Organometallic Ligands

<p>Metabotropic glutamate receptor subtype-5 antagonist</p>

<p>Inhibitor of CDK4/6 serine/threonine kinases; antineoplastic</p>

<p>Inhibitor of ERK1 and ERK2 kinases</p>

<p>Tretinoin is a type of retinoic acid that can be used for the treatment of acne. It is a chemical inhibitor that binds to nuclear receptors and leads to an increase in apoptosis. This type of retinoic acid helps with cell detachment and increases shedding thus increasing cell turnover. Tretinoin has been shown to have antibacterial efficacy against Staphylococcus aureus, as well as synergistic effects when combined with other agents, such as cyclic lipopeptide antibiotics and quinolones. Additionally, Tretinoin is used in the research and treatment for promyelocytic leukaemia.</p>

<p>Potent and selective inhibitor of the glycogen synthase kinase GSK-3. Promotes cell renewal in embryonic stem cells by modulating Notch, MAPK and TGF-β signalling pathways, which are involved in pluripotency. It also affects the Wnt/β-catenin pathway and alters expression of genes coding for proteins, epigenetic regulatory elements and non-coding RNAs. The combination of CHIR 99021 and basic fibroblast growth factor (bFGF) allows long-term self-renewal in adult mouse retinal progenitor cells.</p>

<p>mGluR5 antagonist</p>

<p>Abiraterone is an antiandrogen drug used in the treatment of metastatic prostate cancer. It is a derivative of steroidal progesterone. This drug inhibits the enzyme CYP17 irreversibly, thus inhibiting the synthesis of androgen. It specifically inhibits the conversion of 17-hydroxyprognenolone to dehydroepiandrosterone to decrease serum levels of testosterone and other androgens.</p>

<p>Topoisomerase II inhibitor; chemotherapeutic drug</p>

<p>Camostat is a serine protease inhibitor that is used for the treatment of chronic pancreatitis. This drug has shown to reduce inflammation and pain. Studies have shown that Camostat has also inhibited the entry of SARS-CoV-2 in lung cells by inhibiting the priming process of S-protein, necessary for the viral entry into host cells.</p>

<p>An agonist of 5-HT1A serotonin receptors. Neurotrophic and neuroprotective activities have been demonstrated in neurodegenerative models in vivo. This is mediated by increasing the secretion of nerve growth factor (NGF), when tested in astrocytes in vitro. Anti-nociceptive activity was displayed in a model of acute tonic nociceptive and inflammatory pain.</p>

<p>Inhibits type III tyrosine kinases (PDGFRα, PDGFRβ, FLT3)</p>

<p>β3-adrenoceptor agonist</p>

<p>FP receptor ligand; activator of PGF2αR</p>

<p>Inhibitor of cytochrome P450; inhibitor of prostaglandin synthesis</p>

<p>Imiquimod is a toll-like receptor 7 agonist drug that is used for the treatment of genital warts, basal cell carcinoma and condyloma acuminata. This drug works by relieving and controlling wart production. Studies in mice have shown that this drug may induce cytokines such as interleukins. Imiquimod helps to increase apoptosis of diseased tissues and an infiltration of lymphocytes into tumor lesions.</p>

<p>Ramelteon is a synthetic drug, which is a melatonin receptor agonist with high affinity for MT1 and MT2 receptors. These receptors are primarily located in the suprachiasmatic nucleus of the brain, an area responsible for regulating circadian rhythms. By binding to these receptors, Ramelteon mimics the effects of the endogenous hormone melatonin, promoting the onset of sleep.</p>

<p>Elesclomol is an investigational anticancer agent, which is a small-molecule compound. It functions by targeting the cellular oxidative stress pathway; specifically, it enhances the production of reactive oxygen species (ROS) within cancer cells. By elevating ROS levels beyond the threshold tolerable by cancer cells, Elesclomol induces apoptosis through the disruption of mitochondrial function, making it selective for environments with heightened oxidative stress.</p>

<p>Inhibits phorbol ester TPA/PMA; immunosuppressant</p>

<p>Modifier of the SMN2 gene splicing</p>

<p>Farnesyl pyrophosphate synthase inhibitor; hepatic de novo lipogenesis inhibitor</p>