Synonym |
(3,5-Diiodo-Tyr5)-LHRH |
Species |
Human |
Protein Accession |
P01148 |
Purity |
95% |
Endotoxin Level |
<1 EU/μg |
Biological Activity |
Not specified |
Expression System |
E. coli |
Fusion Tag |
None |
Predicted Molecular Mass |
1182.3 Da |
Formulation |
Lyophilized from a 0.2 μm filtered solution in PBS |
Reconstitution |
Centrifuge vial before opening. Reconstitute in sterile ddH2O or aqueous buffer containing 0.1%
BSA to a concentration of 0.1-1.0 mg/ml. |
Storage & Stability |
Store lyophilized product at -20°C. Once reconstituted, store at 4°C for up to 2 weeks. For long
term storage, aliquot and store at -20°C. |
FAQ
What is (3,5-Diiodo-Tyr5)-LHRH and what is its primary function?
(3,5-Diiodo-Tyr5)-LHRH, also
known as a derivative of Luteinizing Hormone-Releasing Hormone (LHRH), is a peptide that plays a pivotal
role in the reproductive endocrine system. LHRH is a decapeptide produced in the hypothalamus that
triggers the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the
anterior pituitary gland. These hormones are crucial for regulating the reproductive system in both
males and females. The (3,5-Diiodo-Tyr5) modification refers to the introduction of iodine atoms at the
third and fifth positions of the tyrosine residue, which can significantly influence the peptide's
interaction with its receptors, thereby altering its biological effects and potential
applications.
In terms of functionality, (3,5-Diiodo-Tyr5)-LHRH is noteworthy for its role in
managing hormone-related functions and potentially modifying conditions associated with reproductive
health. By triggering or modifying the release of LH and FSH, this peptide can influence testosterone
and estrogen levels, affecting fertility, sexual function, and the menstrual cycle. The iodination at
the tyrosine position can enhance the peptide's resistance to enzymatic degradation, increase its
receptor affinity, or modify its pharmacokinetics, potentially creating derivatives with increased
potency or altered activity duration. This makes it a molecule of interest not only in understanding
reproductive endocrinology but also in medical applications where modulating hormonal outputs might be
beneficial.
Research into LHRH analogs like (3,5-Diiodo-Tyr5)-LHRH extends to their potential use
in treating hormone-sensitive tumors, such as certain types of prostate and breast cancers. By
regulating hormone levels, these analogs may help in reducing the progression of diseases that exhibit
hormone dependency. Furthermore, they are being explored for their utility in situations of hormone
suppression for therapeutic purposes, such as in preparing patients for medical procedures that require
controlled hormone levels. Understanding the subtleties of how modifications like the diiodo
substitution affect the peptide's action opens avenues for novel therapeutic strategies in an array of
endocrine and cancer-related conditions.
How does (3,5-Diiodo-Tyr5)-LHRH differ from natural LHRH
in terms of structure and potential effects?
(3,5-Diiodo-Tyr5)-LHRH differs from natural LHRH
primarily through a structural modification in which iodine atoms are introduced into the tyrosine
residue at specific positions, namely the third and fifth positions of the phenyl ring. This
modification has significant implications for the peptide's biochemical properties and interaction with
its natural receptors. From a structural perspective, the addition of iodine increases the molecular
weight and alters the electronic environment of the peptide. This can impact its hydrophobicity and
polarity, which in turn affects how the peptide penetrates cell membranes, circulates in the
bloodstream, and interacts with LHRH receptors.
The potential effects of this structural
modification are manifold. One of the most notable differences is the potential for increased receptor
binding affinity. Iodination can enhance the peptide's interaction with receptors, possibly leading to a
more potent biological response. Additionally, the presence of halogen atoms may increase the peptide's
stability against enzymatic degradation, prolonging its activity within the body. This could make
(3,5-Diiodo-Tyr5)-LHRH a more effective agent when used in therapeutic contexts where sustained action
is desirable.
Moreover, these structural modifications may alter the traditional effects observed
with natural LHRH. For instance, by potentially enhancing the duration or intensity of receptor
activation, the compound might offer a different pharmacokinetic profile, providing longer-acting
effects or requiring less frequent dosing. These characteristics are particularly appealing in the
development of pharmacological agents where modification of the natural hormone’s duration of action is
beneficial.
