Organometallic Ligands

<p>Venlafaxine is an antidepressant drug used in the treatment of major depression, anxiety disorder and panic disorder. It is classed as an SNRI drug meaning it inhibits the reuptake of serotonin and norepinephrine so that there is an increased level of the neurotransmitters in the synaptic cleft.</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>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>EGFR tyrosine kinase inhibitor; pro-apoptotic; antiproliferative in cancer cells</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>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 prodrug of VRT 043198 that inhibits IL-converting enzyme (ICE)/caspase-1.  Inhibits LPS-induced secretion of cytokines. It has therapeutic potential in autoinflammatory diseases. VX 765 is cardioprotective in addition to the P2Y12 receptor inhibitor congrelor, resulting in reduced myocardial infarction.</p>

<p>Belinostat is a histone deacetylase (HDAC) inhibitor, which is a synthetic compound with a targeted mechanism of action. It is derived from the hydroxamic acid class and functions by inhibiting the activity of HDAC enzymes. These enzymes are responsible for removing acetyl groups from lysine residues on histone and non-histone proteins, altering chromatin structure and affecting gene expression. By inhibiting HDACs, Belinostat leads to an accumulation of acetylated histones, promoting an open chromatin structure and reactivation of silenced genes that can suppress tumor growth.</p>

<p>FTBMT is a GPR52 receptor agonist with an EC50 value of 71 nM. Studies demonstrate antipsychotic-like effects of FTBMT in murine models of schizophrenia. FTBMT elicits beneficial effects on cognitive processes such as spatial working memory and long-term memory in mice.</p>

<p>Reversible inhibitor of trypsin</p>

<p>Meloxicam is a non-steroidal anti-inflammatory drug (NSAID) which is used to treat various types of pain and inflammation caused by arthritis. It is also a COX-2 inhibitor which reduces gastrointestinal effects of this drug. Inhibiting these enzymes, allow for a decrease in inflammatory symptoms.</p>

<p>Immune suppressant; prevents pro-inflammatory cytokine release</p>

<p>Hydroxychloroquine is a drug that is used to treat multiple types of autoimmune diseases, including rheumatoid arthritis, systemic lupus erythematosus and discoid lupus. It is a prodrug, which is activated in the liver to hydroxychloroquine. It inhibits the production of inflammatory cytokines and nitric oxide by binding to the toll-like receptor 4 (TLR4) and inhibiting signaling pathways downstream of TLR4 activation. Additionally, Hydroxychloroquine is used to prevent and treat malaria caused by parasitic protozoan from the Plasmodium genus. Furthermore, recent studies revealed that hydroxychloroquine has beneficial effects on COVID-19 patients, as the current evidence shows that hydroxychloroquine inhibits SARS CoV-2 entry in host cells by interfering with endocytosis and affecting the glycoprofile on the spike glycoprotein.</p>

<p>A serotonin reuptake inhibitor with anticholinergic activity and mild inhibitory activity on noradrenaline reuptake. Paroxetine has been used for the treatment of depression, anxiety disorders, post-traumatic stress disorder, premenstrual dysphoric disorder and obsessive-compulsive disorder.  Also inhibits nitric oxide synthase and cytochrome isoenzyme P450 2D6.</p>

<p>VEGFR tyrosine kinase inhibitor</p>

<p>Inhibitor of MEK1 and MEK2 kinases</p>

<p>Autophagy activator that acts through targeting the ATP6V1A subunit of vATPase</p>

<p>Thymidylate synthase inhibitor</p>

<p>Androgen receptor antagonist</p>

<p>2-[(2-Ethoxy phenoxy)methyl]morpholine HCl is a sophisticated chemical compound utilized extensively in scientific research. As a synthetic organic compound, it is derived through a meticulous process involving the reaction of morpholine with ethoxy phenoxy derivatives, followed by hydrochloride salt formation. This synthesis ensures high purity and accurate functionality, making it suitable for precise laboratory studies.</p>

<p>Inhibitor of 5-lipoxygenase activating protein_x000D_</p>

<p>Antagonist of α-adrenoceptors; vasoactive agent</p>

<p>Benazepril is a nonsteroidal anti-inflammatory drug that can be used to treat hypertension, heart failure and renal failure. It is an angiotensin-converting enzyme (ACE) inhibitor that blocks the conversion of angiotensin I to angiotensin II. This inhibition prevents the vasoconstrictive effects of this peptide, which are mediated through activation of the renin-angiotensin system.</p>

<p>GSK-lsd1 dihydrochloride is a potent chemical inhibitor, which is derived synthetically to target LSD1, a histone demethylase involved in epigenetic regulation. It functions by inhibiting the enzymatic activity of LSD1, thereby affecting the methylation status of histones, a critical process in regulating gene expression. This inhibition leads to alterations in the transcriptional programs of cells, particularly those in oncogenic pathways.</p>

<p>Vadadustat is an orally administered hypoxia-inducible factor prolyl hydroxylase inhibitor (HIF-PHI), which is a synthetic small molecule. Its mode of action involves the inhibition of prolyl hydroxylase enzymes, which normally facilitate the degradation of hypoxia-inducible factor (HIF) under normal oxygen conditions. By stabilizing HIF, vadadustat effectively mimics a hypoxic response, leading to increased endogenous production of erythropoietin (EPO), a key hormone in red blood cell production.</p>

