Synonym |
(D-Phe12)-Bombesin |
Species |
Human |
Protein Accession |
P07492 |
Purity |
95% |
Endotoxin Level |
<1.0 EU per 1 μg of the protein |
Biological Activity |
Measured by its ability to elevate intracellular calcium levels in A431 human epithelial
carcinoma cells. The ED50 for this effect is typically 4-20 ng/mL. |
Expression System |
E. coli |
Fusion Tag |
N/A |
Predicted Molecular Mass |
1610 Da |
Formulation |
Lyophilized from a 0.2 μm filtered solution in Acetonitrile and TFA |
Reconstitution |
Centrifuge the vial prior to opening. Reconstitute in 5% acetonitrile in water to a
concentration of 0.1-1.0 mg/mL. Do not vortex. |
Storage & Stability |
Store at -20°C. Store under desiccating conditions. |
FAQ
What is (D-Phe12)-Bombesin, and what are its primary applications in research and
medicine?
(D-Phe12)-Bombesin is a potent analogue of Bombesin, a tetradecapeptide with a
significant role in physiological processes. It primarily interacts with specific G-protein coupled
receptors, including GRP-R, which makes it a valuable tool for researchers studying the intricate
workings of cell growth, cancer development, and neurobiology. (D-Phe12)-Bombesin has been chemically
altered to include a D-Phe at the twelfth position, enhancing its binding properties and stability
within biological systems. This alteration is crucial for developing more refined research models,
allowing scientists to explore cellular mechanisms with improved accuracy. One of the most profound
applications of (D-Phe12)-Bombesin is in cancer research. The high affinity for GRP receptors, which are
found in abundance on several cancer cell types like prostate, small cell lung cancer, and breast cancer
cells, makes (D-Phe12)-Bombesin a powerful tool for targeted imaging and therapeutic research. By using
this peptide in various assays, researchers can better understand tumor progression, metastasis, and
receptor-mediated signaling pathways. Moreover, (D-Phe12)-Bombesin serves as a guiding compound in
developing radiolabeled peptides for diagnostic purposes and targeted cancer therapy. In these contexts,
radiolabels enable the visualization of tumor sites within the body when paired with suitable imaging
technology like PET or SPECT.
Furthermore, such compounds can also help deliver therapeutic
radiation specifically to tumor sites, minimizing damage to surrounding healthy tissues. Aside from
cancer, (D-Phe12)-Bombesin is also used to explore neurobiological activities. Bombesin-like peptides
are linked to several central nervous system processes, including appetite regulation, circadian rhythm,
thermoregulation, and nociception. Using this analogue allows scientists to assess receptor functions
and signaling more precisely in the brain, propelling forward our understanding of neuropharmacology and
potential therapeutic targets for neurological disorders. As a research tool, its utility is
indispensable for data generation leading to therapeutic innovation. Therefore, understanding
(D-Phe12)-Bombesin and its applications provides insight into not just current scientific pursuits but
also the future of medical treatments where targeted therapies and diagnostics could revolutionize
patient care.
How does (D-Phe12)-Bombesin improve upon the natural Bombesin peptide for
research?
(D-Phe12)-Bombesin offers significant enhancements over natural Bombesin due to its
molecular modification, which improves both its functional stability and specific affinity for cell
surface receptors. This analogue’s development centered on overcoming limitations seen with the native
peptide, mainly its vulnerability to rapid degradation and suboptimal receptor selectivity, which are
crucial factors for its effective application in rigorous scientific research. The incorporation of the
D-phenylalanine at the twelfth position is a key chemical modification that makes (D-Phe12)-Bombesin
more resistant to enzymatic degradation. Natural peptides often face the challenge of rapid breakdown by
peptidases and proteolytic enzymes in biological systems, significantly limiting their operational life
and effectiveness. By including an unnatural amino acid, the longevity of (D-Phe12)-Bombesin is
increased, allowing for prolonged activity and more accurate and consistent experimental outcomes.
Enhanced receptor affinity is another substantial advantage of this analogue. The modification yields
improved binding specificity to the gastrin-releasing peptide receptor (GRP-R), which is highly relevant
in cancer studies. In many cancerous ailments—like prostate and pancreatic cancers—GRP-R expression is
dysregulated, making it an ideal target for diagnostic imaging and therapeutic investigation.
