Organometallic Ligands

<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>Prostaglandin D2 receptor antagonist</p>

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

<p>Glimepiride is a sulfonylurea drug that is used in the treatment of type 2 diabetes mellitus. This drug works by inhibiting ATP-sensitive potassium channels by binding non-specifically to the B sites of both sulfonylurea receptor-1 (SUR1) and sulfonylurea receptor-2A (SUR2A) subunits. As a result, this promotes insulin secretion from beta cells.</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>Interleukin-13 human is a recombinant cytokine, which is derived from the expression of the human IL-13 gene in suitable host systems, such as E. coli or mammalian cells. This cytokine belongs to the interleukin family and plays a pivotal role in the immune response by modulating inflammatory pathways. The mode of action of interleukin-13 involves binding to specific cell surface receptors, IL-13Rα1 and IL-13Rα2, which facilitates the activation of various intracellular signaling cascades, including the JAK/STAT pathway. This promotes the differentiation and proliferation of certain immune cells, influencing the production of IgE and contributing to the regulation of inflammatory responses.</p>

<p>O6-Benzylguanine is a guanine analog that is an antineoplastic agent. It works by acting as a suicide inhibitor of the enzyme O6-alkylguanine-DNA alkyltransferase. This results to an interruption of DNA repair so that damage can occur to local tumor targets.</p>

<p>Inhibits multiple receptor tyrosine kinases (RTKs), including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl. Sitravatinib inhibits proliferation of sarcoma cells and reduced tumor growth in vivo. Promotes immune response in tumor microenvironment and enhances sensitivity to immune checkpoint inhibitors. This compound is undergoing several clinical trials as a potential anti-cancer therapeutic agent.</p>

<p>ÎŽ opioid receptor agonist; anti-nociceptive; anti-depressant</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>Moracin C is a prenylated flavonoid, which is a type of naturally occurring compound. It is derived from the Morus genus, commonly known as mulberry trees. This compound functions primarily as an antioxidant, showing activity that may protect cells from oxidative stress by neutralizing free radicals.</p>

<p>MET tyrosine kinase inhibitor; anti-proliferative; pro-apoptotic</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>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>PMX 53 TFA is a synthetic cyclic peptide, which is derived from the advanced study of complement system interactors. This product, sourced from specialized peptide synthesis methodologies, functions through the inhibition of the C5a receptor, a key player in the immune response. By blocking this receptor, PMX 53 TFA modulates inflammatory pathways, effectively reducing overactive immune responses associated with various pathological conditions.</p>

<p>Tazarotene is an acetylenic retinoid that is used for the treatment of wrinkles, pigmentation of the skin and acne. Although, the mechanism of action for this drug is not yet fully understood, it is thought to bind to all three members of the retinoic acid receptor family. Studies have shown that this drug is associated with increased collagen production.</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>A potent inhibitor of CETP that inhibits transfer of cholesteryl esters and triglycerides. Raises HDL cholesterol levels whilst lowering LDL cholesterol. Reduces cardiovascular events in patients with atherosclerotic vascular disease that receive statin treatment.</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>Prostaglandin E1 analog; agonist of EP2, EP3 and EP4 receptors</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>Losartan is an angiotensin receptor drug that is used to treat hypertension. It works by blocking the activity of angiotensin II binding to the AT1 receptor. As a result, this causes vascular smooth muscle relaxation and lowers blood pressure.</p>

<p>Oxybutynin is an antimuscarinic agent that is used to aid the bladder in relaxing and preventing the urge to void. This drug is used in the treatment of an overactive bladder and reduces detrusor muscle activity. Oxybutynin works by inhibiting the action of acetylcholine on smooth muscle.</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>Inhibitor of activin receptor-like kinases (ALK4, ALK5 and ALK7), members of TGFβ type I receptor family. Blocks activin- and TGFβ-mediated signaling and phosphorylation of Smad2 downstream. Suppresses tumor-promoting and tumor-suppressing effects of TGFβ. Promotes differentiation of human embryonic stem cells (hESCs), whilst sustaining mouse ESCs in the undifferentiated state.</p>

<p>AZD3965 is a potent, selective and orally available monocarboxylate transporter 1 (MCT1) inhibitor with binding affinity of 1.6 nM, 6-fold selective for MTC1 over MCT2.</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 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>Inhibitor of the Smoothened receptor and Hedgehog signalling pathway. Cyclopamine is a steroidal alkaloid that binds to the heptahelical bundle of Smoothened and negatively regulates transcription of downstream genes. In prostate cancer cells, cyclopamine inhibited cell growth, arrested cell cycle and in glioblastoma, it depleted stem cell-like cancer cells.</p>