Synonym |
(D-Phe12,Leu14)-Bombesin |
Species |
Human |
Protein Accession |
P07492 |
Purity |
Greater than 95% as determined by RP-HPLC and SDS-PAGE analysis |
Endotoxin Level |
Less than 1 EU/ug |
Biological Activity |
Binding potency for the receptor is in low nM range. |
Expression System |
E. coli |
Fusion Tag |
His tag at N-terminus |
Predicted Molecular Mass |
Approximately 2.4 kDa |
Formulation |
Lyophilized from a 0.2 µm filtered solution of 20mM PB, 150mM NaCl, pH 7.0 |
Reconstitution |
It is recommended to reconstitute the lyophilized peptide in water or 1x PBS |
Storage & Stability |
Store lyophilized peptide at -20°C. Aliquot and store the product at -20°C for long term. After
reconstitution, the product is stable for several weeks at 4°C or at -20°C for longer periods.
Avoid repeated freezing and thawing cycles. |
FAQ
What is (D-Phe12,Leu14)-Bombesin and how does it work in the body?
(D-Phe12,Leu14)-Bombesin is a
synthetic analog of the naturally occurring peptide known as bombesin. Bombesin is a peptide that was
originally isolated from the skin of the European fire-bellied toad and has since been found to play a
critical role in various physiological processes in mammals, including humans. This peptide functions as
a neurotransmitter and neuromodulator, interacting with bombesin-related receptors present throughout
the body. Specifically, it binds to the gastrin-releasing peptide receptor (GRPR), as well as the
neuromedin B receptor (NMBR).
In the human body, bombesin and its analogs influence a wide array
of biological systems, including the regulation of gastrointestinal functions, the release of hormones,
and the modulation of neuronal responses. The presence of bombesin receptors in the gastrointestinal and
central nervous systems indicates the peptide's role in processes such as regulating gastric acid
secretion, gastrointestinal motility, and even certain aspects of appetite and satiety. Furthermore,
bombesin receptors have been identified in certain types of cancer cells, suggesting a role in tumor
growth and proliferation.
(D-Phe12,Leu14)-Bombesin is structurally modified to enhance its
stability and activity. The specific modifications—replacement of phenylalanine with D-Phe at position
12 and leucine at position 14—help in increasing the half-life of the peptide by making it less
susceptible to enzymatic degradation. This increased stability allows for more prolonged and effective
interaction with receptors, offering a greater potential for therapeutic applications. Research has
highlighted its potential utility in diagnostic or therapeutic imaging, particularly in oncological
settings, where it can help identify and target GRPR-positive tumors.
Furthermore, the analog's
affinity for bombesin receptors makes it a valuable tool in scientific studies examining receptor
behavior and signal transduction pathways in different cell types. By utilizing
(D-Phe12,Leu14)-Bombesin, researchers can gain insights into the basic mechanisms of peptide-receptor
interactions and possibly uncover new therapeutic targets. Thus, (D-Phe12,Leu14)-Bombesin is a compound
of significant interest due to its multifaceted role in biological research and potential therapeutic
applications.
What research has been conducted on (D-Phe12,Leu14)-Bombesin for cancer detection
and treatment?
Research into (D-Phe12,Leu14)-Bombesin as a tool for cancer detection and
treatment has been ongoing, with studies highlighting its promising potential, particularly in targeting
prostate and breast cancer. The analog's affinity for the gastrin-releasing peptide receptor (GRPR),
which is overexpressed in several types of cancers, forms the basis for its utility in oncology. This
high degree of receptor specificity allows for the targeted delivery of radioisotopes or
chemotherapeutic agents, providing a method for both imaging and treatment.
Preclinical studies
have demonstrated that (D-Phe12,Leu14)-Bombesin can be radiolabeled with isotopes such as Indium-111 or
Technetium-99m, facilitating the imaging of GRPR-positive tumors via positron emission tomography (PET)
or single photon emission computed tomography (SPECT). These imaging modalities allow clinicians to
visualize tumors in real-time, providing critical information regarding tumor localization, size, and
potential metastasis. Such imaging techniques can be instrumental in robust tumor detection, staging,
and monitoring therapeutic responses, thus playing a significant role in personalized cancer
care.