(D-Phe12)-Bombesin’s precise alignment with these receptors enables more effective interaction studies,
aiding in the development of specialized detection and treatment methods. Comprehending these
interactions at a molecular level is vital for achieving breakthroughs in therapeutic interventions.
Furthermore, (D-Phe12)-Bombesin's structure-activity relationship has catalyzed innovations in
synthetic peptide chemistry and pharmacology. The detailed understanding of how its particular
modifications influence behavior in biological contexts helps guide new synthetic strategies for
developing analogous compounds, potentially yielding novel medical or diagnostic applications beyond
current uses. These efforts are pivotal as they inform the conception and testing of new agents that
could be more selective and efficient than existing options, thus impacting both the scientific
understanding and practical applications of peptide-based interventions. As a result, (D-Phe12)-Bombesin
represents not only an improvement over Bombesin but also a platform for continuous exploration and
innovation in peptide therapeutics and diagnostics.
What are the challenges and limitations
associated with using (D-Phe12)-Bombesin in research?
Despite its considerable promise and
capabilities, the use of (D-Phe12)-Bombesin in research is not without specific challenges and
limitations that scientists must account for to achieve valid and reproducible results. First and
foremost, one of the main challenges involves understanding the complex interaction dynamics between the
compound and its target receptors in varying biological systems. Even with the enhanced specificity of
(D-Phe12)-Bombesin to GRP receptors, these receptors are still part of a broader network of molecular
interactions within the cellular microenvironment that can complicate the interpretability of results.
The concurrent presence of other peptide receptors or proteins in the cellular milieu potentially
influences receptor binding and signaling pathways, necessitating advanced and often costly technologies
such as high-resolution imaging and biochemical assays to decipher targeted effects
accurately.
Another limitation pertains to the potential immunogenicity or unexpected biological
effects in vivo. Any alteration in a peptide, such as the substitution with D-phenylalanine, while
increasing stability and receptor affinity, might also provoke an unwanted immune response, particularly
in settings that involve prolonged exposure or high concentrations. This context is of utmost concern in
translational research or therapeutic development phases since immunogenicity can undermine safety and
efficacy. Thorough preclinical evaluation using animal models, although resource-intensive, is crucial
to mitigate these risks before advancing to clinical stages.
Additionally, the economic aspect
cannot be overlooked. Synthesizing analogues like (D-Phe12)-Bombesin requires rigorous quality control,
precise analytical assessment, and robust characterization techniques, all contributing to higher
production costs. This financial barrier can limit access, particularly for resource-constrained
laboratories, potentially stymying broader research and innovation.
Moreover, ethical
considerations surrounding the use of potent bioactive compounds like (D-Phe12)-Bombesin must be
considered. Research involving these agents requires strict adherence to ethical guidelines and
regulatory standards established for peptide research. Ensuring ethical compliance throughout research
procedures, while essential for maintaining integrity and credibility, also introduces additional layers
of complexity and oversight that can delay research timelines.
In summary, while
(D-Phe12)-Bombesin is an invaluable research tool, prevalent challenges like understanding complex
interactions, managing potential biological responses, ensuring economic feasibility, and adhering to
ethical frameworks exist. Addressing these barriers requires a concerted effort from the scientific
community, incorporating advances in technology, strategic collaboration, and policy development to
fully capitalize on the capabilities this analogue offers.
What are the current trends in
research using (D-Phe12)-Bombesin?
Research utilizing (D-Phe12)-Bombesin is currently thriving
with innovative applications that span from fundamental science to translational studies, reflective of
its unique ability to target GRP receptors prominently expressed in certain disease states. One of the
significant trends is the emphasis on its utility in precision oncology. With a growing appreciation for
personalized medicine, agents like (D-Phe12)-Bombesin are being incorporated into research models that
aim to fine-tune cancer diagnostics and therapies to individual patient profiles. Researchers are
advocating for the concept of theranostics—a field combining therapeutic and diagnostic capabilities—to
harness peptides for dual-purpose roles. For instance, the incorporation of radioactive isotopes with
(D-Phe12)-Bombesin for use in radiolabeling technology has shown promising results in non-invasively
visualizing tumors while potentially delivering targeted radiation therapy. This strategy could lead to
the advancement of non-conventional treatment regimens that minimize side-effects while improving
therapeutic outcomes.
