Ligands organométalliques

<p>Casein kinase (CK1ε and CK1Ύ) inhibitor</p>

<p>Dopamine reuptake inhibitor</p>

<p>Diacerein is a slow-onset anthraquinone IL-1 inhibitor that is used in the treatment of joint diseases such as osteoarthritis. This drug is also being studied for the treatment of insulin resistance and diabetes mellitus. Diacerein works to decrease inflammation and cartilage destruction by reducing the level of interleukin-1.</p>

<p>Dapagliflozin is a sodium-glucose cotransporter subtype 2 (SGLT2) inhibitor that can be used in the treatment of diabetes mellitus type 2. It inhibits glucose reabsorption in the proximal tubule of the nephron and results in glycosuria, which helps to improve glycaemic control. Also, Dapagliflozin is used to lower the risk of sustained eGFR decline, end-stage renal disease, cardiovascular death, and hospitalization for heart failure in patients with chronic kidney disease who are at risk of progression.</p>

<p>Inhibitor of 3β-hydroxysteroid dehydrogenase in steroid biosynthesis</p>

<p>Ranitidine is classified as a histamine antagonist that reduces gastric acid section by blocking the H2- receptor. It decreases the amount of acid in the stomach. It is used to treat conditions such as ulcers, Zollinger-Ellison syndrome and GERD.</p>

<p>Potent and selective MAP/ERK kinase 1/2 inhibitor. Reduces growth of tumor cells with B-Raf and Ras mutations. Tumor regression observed after chronic treatment in in vivo xenograft models. Enhances anti-tumor effect in combination with irinotecan or docetaxel.</p>

<p>Cetilistat is a drug that is used to treat obesity. This drug inhibits the enzyme pancreatic lipase and so it prevents triglycerides from being hydrolyzed into absorbable free fatty acids.</p>

<p>Inhibitor of HIF1-α transcription factor and repressor of HIF1-α-regulated genes in adult and embryonic stem cell models as well as in tumoral cell lines. FM19G11 inhibits the expression of undifferentiating factors Oct4, Sox2, Nanog, and Tgf-α at transcriptional and protein level. FM 19G11 affects also epigenetic events by reducing histone acetylation and leading to repression of p300, a HIF-transcription activation co-factor.</p>

<p>Lodoxamide is a type of ophthalmic medication known as a mast cell stabilizer, which is chemically synthesized from non-steroidal structures. It works by inhibiting the degranulation of sensitized mast cells and subsequent release of inflammatory mediators such as histamine. This action is achieved through the stabilization of the cell membrane of mast cells, thus preventing cellular activation.</p>

<p>Inhibitor of oxidative phosphorylation which acts on the F0F1 ATP synthase in the inner mitochondrial membrane and causes acute increase in mitochondrial membrane potential. Gboxin was shown to accumulate in mitochondria of cancer cells, to cause cellular toxicity and cell growth inhibition in mouse glioblastoma. However, Gboxin did not inhibit growth of mouse embryonic fibroblasts or neonatal astrocytes.</p>

<p>An irreversible GSK-3β inhibitor that reduces phosphorylation of tau proteins, protects from neuronal loss and has cognitive and behavioural benefits in murine models. Studied for its potential as a therapeutic agent in Alzheimer’s disease and other neurodegenerative diseases. Tideglusib was also shown to inhibit the main protease Mpro from the SARS-CoV-2 virus with IC50 of 1.55 μM.</p>

<p>Inhibitor of 8-oxoguanine DNA glycosylase OGG1 with IC50 of 0.059 μM and excellent specificity over other DNA repair enzymes. OGG1 and its substrate 8-oxoguanine are involved in mutagenesis, genotoxicity, inflammation and cancer. The compound can cause accumulation of 8-oxoguanine in DNA in vitro and is a potent tool for the study of OGG1 biology.</p>

<p>Lomustine is an alkylating agent that is used as chemotherapy for treating metastatic brain tumors and relapsed Hodgkin’s disease in combination with radiation treatments. This drug causes alkylation and cross-linking of DNA, thus inducing cytotoxicity. Furthermore, this drug inhibits DNA synthesis.</p>

<p>Omeprazole is a proton pump inhibitor (PPI) that inhibits the production of gastric acid in the stomach. This is due to Omeprazole binding through a stable disulphide bond to the H+/K+ ATPase enzyme found on parietal cells, and preventing hydrogen ion transport. Consequently, gastric acid secretion is supressed. As a PPI, Omerprazole can be used to treat disorders where gastric acid is over-secreted. Examples of these disorders are gastroesophageal reflux disease (GERD) and peptic ulcer disease.</p>

<p>Bruton's tyrosine kinase antagonist; reduces Fcγ receptor signaling</p>

<p>Rabeprazole is a proton pump inhibitor drug that is used to treat symptoms of GERD, heal gastrointestinal ulcers and eradicate Helicobacter pylori. This antiulcer drug suppresses gastric acid by inhibiting the gastric H+/K+ ATPase at the parietal cell.</p>

<p>Eliglustat is an oral medication used as a substrate reduction therapy for Gaucher disease type 1, which is an inherited lysosomal storage disorder. This product is a small-molecule inhibitor derived via chemical synthesis. Its primary mode of action involves the selective inhibition of glucosylceramide synthase, an enzyme responsible for the first committed step in glycosphingolipid biosynthesis. By reducing the production of glucosylceramide, eliglustat decreases the substrate accumulation that contributes to the pathophysiology of Gaucher disease.</p>

