boc-Met-Enkephalin-t-butyl ester is another significant safety
consideration. The peptide should be stored following the manufacturer's guidelines, generally in a
cool, dry place or at specific temperatures (such as refrigerated or frozen) to maintain its stability
and effectiveness. Keeping it in airtight containers will prevent moisture uptake and potential
degradation.
Handling Boc-Met-Enkephalin-t-butyl ester also involves using appropriate
containment measures to avoid inhalation or ingestion. While working with powdered forms of the peptide,
using a fume hood is advisable to limit inhalation exposure. Moreover, the laboratory environment should
be well-ventilated, and no food or drink should be present to prevent accidental ingestion.
Spill
management protocols are essential, too. In case of a spill, it is crucial to contain and clean it
immediately using appropriate absorbent materials and following the procedures outlined in the MSDS.
Dispose of waste materials in compliance with institutional regulations and environmental safety
standards.
Finally, all personnel must be appropriately trained in emergency response procedures,
including the operation of safety showers and eyewash stations. It is advisable for labs to regularly
conduct safety drills to ensure readiness in case of accidental exposure or chemical spills.
By
respecting these safety guidelines and handling protocols, researchers can minimize risks and ensure a
safe environment when working with Boc-Met-Enkephalin-t-butyl ester, enabling focused and efficient
progression in experimental endeavors.