Another standout trend lies in simultaneous studies focused on
neurodegenerative diseases and psychiatric disorders. As a variant influenced by neuropeptides,
(D-Phe12)-Bombesin is pivotal in modulating neurobiological pathways. Researchers are now exploring its
impacts on regulatory mechanisms within the central nervous system, studying its influence on receptors
involved in conditions such as schizophrenia, Alzheimer's, and Parkinson's disease. By exploring these
neural pathways further, novel therapeutic avenues focused on neuropeptide signaling can be developed,
offering alternatives to traditional therapies that often come with significant limitations or side
effects.
In addition, cutting-edge research is coupling (D-Phe12)-Bombesin with nanotechnology to
improve peptide delivery systems, enhancing specificity and minimizing systemic exposure. The
integration of nanocarriers helps in improving the peptide’s stability and solubility while providing
opportunities for simultaneous multi-drug delivery systems—a potential breakthrough for multi-modal
cancer therapy and advanced diagnostics.
Furthermore, advances in computational modeling and
bioinformatics are also contributing to (D-Phe12)-Bombesin research. Computational models enable
researchers to simulate and predict binding behaviors, receptor interactions, and pharmacokinetic
profiles with greater accuracy, paving the way for more efficient experimental design and hypothesis
testing.
Overall, the study of (D-Phe12)-Bombesin is at the forefront of bridging fundamental
research with applied sciences, emphasizing targeted therapies, improved diagnostics, and enhanced
understanding of complex biological systems. Progress in these areas holds the potential to
revolutionize our approach to disease treatment and diagnosis, making it a constantly evolving and
exciting field of research.
What safety considerations should be kept in mind when working with
(D-Phe12)-Bombesin in a laboratory setting?
Ensuring safety during research involving
(D-Phe12)-Bombesin is of paramount importance, given the bioactive nature of peptides and the
potentially profound biological effects they may elicit. To safeguard researchers and the integrity of
their work, several key considerations must be adhered to meticulously. First and foremost, thorough
training and education regarding the compound’s properties, handling procedures, and potential
biological impact are essential for all laboratory personnel. Understanding its potential interactions,
especially as a peptide targeting GRP receptors that are heavily involved in cancer pathways, helps in
anticipating the nature of experiments and associated risks. This knowledge dictates safety protocols
when handling the compound, ensuring both effective experimentation and researcher
well-being.
Proper laboratory attire and safety gear are fundamental for handling
(D-Phe12)-Bombesin. Appropriate PPE must include lab coats, gloves, and eye protection to prevent
accidental exposure to the skin or mucous membranes. It’s also advisable to work in fume hoods when
there’s a risk of aerosolization, ensuring adequate containment. Working within a designated laboratory
area that’s specifically equipped and maintained for chemical and biological research further
contributes to a safe working environment. Another crucial component is robust waste management and
decontamination procedures. Waste products, including unused (D-Phe12)-Bombesin and contaminated
materials, need disposal in compliance with hazardous waste regulations to prevent environmental
contamination or inadvertent exposure. Specialized deactivation protocols must be followed rigorously
when cleaning equipment and surfaces to prevent cross-contamination with other experiments or laboratory
sections.
Communicating and documenting all experimental procedures and deviations is equally
critical. Lab members should maintain detailed lab notes and communicate possible exposure incidents
immediately, using incident reporting systems. This transparency facilitates quick response measures and
ensures that safety protocols are updated based on real-world data. Furthermore, all research should
receive approval from relevant ethical review boards and institutional safety committees, ensuring that
experimental designs meet the highest safety standards.
Finally, considering the experimental
nature of (D-Phe12)-Bombesin, securing clearances from supplier material safety data sheets (MSDS) and
following institutional guidelines crafted to handle new or particularly potent compounds is imperative.
By maintaining stringent safety practices, scientists can not only ensure personal safety and
environmental compliance but also uphold the reliability and credibility of their research findings.
Through these dedicated protocols, the risks associated with handling (D-Phe12)-Bombesin can be
substantially mitigated, paving the way for safe and productive research outcomes.