<p>Selective c-Met kinase inhibitor</p>

<p>Amlexanox is an antiallergic and anti-inflammatory drug that has been shown to be effective in treating rhinitis and allergic asthma in clinical studies. It prevents the slow-reacting substance of anaphylaxis (SRS-A) from being released chemically as a mediator and may have antagonistic effects on interleukin-3.</p>

<p>Monoamine oxidase-B inhibitor; anti-parkinsonian; neuroprotective</p>

<p>This compound is a novel negative allosteric modulator of glutamate metabotropic receptor mGlu7. It is highly selective for mGlu7 over other receptors of mGlu class with IC50 = 795 nM. Although VU 6010608 showed favourable brain penetration in rats, it has been proposed as an in vitro tool for electrophysiology studies. The mGlu7 is broadly distributed within the mammalian central nervous system and it plays a key role in neuronal function and synaptic plasticity.</p>

<p>Synthetic antineoplastic agent</p>

<p>Solifenacin is a muscarinic antagonist drug that is used to treat symptoms associated with an overactive bladder such as urine urgency and urinary incontinence. This drug has high affinity for M1, M2 and M3 receptors, with its highest being for M3 receptors. Antagonism of these receptors prevent contraction of smooth muscles in the bladder.</p>

<p>AZD 1152 is an Aurora kinase inhibitor, which is a type of small-molecule therapeutic agent. It is derived from the pharmaceutical research conducted by AstraZeneca. Its primary mode of action involves the selective inhibition of Aurora B kinase, an enzyme crucial for the regulation of mitosis. By interfering with this enzyme, AZD 1152 disrupts the normal progression of cell division, leading to the inhibition of proliferation and induction of apoptosis in rapidly dividing cells.</p>

<p>Androgen receptor antagonist; anti-cancer agent</p>

<p>Albuterol is a selective beta-2 adrenergic receptor agonist drug that is used to prevent and treat wheezing, shortness of breath, and other breathing difficulties caused by asthma. It relaxes the muscles in the airways, making them more open. Albuterol also has an anti-inflammatory effect.</p>

<p>An inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase that reduces total cholesterol and low-density lipoprotein (LDL). Cerivastatin is cardioprotective and anti-atherosclerotic. Cerivastatin inhibits the expression of the atherosclerotic genes monocyte chemoattractant protein-1 (MCP-1) and C-C chemokine receptor type 2 (CCR2), whilst inducing the expression of Kruppel-like factor 2 (KLF2).</p>

<p>ÎŽ opioid receptor agonist; anti-nociceptive; anti-depressant</p>

<p>Imiquimod maleate is an immune response modifier, which is a synthetic compound sourced from chemical synthesis. Its mode of action involves the activation of the immune system through the stimulation of toll-like receptor 7 (TLR7), leading to the induction of various cytokines, such as interferon-alpha, that initiate an antiviral and anti-tumor response.</p>

<p>MET tyrosine kinase inhibitor; anti-proliferative; pro-apoptotic</p>

<p>Anastrozole is a non-steroidal drug that belongs to the class of aromatase inhibitors. It inhibits the production of estrogen by blocking the conversion of androgens to estrogens in peripheral tissues. The drug has been shown to be effective in treating breast cancer in postmenopausal women. In vitro assays have shown that Anastrozole can inhibit tumor growth as well as induce apoptosis in human serum cells, which suggests that it may be effective against a variety of cancers.</p>

<p>Hyp9 is an advanced biochemical reagent, which is derived from sustainably sourced natural compounds with a proprietary purification process. Its mode of action involves targeted binding to specific molecular sites, enabling the modulation of biochemical pathways with high precision.</p>

<p>Thioglycosyl Naphthalimide is a highly potent human O-GlcNAcase (hOGA) inhibitor with good selectivity against human β-N-acetylhexosaminidase B (HsHexB).</p>

<p>Fingolimod is a sphingosine 1-phosphate receptor modulator that is used in the treatment of relapsing-remitting form of multiple sclerosis. It is also being studies to manage lung complications in patients with COVID-19. This drug binds to various sphingosine 1-phospahte receptors and suppresses the exit of lymphocytes from lymph nodes.</p>

<p>NMDA glutamate receptor antagonist</p>

<p>Androgen receptor antagonist</p>

<p>Atenolol is a beta-blocker that slows the heart rate and decreases the force of contraction, which reduces the workload on the heart. Atenolol has been shown to be effective in lowering blood pressure in people with chronic kidney disease who are not taking angiotensin-converting enzyme inhibitors. It is also used to treat hypertension and chronic angina.</p>

<p>Pemirolast is an antihistamine drug that is used for the treatment of allergies such as hay fever and allergic conjunctivitis. This drug binds to the histamine H1 receptor and blocks the action of histamine which results in the relief of allergic symptoms brought on by histamine. This drug is also a mast cell stabilizer.</p>

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

<p>Inhibitor of ERK1 and ERK2 kinases</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>5-HT1A serotonin receptor agonist; alleviates symptoms of depression</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>Inhibits type III tyrosine kinases (PDGFRα, PDGFRβ, FLT3)</p>

<p>Retinoic acid receptor alpha agonist; antineoplastic</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>Rivastigmine is a cholinergic agent that is used in the treatment of dementia in Parkinson’s and Alzheimer’s disease. This drug is a carbamate derivative that binds to and inactivates cholinesterase such as acetylcholinesterase and butyrylcholinesterase. This leads to an increase concentration of acetylcholine at cholinergic synapse.</p>

<p>Prodrug of 5-aminosalicylic acid; anti-inflammatory</p>

<p>CholecystokininB (CCKB) receptor antagonist</p>