Organometallic Ligands

<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>Bupropion is an antidepressant drug that has been used in treatment trials for major depressive disorder. It has been shown to be effective in combination therapy with other drugs, such as a serotonin reuptake inhibitor (SSRI) or a tricyclic antidepressant (TCA). The drug's mechanism of action is not well understood but is said to increase the levels of dopamine and norepinephrine by inhibiting their reuptake.</p>

<p>MET tyrosine kinase inhibitor; anti-proliferative; pro-apoptotic</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>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>Cladribine is a purine nucleoside analogue that interferes with DNA synthesis by acting as a false building block in the DNA chain during replication. Cladribine is incorporated into the growing DNA chain, causing chain termination and leading to DNA damage, apoptosis (programmed cell death), and ultimately cell death. Cladribine is structurally similar to adenosine, but is partially resistant to breakdown by adenosine deaminase due to a chlorine molecule at position 2. This causes it to accumulate in cells and interfere with the targeted cell's ability to process DNA. This mechanism of action makes cladribine an effective treatment for certain types of cancer and autoimmune diseases, where it targets rapidly dividing cells.</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>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>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>GABAA receptor antagonist that displaces [3H]-GABA in membranes of rat brain (Ki value 0.15 µM). Has greater affinity for GABAA than bicuculline (20-fold greater). Inhibits Cl- current induced by GABA, but not pentobarbitone. Low-affinity inhibitor of glycine receptors.</p>