Taiy Chemical
(3,5-Diiodo-Tyr5)-LHRH
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.
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