Organometallic Ligands

<p>Tiotropium is a bronchodilator that is used for the management of chronic obstructive pulmonary disease or COPD. It is an antimuscarinic drug that also treats asthma. Tiotropium acts mainly on M3 muscarinic receptors located in the airways to produce smooth muscle relaxation and bronchodilation.</p>

<p>Specific inhibitor of 8-oxoguanine glycosylase OGG1 with IC50 in submicromolar range. The compound inhibits binding of OGG1 to its substrate 8-oxoguanine, a guanine analog generated in the presence of reactive oxygen species (ROS). It was shown that TH5487 decreases inflammation level by inhibiting the base excision DNA repair in mice and altering the OGG1 chromatin dynamics. The compound also has implications in cancer biology since OGG1 inhibitors sensitise tumours to chemotherapy.</p>

<p>Opioid analgesic</p>

<p>Sunitinib is a tyrosine kinase inhibitor drug. It is a drug that is used as a treatment for renal cell carcinoma, gastrointestinal stromal tumor, and other solid tumors. This drug inhibits tyrosine kinases such as VEGFRs, this prevents tumour growth and pathologic angiogenesis.</p>

<p>A cytidine analogue and inhibitor of DNA methyl transferases (DNMTs) with anti-cancer activity. This stable, hydrophilic compound forms covalent complexes between DNMT and zebularine-substrate DNA. It causes DNA lesions that block replication and cause replication fork collapse, leading to the formation of DNA double-strand breaks. It was also shown that zebularine-induced DNA methylation decrease in the IL-1β promoter region and disrupts molecular mechanisms of neuroinflammation. Moreover, this molecule down-regulates the DNA-methylation profile in the pluripotency genes’ promoters, which leads to improved development of somatic cell nuclear transfer (SCNT) embryos.</p>

<p>Inhibitor of HMG-CoA reductase</p>

<p>The racemic mixture of cis-trans isomers of clomiphene citrate The cis-isomer, now termed zuclomiphene, is more estrogenic, while the trans-isomer, presently known as enclomiphene, is relatively anti-estrogenic. The racemic mixture utilized for ovulation induction typically contains 38% zuclomiphene and 62% enclomiphene.</p>

<p>D-Fructose-1,6-diphosphate trisodium salt octahydrate is a biochemical compound, an important intermediate in carbohydrate metabolism. It is sourced from the glycolytic pathway, where it functions as a phosphorylated sugar derivative formed from fructose-6-phosphate through the action of phosphofructokinase. As an allosteric regulator, it plays a crucial role in glycolysis, acting to accelerate enzyme reactions that convert glucose to pyruvate, thus providing energy to cells.</p>

<p>Corticosteroid; anti-inflammatory; treats dermatological conditions</p>

<p>Irsogladine is a gastroprotective drug that is used for the treatment of GERD and gastric ulcers. This drug also has antioxidant properties. Irsogladine is a phosphodiesterase-4 inhibitor and increases levels of cAMP. It helps to prevent and heal damage to the stomach lining.</p>

<p>EGFR tyrosine kinase inhibitor; pro-apoptotic; antiproliferative in cancer cells</p>

<p>Nimustine is an antineoplastic agent that is being studied for use in treating Glioblastomas. It is suggested to be a DNA alkylating agent although, its exact mechanism is still unknown.</p>

<p>Pomalidomide is an immunomodulatory agent that inhibits transcriptional regulation by interacting with the pomalidomide-binding protein, which prevents its interaction with RNA polymerase II and thereby prevents DNA transcription. The study with U266 cells demonstrated that pomalidomide targets CRBN, part of an E3 ligase complex, and inhibits its autoubiquinitation and supresses a critical gene (IRF4, interferon regulatory factor 4) for myeloma cell growth with concentrations up to 10 μM.In vitro assays have shown that pomalidomide has inhibitory effects on cell signaling pathways, such as the NF-κB pathway. Pomalidomide also decreases the production of proinflammatory cytokines, such as TNFα and IL-1β, by inhibiting their synthesis or their release from activated monocytes. Recently, the promoting effect of pomalidomide, as its analog lenalidomide, on erythropoiesis (production of red blood cells) has been investigated, demonstrating positive results for its use as a potential new therapy agent for β-hemoglobinopathies.</p>

<p>6-Thioguanine is a purine analog used in the therapy for leukemia and for remission consolidation in patients with acute nonlymphocytic anemia. This drug also has antimetabolite action. It replaces guanine during DNA replication. This substitution disrupts the accurate pairing of DNA bases, leading to errors in DNA replication and hinders cell division.</p>

<p>Picrotoxin is a GABA-A receptor antagonist that is used to relieve respiratory distress. This drug also is used as an antidote from poisoning by CNS depressants. Picrotoxin works by blocking the GABA activated chloride ionophore.</p>

<p>Inhibitor of glutathione peroxidase GPX4</p>

<p>Smoothened receptor agonist; induces mesenchymal progenitor cell differentiation</p>

<p>Activater of the Nrf2 pathway and an inhibitor of the NF-κB pathway.  Possible applications have extended to anti-viral treatment of COVID-19.</p>

<p>PF 05214030 is a biosimilar monoclonal antibody, which is sourced from recombinant DNA technology and designed to inhibit tumor necrosis factor-alpha (TNF-α). This product functions by binding to TNF-α, a cytokine that plays a critical role in mediating inflammation. By preventing TNF-α from interacting with its receptors on cell surfaces, PF 05214030 effectively reduces the inflammatory response associated with various autoimmune and inflammatory conditions.</p>

<p>A potent prostanoid receptor (FP) agonist and PGF2α analog. Its biological activity is mediated by action on prostamide receptors. Has therapeutic potential for glaucoma and ocular hypertension.</p>