In terms of treatment, the high receptor affinity of (D-Phe12,Leu14)-Bombesin offers
possibilities for therapeutic interventions through peptide receptor radionuclide therapy (PRRT). This
approach involves coupling the bombesin analog to a radioactive compound that can deliver targeted
cytotoxic radiation to the cancer cells, minimizing damage to surrounding healthy tissues. Experimental
models have shown that this strategy can effectively reduce tumor size and proliferation in
GRPR-expressing tumors.
Additionally, studies are looking into the application of
(D-Phe12,Leu14)-Bombesin as a vector for delivering chemotherapeutic drugs directly to tumors,
potentially enhancing the efficacy of traditional cancer treatments while reducing systemic toxicity.
The peptide's ability to specifically target GRPR-expressing cells makes it an ideal candidate for such
directed therapies, which remain a focal point of research efforts aiming to improve cancer treatment
outcomes.
While human trials are necessary to fully establish the safety and effectiveness of
(D-Phe12,Leu14)-Bombesin in clinical settings, preliminary data from in vitro and in vivo studies
provides a solid foundation for further exploration. The integration of this analog into cancer
diagnostic and therapeutic protocols holds promise for advancing precision medicine, offering targeted,
less invasive, and more accurate oncological care.
How is (D-Phe12,Leu14)-Bombesin utilized in
scientific research outside of oncology?
Beyond its applications in oncology,
(D-Phe12,Leu14)-Bombesin serves as an invaluable research tool in various scientific disciplines owing
to its interaction with the body's bombesin receptors. The peptide’s ability to bind potently and
specifically to these receptors allows researchers to explore a wide range of physiological and
pathological processes.
One significant area of study is the investigation of the central nervous
system. Bombesin and its analogs play neuromodulatory roles and are implicated in behavior modulation,
stress responses, and appetite regulation. (D-Phe12,Leu14)-Bombesin can be employed in experimental
models to analyze these neural pathways, helping to elucidate the mechanisms through which bombesin
influences neurological processes. This research is crucial in understanding conditions such as obesity,
anxiety, and depression, potentially unveiling new therapeutic targets for managing these
disorders.
Additionally, the analog is utilized in gastrointestinal studies to examine its
effects on gastric functions like digestive motility and hormone release, as well as its potential
influence on the gut-brain axis. The understanding of such interactions can contribute significantly to
gastroenterology, especially concerning disorders related to gastrointestinal motility and function. By
modulating these actions or blocking specific receptor pathways, new treatments might be developed for
conditions such as irritable bowel syndrome and chronic indigestion.
Moreover, in endocrinology,
(D-Phe12,Leu14)-Bombesin can serve as a tool to explore how bombesin receptors on endocrine cells affect
hormone release and action. The receptor's presence in tissues involved in energy metabolism and
regulation opens avenues for studying metabolic syndromes and their treatments.
Research
applications extend into developmental biology as well, where bombesin-like peptides have shown
influences on cell proliferation and differentiation. Understanding these processes can provide insights
into developmental disorders and potential regenerative medicine applications.
Due to its
stability and high receptor affinity, (D-Phe12,Leu14)-Bombesin is a valuable component in receptor
binding assays, proteomics, and molecular imaging, and serves as a model for studying peptide
modification effects on receptor interaction. Its diverse applications demonstrate its utility across
multiple domains, contributing to a better grasp of physiological regulation and pathology and offering
perspectives that may foster novel therapeutic approaches.
What potential benefits does
(D-Phe12,Leu14)-Bombesin offer in personalized medicine?
Personalized medicine revolves around
the customization of healthcare, with medical decisions and treatments tailored to the individual
patient. (D-Phe12,Leu14)-Bombesin stands out as a potential asset in this realm due to its specificity
for the gastrin-releasing peptide receptor (GRPR), which is variably expressed among patients and
associated with different disease states.
One of the primary benefits of (D-Phe12,Leu14)-Bombesin
in personalized medicine is its role in targeted cancer therapies. In patients whose tumors express high
levels of GRPR, this analog can be utilized for precise tumor imaging and, when attached to cytotoxic
agents or radiotherapeutics, for specific targeting of cancer cells. This tailored approach can optimize
treatment efficacy while minimizing the adverse effects typically associated with conventional
chemotherapy and radiotherapy.
