Synonym |
(Des-Pyr1)-LHRH |
Species |
Human |
Protein Accession |
P01148 |
Purity |
Greater than 95% |
Endotoxin Level |
Less than 1 EU/µg |
Biological Activity |
Not specified |
Expression System |
E. coli |
Fusion Tag |
None |
Predicted Molecular Mass |
1184.4 Da |
Formulation |
Lyophilized |
Reconstitution |
It is recommended to reconstitute the lyophilized (Des-Pyr1)-LHRH in sterile 18MΩ-cm H2O not
less than 100µg/ml, which can then be further diluted to other aqueous solutions. |
Storage & Stability |
Lyophilized (Des-Pyr1)-LHRH although stable at room temperature for 3 weeks, should be stored
desiccated below -18°C. Upon reconstitution (Des-Pyr1)-LHRH should be stored at 4°C between 2-7
days and for future use below -18°C. |
FAQ
What is (Des-Pyr1)-LHRH and how does it work in the human body?
(Des-Pyr1)-LHRH is a modified
form of the naturally occurring gonadotropin-releasing hormone (GnRH). In its native form, LHRH
(Luteinizing Hormone-Releasing Hormone) is a decapeptide that plays a crucial role in the regulation of
the reproductive system. It is secreted by the hypothalamus in a pulsatile manner and stimulates the
anterior pituitary gland to release two key gonadotropins: luteinizing hormone (LH) and
follicle-stimulating hormone (FSH). These hormones are essential for the proper functioning of the
gonads, influencing processes such as spermatogenesis in males and follicular development and ovulation
in females.
(Des-Pyr1)-LHRH is a derivative of GnRH where the first amino acid, pyroglutamic
acid, is removed. This modification can significantly alter the properties of the peptide, potentially
changing its affinity for GnRH receptors or extending its half-life in the body. These changes make
(Des-Pyr1)-LHRH an interesting candidate for therapeutic uses, particularly in contexts where modulation
of the reproductive hormone axis is desired.
The mechanism of action for (Des-Pyr1)-LHRH involves
binding to GnRH receptors located on the anterior pituitary gland cells, leading to a cascade of
intracellular events that result in the synthesis and release of LH and FSH. By potentially altering
these interactions through structural modifications, (Des-Pyr1)-LHRH may provide unique advantages,
either as a more potent agonist or even an antagonist, depending on its binding characteristics and
subsequent receptor activation effects.
Understanding the potential applications of
(Des-Pyr1)-LHRH requires a grasp of this regulatory pathway. It opens numerous research opportunities,
particularly in the field of reproductive health, oncology—where hormone-dependent cancers may be
influenced by GnRH analogs—and even in veterinary medicine where similar hormonal pathways are of
interest. Researchers are investigating how modifying this pathway with (Des-Pyr1)-LHRH can potentially
lead to therapeutic benefits, including fertility treatments or the management of hormone-driven
diseases.
What potential medical applications does (Des-Pyr1)-LHRH have?
The potential
medical applications of (Des-Pyr1)-LHRH are primarily centered around its ability to modulate the
reproductive hormone axis. Given its modified structure, (Des-Pyr1)-LHRH can offer unique interactions
with the GnRH receptors in the anterior pituitary gland, making it a molecule of interest in several
therapeutic contexts.
One promising application of (Des-Pyr1)-LHRH is in the management of
hormone-dependent conditions, such as certain types of breast and prostate cancers. These cancers are
often driven by sex hormones—estrogen and testosterone, respectively—and (Des-Pyr1)-LHRH, by altering
hormone release, could help control tumor growth. It can act by manipulating the levels of LH and FSH,
leading to a decrease in the production of sex hormones from the gonads, effectively suppressing the
environment in which these cancers thrive. Researchers are keenly interested in exploring the role of
(Des-Pyr1)-LHRH as either an agonist that stimulates or an antagonist that blocks GnRH receptors, as
both modalities might offer clinical benefits depending on the disease context.
In addition to
oncology, (Des-Pyr1)-LHRH may have applications in treating conditions like endometriosis, uterine
fibroids, and precocious puberty. These disorders can also benefit from hormonal regulation strategies.
By potentially suppressing ovarian or testicular hormone production via the downregulation of GnRH
receptors, (Des-Pyr1)-LHRH may offer relief from symptoms or halt disease
progression.
Furthermore, in reproductive medicine, (Des-Pyr1)-LHRH could be explored as a novel
fertility treatment. By selectively manipulating gonadotropin release, it might aid in protocols
requiring precise control over ovulation timing or spermatogenesis, which are critical in assisted
reproductive technologies like in vitro fertilization (IVF).
Across veterinary medicine, similar
physiological processes governed by the GnRH axis make (Des-Pyr1)-LHRH relevant. Its potential to
control reproductive cycles in livestock or pets for breeding or population control purposes is yet
another avenue of exploration. Overall, the medical applications of (Des-Pyr1)-LHRH remain a promising
field, with ongoing research likely to unlock new therapeutic strategies and improve the management of
various health concerns.
How does (Des-Pyr1)-LHRH compare to traditional LHRH
therapies?
(Des-Pyr1)-LHRH offers an intriguing comparison to traditional LHRH therapies,
primarily due to its altered structure and the effects this modification could have on its interaction
with the GnRH receptors. Traditional LHRH therapies utilize either agonists or antagonists to manage
several medical conditions related to the reproductive hormone axis, in which the timing and nature of
hormone release are critical factors.
Standard LHRH agonists mimic the natural hormone and
initially stimulate an increase in LH and FSH production. However, continuous exposure eventually leads
to desensitization of the pituitary gland, resulting in a decrease in these hormones and consequently
reducing the production of sex hormones like estrogen and testosterone. This downregulation is
beneficial in treating hormone-dependent cancers and disorders such as endometriosis and uterine
fibroids. GnRH antagonists, on the other hand, provide an immediate blockade of receptor activity,
preventing the usual hormone surge and offering a faster mechanism of action.
