Organometallic Ligands

<p>LW-II-41-27 is a novel Eph receptor tyrosine kinase inhibitor used for cancer treatment.</p>

<p>NADPH oxidase inhibitor; anti-inflammatory</p>

<p>Bremelanotide acetate is a synthetic peptide therapeutic, which is derived from the melanocortin receptor agonist class. Its primary source involves chemical synthesis designed to mimic endogenous hormone analogs that target specific receptors in the body. The mode of action of bremelanotide acetate involves activating melanocortin receptors, particularly the MC4 receptor in the central nervous system. This activation leads to modulation of brain pathways involved in sexual arousal and desire.</p>

<p>Carmustine is a DNA alkylating agent which also cross-links DNA. As a result, Carmustine disrupts the function of DNA, resulting in the arrest the cell cycle and apoptosis. Consequently these properties of Carmustine, in addition to its ability to easily transmit through the blood-brain barrier, means it can be used as a cancer treatment, treating cancers such as, breast, ovarian and pancreatic as well as lymphomas and leukemias. Furthermore Carmustine can contribute to cytotoxic effects through its ability to carbamoylate DNA repair enzymes and proteins.</p>

<p>Haloperidol is an antipsychotic drug that is used for the treatment of schizophrenia and for managing its symptoms such as agitation and delusions. This drug is a dopamine antagonist and aids in improving symptoms that are caused by an overproduction of dopamine. .</p>

<p>Specific inhibitor of the phosphoinositide 3-kinase (PI3K) alpha subunit with IC50 of 32 nM. In heart muscle it negatively regulates hypertrophic growth, causes increase in late sodium current and leads to arrhythmias. In tumours it inhibits the p110α subunit of PI3K and blocks growth factor signalling resulting in reduced tumour growth.</p>

<p>Maprotiline is a tetracyclic antidepressant that is used for the treatment of major depressive disorder and anxiety that is associated with depression. This drug inhibits noradrenaline reuptake and has anticholinergic properties. Additionally, Maprotiline inhibits the amine transporter which allows for a delay in the reuptake of noradrenaline.</p>

<p>Inhibitor of COX-1 and COX-2 cyclooxygenases</p>

<p>A specific inhibitor of Bone Morphogenetic Protein (BMP) type 1 receptors ALK2 and ALK3 (IC50  &lt; 0.5 µM). Dorsomorphin analog that exclusively targets the BMP but not VEGF signaling. It is able to inhibit the BMP-induced Smad1/5/8 activation but not the p38/MAP kinase signaling or Activin A-induced Smad2 activation.</p>

<p>Lapatinib is an antineoplastic agent used to treat breast and lung cancer. This drug is also a tyrosine kinase inhibitor and inhibits human epidermal growth factor receptor type 2 (HER2/ERBB2) and epidermal growth factor receptor (HER1/EGFR/ERBB1). Lapatinib has shown to inhibit ERBB-driven tumor cell growth in vitro and in various animal models.</p>

<p>6-OAU is a chemical compound categorized as a cytokinin-like molecule, which is derived from natural plant sources. It functions by modulating gene expression and hormone pathways involved in various plant growth and developmental processes. The mode of action of 6-OAU largely revolves around mimicking the activity of cytokinins, essential plant hormones that regulate cell division, shoot and root growth, as well as delay senescence.</p>

<p>SCO-267 is a highly purified chemical compound used as a selective enzyme inhibitor, which is derived from synthetic sources. This compound acts by specifically binding to the active site of its target enzyme, effectively inhibiting its biological activity. Through competitive inhibition, SCO-267 modulates enzymatic pathways, facilitating research into metabolic processes and enzyme kinetics.</p>

<p>Cilastatin is a renal dehydropeptidase inhibitor, which is a compound sourced from synthetic processes designed to augment the pharmacokinetic profile of certain beta-lactam antibiotics. Its primary mode of action is to inhibit the enzyme dehydropeptidase I (DHP-I), located in the renal brush border. This enzyme typically degrades antibiotics, like imipenem, within the renal tubules. By inhibiting DHP-I, cilastatin prevents the inactivation of these antibiotics, thereby prolonging their active presence in the body and enhancing their antimicrobial efficacy.</p>

<p>Olopatadine is a histamine H1 antagonist that is used to treat allergic conjunctivitis and rhinitis. This drug is also a mast cell stabilizer. Upon binding, Olopatadine blocks the H1 receptor signaling pathway, inhibiting the release of inflammatory mediators, such as tryptase, prostaglandin D2, TNF-alpha, as well as pro-inflammatory cytokines.</p>

<p>Carmofur is an antineoplastic agent that is used to treat various cancers such as breast and colorectal cancer. This drug is a derivative of fluorouracil. Carmofur is an inhibitor of the human acid ceramidase, a lysosomal amidase involved in the development of cancer cells.</p>

<p>Ticagrelor is a P2Y12 receptor antagonist that has been shown to reduce the risk of myocardial infarction. It inhibits the formation of thromboses. Ticagrelor binds to the adenosine diphosphate (ADP) site on the platelet P2Y receptor and prevents ADP from activating this receptor. It is used for the prevention of myocardial infarctions, strokes and cardiovascular disease.</p>

<p>Inhibits actin polymerization</p>

<p>Adenosine-A1 receptor agonist</p>

<p>Inhibitor of dihydroorotate dehydrogenase; anti-inflammatory; immunomodulatory</p>

<p>Sumatriptan is a serotonin receptor agonist that is used for treating migraines and cluster headaches. This drug binds to 5-HT1B/1D receptors and leads to constriction of cranial blood vessels. It also inhibits the release of pro-inflammatory neuropeptides.</p>