Moreover, such targeted therapies can be adjusted based on the
receptor expression levels in individual patients’ tumors, ensuring an optimal therapeutic window.
Personalized approaches employing (D-Phe12,Leu14)-Bombesin can lead to better patient outcomes by
concentrating treatment exactly where it's needed and by potentially reducing the overall treatment
burden on healthy tissues.
Additionally, the use of (D-Phe12,Leu14)-Bombesin in diagnostics can
aid in the more precise characterization of a given patient's disease state. Molecular imaging
techniques that leverage this analog allow for a detailed view of receptor expression, which can inform
treatment decisions—from identifying suitable candidates for receptor-targeted therapies to monitoring
responses to such interventions.
Furthermore, in non-oncological applications, its role in
studying neural pathways and gastrointestinal functions can provide insights into individual variations
in receptor activity, influencing personalized treatment strategies for neurological and digestive
diseases. As researchers continue to map out the individual variations in bombesin receptor distribution
and expression, the data gleaned from studies involving (D-Phe12,Leu14)-Bombesin can help inform more
precise, individualized medication regimens for these complex conditions.
Ultimately,
(D-Phe12,Leu14)-Bombesin offers significant promise for advancing personalized medicine through its
capability for receptor-targeted diagnostics and treatments. This potential is underscored by its
capacity to refine therapeutic specificity and efficacy on a patient-by-patient basis, heralding an era
where the one-size-fits-all approach is augmented by individualized, receptor-guided treatment
strategies. Although more clinical research is needed, the incorporation of (D-Phe12,Leu14)-Bombesin
into personalized medicine paradigms could significantly enhance healthcare outcomes and patient
experience.
Are there any known side effects or risks associated with (D-Phe12,Leu14)-Bombesin
usage?
Understanding potential side effects or risks associated with (D-Phe12,Leu14)-Bombesin is
critical for both researchers and clinicians who anticipate using this compound in clinical and
experimental settings. Like any peptide or biologically active compound, its interactions within human
biological systems must be carefully evaluated to ensure safety and efficacy.
The primary concern
with (D-Phe12,Leu14)-Bombesin lies in its interaction with the bombesin receptor family, which, although
providing the therapeutic and diagnostic benefits, also entails the possibility of unintended
physiological effects. Given the widespread distribution of bombesin receptors, off-target effects can
occur, impacting systems where these receptors play regulatory roles, such as within the central nervous
system or gastrointestinal tract. Such effects might translate into nausea, changes in appetite, or
disturbances in gastrointestinal motility, mirroring some natural bombesin effects.
When
(D-Phe12,Leu14)-Bombesin is used for imaging or therapeutic purposes, especially when conjugated with
radioisotopes or chemotherapeutic agents, the risks can also extend to those compounds. Radiolabeled
therapies, while offering targeted treatment, carry inherent risks associated with radiation, including
potential damage to non-targeted tissues and long-term radiation exposure effects. Radiopharmaceuticals
typically necessitate stringent safety protocols and monitoring to mitigate such
risks.
Additionally, allergic reactions or immune responses to peptide-based compounds represent
another risk. Although peptides are generally less likely to provoke significant immune responses
compared to larger proteins, individual sensitivity can vary. Rare allergic reactions might pose
concerns, particularly in sensitive individuals or those with pre-existing allergic
conditions.
Due to these possibilities, (D-Phe12,Leu14)-Bombesin should ideally be used within
controlled research settings or closely monitored clinical conditions, where comprehensive assessments
of benefits versus risks are conducted. Rigorous preclinical and clinical testing phases are essential
to ascertain its safety profile, therapeutic windows, and potential contraindications before broader
usage.
In conclusion, while (D-Phe12,Leu14)-Bombesin holds considerable promise due to its role
as a targeted diagnostic and therapeutic tool, attention to possible side effects and risks is
paramount. Researchers and healthcare providers should maintain vigilance by staying informed of
emerging data on the compound's safety and by observing standard protocols designed to prevent or manage
adverse events. As with any novel medical intervention, its ultimate integration into clinical and
functional settings mandates a thorough understanding and consideration of its complete side effect
profile.