(Des-Pyr1)-LHRH,
with its structural modification, may offer advantages over these traditional therapies. By removing the
first pyroglutamic acid residue, researchers aim to enhance its pharmacokinetic and pharmacodynamic
profiles, potentially offering benefits such as increased potency, selective receptor targeting, or
extended duration of action. This could mean more efficient downregulation of the GnRH axis or a more
nuanced modulation of hormone release.
Moreover, (Des-Pyr1)-LHRH could be explored for its use in
patients who are resistant to or experience adverse effects from traditional LHRH therapies. The
modification might alter its immunogenic profile, leading to fewer side effects or reducing the
incidence of flare reactions commonly seen when initiating standard LHRH agonist
therapy.
Comparatively, (Des-Pyr1)-LHRH could provide new avenues in clinical settings that have
yet to be addressed fully by current LHRH treatments. Its development underscores a broader trend in
therapeutic research, aiming to refine and improve the specificity and safety of peptide-based
treatments. As research progresses, the potential of (Des-Pyr1)-LHRH to integrate into or even replace
certain conventional therapies will depend on how these theoretical advantages manifest in clinical
trials and patient outcomes.
What are the potential side effects or risks associated with
(Des-Pyr1)-LHRH therapy?
In assessing the potential side effects or risks associated with
(Des-Pyr1)-LHRH therapy, it's crucial to draw insight from existing knowledge about GnRH analogs in
general. GnRH therapies, which mimic or alter the action of endogenous LHRH, often carry a range of side
effects due to their impact on hormone levels. With (Des-Pyr1)-LHRH, these may mirror common issues
observed with LHRH agonists and antagonists, albeit with unique aspects given its specific structural
modification.
Common side effects associated with traditional GnRH therapy might include symptoms
of hypoestrogenism or hypogonadism due to suppressed levels of sex hormones. These can manifest as hot
flashes, decreased libido, mood changes, fatigue, and osteoporosis, as a result of reduced estrogen
levels in females or testosterone in males. If (Des-Pyr1)-LHRH functions by reducing these hormone
levels similarly, patients could experience comparable symptoms and need monitoring for bone density and
overall hormonal health.
Beyond these general side effects, there might be specific risks unique
to the longer latency or potency that could be engineered into (Des-Pyr1)-LHRH. For instance, increased
potency might heighten the risk of initial hormone surges or 'flare' responses seen with some agonist
therapies, leading to temporary exacerbation of symptoms or cancer cell proliferation in the short term.
Addressing such risks would involve carefully designed dosing regimens and initial use of antagonists to
mitigate flares if necessary.
Additionally, as with any peptide-based therapy, there's a
potential for allergic reactions or immunogenic responses, though these are typically rare. The side
effect profile could also differ based on individual patient factors, including pre-existing health
conditions, concurrent medication, and overall hormone sensitivity.
Given the exploratory nature
of (Des-Pyr1)-LHRH at this stage, comprehensive clinical trials are indispensable to fully evaluate its
safety and risk profile. During such trials, data collected on adverse effects would be critical in
determining appropriate patient selections, dosing guidelines, and long-term implications of therapy. As
the therapeutic development of (Des-Pyr1)-LHRH progresses, ensuring rigorous monitoring and mitigation
of side effects will be key components in its successful clinical application.
How can
(Des-Pyr1)-LHRH enhance research in reproductive health?
(Des-Pyr1)-LHRH has the potential to
significantly enhance research in reproductive health through its unique characteristics and
modifications to the traditional GnRH structure. Reproductive health is a field where hormonal
regulation plays an integral role, and any advancement in understanding or modulating this system can
have profound implications.
One of the primary ways (Des-Pyr1)-LHRH can contribute is by
providing a new tool for exploring the nuanced control of reproductive hormones. By investigating how
this derivative binds to and affects GnRH receptors differently than native LHRH, researchers can gain
insights into the dynamics of receptor interactions, signaling pathways, and subsequent hormone release.
Such knowledge is vital for developing targeted therapies that can more precisely manipulate
reproductive hormones, thus addressing conditions like polycystic ovary syndrome (PCOS), infertility, or
hypogonadism with greater efficacy and fewer side effects.
Furthermore, (Des-Pyr1)-LHRH could
facilitate research into the timing and pulsatility of hormone release, both of which are crucial for
normal reproductive function. By providing a means to either enhance or dampen this rhythmic release,
depending on the therapeutic design of the modified peptide, researchers could better understand
disorders caused by dysregulated hormonal rhythms, such as certain infertility types or menstrual
irregularities. This could lead to novel treatments that more accurately mimic or restore natural
hormone cycles.
In the context of contraceptive research, (Des-Pyr1)-LHRH might also provide
innovative avenues for development. By carefully modulating the reproductive hormone axis, it might
offer a new strategy for reversible contraception, expanding options beyond current methodologies that
have variable side effect profiles and efficacy.
Furthermore, in reproductive biology research,
animal models frequently utilize GnRH analogs to study reproductive processes or endocrinology.
(Des-Pyr1)-LHRH could offer distinct advantages, perhaps through prolonged action or reduced
degradation, thus ensuring consistent and reliable experimental conditions.
Overall, the
contributions of (Des-Pyr1)-LHRH to reproductive health research are anticipated to be multifaceted. Its
development and study could break new ground in how hormonal therapies are approached, leading to
improved treatments and greater understanding of reproductive physiology. These advances could
ultimately translate into significant clinical benefits, particularly in fertility treatments, hormone
replacement therapies, and the general management of reproductive health challenges.