In therapeutic applications, these differences carry significant potential.
Modifications such as iodination are often investigated for their ability to reduce side effects,
increase specificity, and enhance efficacy in targeted treatments. When discerning the therapeutic
window for conditions related to reproductive health or endocrinological disorders, such modifications
might provide an edge over other treatments. However, with these benefits comes the responsibility to
rigorously evaluate the modified peptide’s full spectrum of effects, to ensure that enhanced potency or
altered action does not lead to unexpected side effects or negative interactions with other
physiological systems.
What are the therapeutic indications of (3,5-Diiodo-Tyr5)-LHRH in current
medical research?
Current medical research into (3,5-Diiodo-Tyr5)-LHRH primarily focuses on its
role in modulating the endocrine system, with potential applications in treating hormone-dependent
conditions and various forms of hormone-responsive cancers, such as prostate or breast cancer. This
derivative is part of an extensive category of LHRH analogs, which are studied for their ability to
regulate hormone production and secretion when natural balance is disrupted, or in situations where
hormone modulation is therapeutically beneficial.
The primary therapeutic indication of
(3,5-Diiodo-Tyr5)-LHRH lies in its potential use as part of endocrine therapy. In conditions such as
prostate cancer, where the disease's growth is often stimulated by testosterone, LHRH analogs can be
employed to suppress testosterone production by overstimulating LHRH receptors, leading to a
downregulation of LH and FSH release. This process ultimately results in reduced testosterone production
by the testes, thereby slowing the progression of hormone-sensitive tumors. Similarly, in
estrogen-receptor-positive breast cancer, reducing the estrogen levels through LHRH analogs can impede
tumor growth.
Beyond oncological uses, this peptide might also find relevance in managing
conditions like endometriosis and uterine leiomyoma, where hormone suppression can relieve symptoms and
inhibit disease progression. By modulating the levels of gonadotropins, which influence the menstrual
cycle and reproductive tissues, LHRH analogs can help in maintaining symptomatic
control.
Furthermore, there is ongoing research into the application of LHRH analogs, including
(3,5-Diiodo-Tyr5)-LHRH, in infertility treatments. By precisely controlling the timing and levels of
gonadotropin release, these compounds can assist in preparing the body for procedures such as in vitro
fertilization (IVF), where synchronized control of ovulation is crucial. In such contexts, the ability
of modified LHRH peptides to offer enhanced potency, prolonged action, or increased stability could
provide tangible benefits over unmodified variants.
While the therapeutic indications of
(3,5-Diiodo-Tyr5)-LHRH are promising, it is crucial to understand that significant research is still
needed to fully realize and optimize these applications. Clinical trials, pharmacodynamic studies, and
rigorous safety assessments are necessary components of this process to ensure that these derivatives
can be safely and effectively integrated into treatment paradigms. The potential breadth of applications
underlines the importance of continuing to explore and expand our understanding of these compounds
within therapeutic sciences.
What are the potential advantages of modified LHRH analogs like
(3,5-Diiodo-Tyr5)-LHRH compared to conventional therapies?
Modified LHRH analogs, such as
(3,5-Diiodo-Tyr5)-LHRH, can offer several potential advantages over conventional therapies, particularly
in contexts involving hormone regulation and the treatment of hormone-responsive conditions. One of the
primary benefits is their ability to provide a more targeted approach to managing hormone levels. Unlike
some other therapies that might systemically alter endocrine functions, LHRH analogs operate primarily
by interacting specifically with LHRH receptors, thus providing a more focused modulation of hormone
secretion pathways.
One significant advantage is the potential for enhanced potency and prolonged
duration of action provided by modifications like iodination. Introducing iodine atoms at strategic
positions can increase the stability of the peptide against enzymatic degradation, which enhances its
biological half-life. This means that the peptide can remain active longer in the body, potentially
reducing the frequency of administration required and maintaining a more consistent therapeutic effect.
This prolonged activity can be especially beneficial in managing chronic conditions requiring long-term
hormone regulation, such as in palliative treatment for hormone-dependent cancers.
