Organometallic Ligands

<p>Naloxone hydrochloride is a competitive antagonist at mu-, delta- and kappa-opioid receptors. Naloxone binding to receptors blocks the effects of opioids such as morphine, heroin, or oxycodone. Naloxone has been shown to be effective in treating acute overdoses of these drugs and reversing the depression of respiratory function that accompanies opioid overdose. It is also used to alleviate withdrawal symptoms and in the treatment of neonatal abstinence syndrome (NAS). NAS is a condition that occurs when infants are exposed to addictive levels of opioids in utero and go through withdrawal after birth.</p>

<p>Inhibitor of VEGFR; antineoplastic</p>

<p>Inhibitor of TRPC6 cation channel</p>

<p>Eplerenone is a drug known as an aldosterone antagonist. It is a type of potassium-sparing diuretic that is used to treat chronic heart failure and high blood pressure, particularly for patients with resistant hypertension due to elevated aldosterone. It does this by blocking the activity of the enzyme that produces aldosterone, which increases levels of sodium and water in the body. This leads to a decrease in blood pressure.</p>

<p>Etodolac is a non-steroidal anti-inflammatory drug (NSAID) used to treat osteoarthritis and rheumatoid arthritis. It is also used to treat acute pain. This drug works by inhibiting prostaglandin synthesis from the inhibition of the enzyme cyclooxygenase.</p>

<p>Potent inhibitor of c-Met catalytic activity. Selective over other tyrosine and serine-threonine kinases (600-fold selectivity). Ability to block constitutive or HGF-stimulated phosphorylation of c-Met demonstrated in vitro. JNJ 38877605 reduces radiation-induced invasion, apoptosis and proliferation of cancer cells in vitro.</p>

<p>BMH-7 is a small molecule inhibitor used in molecular biology, which is derived from chemical synthesis methods. It interacts with specific protein domains to disrupt protein-protein interactions within cellular pathways. The mode of action involves binding to target proteins, thereby inhibiting essential interactions that are crucial for the stability and function of multiprotein complexes. This targeted approach allows researchers to dissect complex signaling pathways and understand the underlying mechanisms of cellular functions.</p>

<p>Agonist of ghrelin receptor; growth hormone secretagog</p>

<p>BMH-9 is a peptide inhibitor, which is sourced from natural extracellular matrix components. Its mode of action involves binding specifically to target proteins, thereby inhibiting their interaction with other molecules. This specificity makes it a valuable tool in biochemical and cellular studies designed to elucidate protein functions and pathways.</p>

<p>Inhibitor of protein kinase CK2</p>

<p>Selective and potent inhibitor of 8-oxoguanine DNA glycosylase OGG1 with IC50 of 0.6 μM. OGG1 is a key enzyme in DNA repair mechanism called base excision repair (BER). The compound inhibits the hydrolysis of glycosidic bond required for the excision of 8-oxoguanine from double stranded DNA, which leads to accumulation of mutations. It has been proposed as monotherapy for certain types of cancers as well as adjuvant for cancer therapy with DNA damaging agents. It has potential to sensitize tumours for chemotherapy and inhibit development of drug resistance mechanisms.</p>

<p>Lenvatinib is a tyrosine kinase inhibitor that is used to treat cancers such as solid tumours. This drug inhibits the activity of VEGR receptors. It also inhibits other receptors such as fibroblast growth factor.</p>

<p>NAP is a neuroprotective peptide, which is derived from activity-dependent neuroprotective protein (ADNP), with a mechanism involving microtubule stabilization and neuronal protection. It exhibits the ability to protect neurons from various types of damage, including oxidative stress and conditions mimicking neurodegenerative diseases. NAP enhances axonal transport and increases the resilience of neurons to insults that would typically result in cell death. This peptide has shown promise in preclinical studies for its potential to halt or reverse cognitive decline, making it a focal point for research into therapeutic strategies for disorders like Alzheimer's disease and other tauopathies. The peptide operates by binding to microtubules, promoting stability, and facilitating efficient transport of cellular components. Studies have highlighted its role in traversing the blood-brain barrier, which makes it a viable candidate for central nervous system-targeted therapies. Researchers continue to explore its efficacy and possible applications in improving cognitive function and providing neuroprotection in aging populations.</p>

<p>Endothelin receptor antagonist</p>

<p>4,5,6,7-Tetrabromobenzimidazole is a brominated heterocyclic compound, which is synthesized chemically from benzimidazole. Its bromination at the 4, 5, 6, and 7 positions of the benzimidazole ring enhances its reactivity, making it a highly potent inhibitor in various enzymatic processes. This compound is primarily sourced through methods that involve controlled bromination reactions in laboratory settings.</p>

<p>Icatibant is a 10 amino acid peptidomimetic of bradykinin and a selective antagonist to the bradykinin B2 receptor. Icabinant has been used for the treatment of attacks in patients with hereditary angioedema. Recent evidence has shown a link between dysregulated bradykinin‐mediated inflammation and acute respiratory distress syndrome (ARDS), a common complication in COVID-19 patients. Icatibant was proposed to inhibit excessive activation of the bradykinin B2 receptor during the SARS-CoV-2 infection, reducing the risk of ARDS.</p>

<p>PD 168393 is a potent and selective irreversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It is synthesized through advanced chemical processes, designed to specifically target and covalently modify the ATP-binding site of EGFR. The mode of action involves the irreversible binding to the cysteine residue in the ATP-binding pocket, leading to the inhibition of EGFR autophosphorylation and subsequent downstream signaling pathways.</p>

<p>Pan-class I phosphatidylinositide 3-kinase (PI3K) inhibitor (IC50 = 3, 33, 3 and 75 nM at catalytic subunits p110α, p110β, p110δ and p110γ respectively). Inhibits proliferation in several cancer cell lines, such as glioblastoma, breast and prostate cancer cells. Has synergistic anti-cancer effect in combination with MEK/ERK kinase inhibitor GDC-0973 (cobimetinib).</p>

<p>Tretoquinol is a bronchodilator, which is synthesized from specific chemical reactions involving quinoline derivatives. It functions primarily as a beta-adrenergic agonist, stimulating beta-2 adrenergic receptors. This activation leads to the relaxation of bronchial smooth muscle, resulting in widened air passages and improved airflow. Tretoquinol's mechanism of action involves enhancing cyclic adenosine monophosphate (cAMP) levels, which then promotes the relaxation of the bronchial and vascular musculature.</p>

<p>Dofetilide belongs to the class of antiarrhythmic agents. It is a class III antiarrhythmic agent, which acts by blocking the potassium ion channels in the heart. It is used for the management of normal sinus rhythm and in atrial fibrillation. In vitro studies have shown that Dofetilide can prevent arrhythmias resulting from experimental models of congestive heart failure and can prevent re-entry mechanisms that lead to tachycardia.</p>