Related Experiment Video
Updated: Jul 29, 2025
09:22
Multi-Faceted Mass Spectrometric Investigation of Neuropeptides in Callinectes sapidus
Published on: May 31, 2022
2.5K
Dynorphin 1-17 biotransformation peptides: properties, challenges and solutions for future therapeutics development
Rama Ballouze1, Salizawati Muhamad Salhimi1, Noratiqah Mohtar1
1School of Pharmaceutical Sciences, Universiti Sains Malaysia, USM, Penang, 11800, Malaysia.
Future Medicinal Chemistry
|May 25, 2023
Summary
Dynorphin 1-17 (DYN 1-17) peptides and their fragments play roles in neurological and inflammatory disorders. This review covers their therapeutic potential, challenges, and solutions for drug development.
Area of Science:
- Neuroscience
- Pharmacology
- Biochemistry
Background:
- Endogenously produced dynorphin 1-17 (DYN 1-17) undergoes enzymatic degradation into unique fragments.
- These peptides and fragments are implicated in neurological and inflammatory disorders via opioid and non-opioid receptor interactions.
- DYN 1-17 fragments show potential as drug candidates due to their diverse biological activities.
Purpose of the Study:
- To provide comprehensive updates on DYN 1-17 biotransformed peptides.
- To review their pharmacological roles, pharmacokinetic profiles, and clinical trial status.
- To discuss challenges and propose solutions for developing these peptides as therapeutics.
Main Methods:
- Literature review of existing studies on DYN 1-17 and its fragments.
- Analysis of pharmacological data, pharmacokinetic research, and clinical trial outcomes.
- Synthesis of information regarding therapeutic development hurdles and potential strategies.
Main Results:
- DYN 1-17 fragments exhibit significant roles in central and peripheral nervous system functions and inflammatory processes.
- Pharmacological and pharmacokinetic data reveal both therapeutic promise and development challenges.
- Several clinical trials are investigating the therapeutic applications of DYN 1-17 related peptides.
Conclusions:
- DYN 1-17 biotransformed peptides represent a promising class of therapeutics for neurological and inflammatory conditions.
- Overcoming challenges related to stability, delivery, and specificity is crucial for successful drug development.
- Further research and strategic development approaches are needed to fully realize the therapeutic potential of these peptides.
Related Concept Videos
01:15Opioid Analgesics: Synthetic and Semisynthetic Opioids
353
Synthetic and semisynthetic opioids are pivotal in pain management and tackling opioid addiction. Semisynthetic opioids, including morphinans (morphine derivatives), oxycodone, oxymorphone, hydrocodone, and hydromorphone, have improved pharmacokinetic profiles compared to morphine. Additionally, heroin and 6-MAM (6-Monoacetylmorphine) show better CNS penetration than morphine due to heightened lipid solubility. Hydromorphone, a potent opioid, undergoes hepatic metabolism to form the active...
353
01:16Drug Biotransformation: Overview
2.5K
Pharmaceutical substances known as xenobiotics are predominantly lipophilic and nonionized. This enables them to permeate lipid bilayers, such as cell membranes, and interact with intracellular target receptors. Lipophilic drugs have an advantage in crossing biological barriers and reaching their intended sites of action. However, lipophilic drugs often have a restricted capacity for renal expulsion or elimination from the body. When these drugs enter the kidneys and undergo glomerular...
2.5K
01:22Opioid Receptors: Overview
1.2K
Opioid receptors, including the mu (μ, MOR), delta (δ, DOR), and kappa (κ, KOR) types, belong to the rhodopsin family of G protein-coupled receptors. These receptors are located throughout the central and peripheral nervous systems and in non-neuronal tissues such as macrophages and astrocytes. Opioid receptor ligands can be categorized into agonists or antagonists. Highly selective agonists include [d-Ala2, MePhe4, Gly(ol)5]-enkephalin or DAMGO for MOR, [D-Pen2,...
1.2K
01:27Transducer Mechanism: Enzyme-Linked Receptors
2.6K
Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Major types that are helpful drug targets include:
2.6K
01:20Opioid Analgesics: Morphine and Other Natural Cogeners
306
Opioids are a class of drugs that mimic endogenous opioid peptides and act on opioid receptors, and help in pain relief. These compounds are classified as natural, synthetic, or semi-synthetic. Natural opioids, like morphine, codeine, and thebaine, are derived from the opium poppy plant (Papaver somniferum or Papaver album) and are termed opiates. Synthetic opioids are artificial, while semi-synthetic opioids combine natural and synthetic compounds. Morphine, a prototypical opioid, possesses a...
306
01:25Analgesia and Pain Management
676
Pain is critical to various clinical pathologies, provoking an urgent need for effective management. Pain, whether acute or chronic, is a complex neurochemical process. Its alleviation depends on the type, with nonopioid analgesics effective for mild to moderate pain, such as musculoskeletal or inflammatory pain, while neuropathic pain responds best to anticonvulsants, tricyclic antidepressants, or serotonin/norepinephrine reuptake inhibitors. For severe acute or chronic pain, opioids may be...
676