Furthermore,
by modifying the structure of the LHRH analog, researchers can attempt to fine-tune its pharmacokinetic
properties to achieve an optimal balance of efficacy and safety. Enhanced receptor affinity resulting
from modifications can allow for greater specificity in receptor binding, potentially leading to
increased efficacy at lower doses, which can reduce the risk of adverse effects. This targeted approach
also implies that treatment could be more effective in achieving desired outcomes with minimized
systemic impact, which is advantageous for patient compliance and quality of life.
Another
potential advantage of derivatives like (3,5-Diiodo-Tyr5)-LHRH involves their versatility in addressing
a range of conditions. The same fundamental mechanism of action—the modulation of gonadotropin
release—offers a versatile tool in treating diverse conditions, from hormone-sensitive tumors to
reproductive health issues like endometriosis and infertility management. This versatility may
streamline therapeutic approaches, utilizing a common mechanism to act across various disorders linked
to hormonal dysregulation.
Moreover, given the precision with which these analogs can be
developed, they hold potential in creating combinatorial regimens that integrate with other therapies,
providing more comprehensive treatment solutions. For instance, integrating LHRH analogs with
chemotherapy or other hormonal therapies could enhance overall treatment effectiveness, thereby offering
an innovative direction for advanced therapeutic strategies.
However, while these advantages are
promising, it is imperative to ensure that each modified analog undergoes thorough research, including
clinical trials and safety assessments, to affirm its efficacy and safety in specific therapeutic
contexts. This process is critical for these potential benefits to be fully realized and effectively
translated into improved patient outcomes in contemporary medical practice.
What ongoing research
exists regarding (3,5-Diiodo-Tyr5)-LHRH, and how does it reflect future potential
applications?
Ongoing research into (3,5-Diiodo-Tyr5)-LHRH reflects a keen interest in the
exploration of its modified characteristics and potential applications across various domains of
medicine. This research primarily focuses on understanding how the incorporation of iodine molecules
impacts the peptide's stability, potency, and efficacy in therapeutic applications. Multiple studies are
currently evaluating its role in the treatment of hormone-dependent disorders, exploring both efficacy
and safety profiles in preclinical and clinical settings.
One area of active research is
oncology, particularly concerning hormone-responsive cancers such as prostate and breast cancer. By
understanding how (3,5-Diiodo-Tyr5)-LHRH functions at the cellular level, including its receptor binding
dynamics, researchers aim to establish whether its properties can be leveraged for enhanced tumor
suppression. Investigations often involve assessing its effectiveness in reducing the activation of
these tumors by their respective hormones, which is pivotal for managing disease
progression.
Beyond oncology, research is also delving into the compound's application in
reproductive health. For instance, work is being done to see if these derivatives can improve outcomes
in infertility treatments or provide more effective management for endometriosis. The timed release and
prolonged action of (3,5-Diiodo-Tyr5)-LHRH can be particularly beneficial in infertility protocols such
as in vitro fertilization (IVF) where precise hormonal control is necessary. Additionally, its potential
impact on menstrual cycle regulation offers a promising avenue for treating endometriosis, a condition
where hormone regulation can substantially alleviate symptoms.
Beyond its direct applications,
broader research is examining how chemically modifying LHRH analogs like (3,5-Diiodo-Tyr5)-LHRH can
guide future drug development. The insights gained from these modifications can inform strategies for
developing new analogs with even more refined properties, whether through further receptor specificity,
stability, or novel delivery mechanisms.
Furthermore, interdisciplinary studies incorporating
bioinformatics and molecular modeling are providing deeper insights into the precise interactions of
these modified peptides at the molecular level. This level of understanding is invaluable for tailoring
analogs to have desired characteristics, predicting their in vivo behavior, and anticipating possible
adverse effects or interactions in complex biological systems.
The future of
(3,5-Diiodo-Tyr5)-LHRH is indeed promising, reflected in its burgeoning research portfolio. As
understanding of how this and similar compounds operate deepens, there is potential for expanding their
use into broader therapeutic areas. Whether improving existing treatments or introducing completely
novel therapies, advancements in research today promise to deliver substantial developments in medical
treatments for a variety of hormone-related conditions. As always, rigorous clinical validation remains
a critical component to transition these potentials into tangible clinical applications.