<p>Inhibitor of leucine-rich repeat kinase LRRK2Â</p>

<p>Inhibitor of Factor Xa; anti-thrombotic</p>

<p>Peripheral vasodilator; nootropic agent</p>

<p>t-TUCB is a potent soluble epoxide hydrolase (sEH) inhibitor, which is a chemically synthesized compound. The mode of action of t-TUCB involves the inhibition of sEH, an enzyme responsible for the degradation of epoxyeicosatrienoic acids (EETs). By inhibiting sEH, t-TUCB effectively increases the levels of EETs, which are signaling molecules involved in numerous physiological processes, including inflammation, blood pressure regulation, and pain perception.</p>

<p>MYCi975 is a microbial inoculant, which is a bio-based product designed for agricultural use. It originates from a carefully selected consortium of rhizobial bacteria, specifically tailored to establish a symbiotic relationship with leguminous plants. The mode of action involves the colonization of the plant roots by these rhizobia, which then form nodules. Within these structures, the bacteria convert atmospheric nitrogen into ammonia through biological nitrogen fixation, a process that enriches the soil and provides essential nitrogen to the host plant.</p>

<p>Drotaverine is an antispasmodic drug that is used to alleviate gastrointestinal and genitourinary smooth muscle spasms. This drug works by inhibiting phosphodiesterase-4 and increasing levels of cAMP leading to smooth muscle relaxation.</p>

<p>Inhibits RNAPII-mediated trasncription; immunosuppressant; anti-inflammatory</p>

<p>Antagonist of nicotinic acetylcholine receptors; nondepolarising muscle relaxant</p>

<p>Apremilast is the commercial name of a phosphodiesterase-4 (PDE4) inhibitor developed to treat chronic inflammatory disorders. Similarly to thalidomide, the apremilast molecule carries a phthalimide ring, but it lacks however the glutarimide ring needed to bind to cereblon, specifically targeted by thalidomide. As a drug, apremilast is indicated for the treatment of psoriasis and psoriatic arthritis.</p>

<p>Galloylpaeoniflorin is a bioactive compound derived from the roots of Paeonia lactiflora, a plant traditionally used in various herbal medicines. This compound plays a significant role in the realm of natural products, offering intriguing possibilities for research due to its complex chemical structure and biological activities.</p>

<p>N-Acetyl mescaline is a synthetic compound derived from the naturally occurring hallucinogen mescaline, which is sourced from the Peyote cactus (Lophophora williamsii) and other cacti. As an N-acetylated derivative, its chemical modification impacts the compound's mode of action, particularly in its interaction with serotonin (5-HT) receptors.This acetylation can alter the pharmacokinetics, potentially influencing its binding affinity and efficacy at various receptor sites, such as 5-HT2A. This receptor is notably implicated in the mechanism of action of classic psychedelics, mediating their sensory and cognitive effects.While mescaline is known for its strong psychotropic effects, N-Acetyl mescaline presents a modified profile, which may alter its psychoactive properties and duration of action. This compound is primarily studied in research settings to investigate its unique interactions with the neural network and its potential implications for neuroscience.</p>

<p>Agonist of hypothalamic neuropeptide LHRH</p>

<p>Ondansetron is a serotonin 5-HT3 receptor antagonist that is used to prevent vomiting and nausea in patients undergoing chemotherapy. This drug blocks the initiation of the vomiting reflex.</p>

<p>Mianserin is a tetracyclic antidepressant drug that has antihistaminic and hypnosedative properties. It is used to treat depression in adults and children, as well as other disorders such as chronic pain and irritable bowel syndrome. This drug’s mechanism of action is not fully understood but is said to block alpha-adrenergic, histamine H1 and serotonin receptors.</p>

<p>Nicardipine is calcium channel blocker drug that is used for the treatment of hypertension and angina. This drug can also be used in the treatment of asthma and is said to enhance the action of various antineoplastic agents.</p>

<p>2-[4-(Piperidin-3-yl)phenyl]-2H-indazole-7-carboxamide is a synthetic small molecule compound, which is a product of advanced medicinal chemistry. This compound is derived from a structured synthesis process focusing on the indazole core, which is known for its bioactive properties. The piperidin-3-yl phenyl moiety is intricately designed to optimize interaction with biological targets.</p>

<p>Naftopidil is an alpha adrenergic antagonist drug that is used to treat urinary symptoms and conditions related to benign prostatic hypertrophy. This drug works to relax smooth muscles by inhibiting alpha adrenergic receptors, thus allowing an improvement in urine flow.</p>

<p>Methotrexate is a chemotherapeutic and immunosuppressive medication, which is a synthetic analog of folic acid. Its source is through chemical synthesis, mimicking the structure of dihydrofolate in order to exert its effects. Methotrexate acts primarily by inhibiting the enzyme dihydrofolate reductase (DHFR), leading to a decrease in tetrahydrofolate production. This disruption in folate metabolism results in the inhibition of DNA, RNA, and protein synthesis, which affects rapidly dividing cells.Methotrexate is employed broadly in clinical oncology as an antineoplastic agent, particularly in the treatment of leukemias, lymphomas, breast cancer, and osteosarcoma. Additionally, it serves as a cornerstone for managing autoimmune diseases such as rheumatoid arthritis and psoriasis, where it helps modulate the aberrant immune response. The dual role of Methotrexate in oncology and immunosuppression underscores its versatility and critical importance in therapeutic regimens. However, its use demands careful monitoring due to potential adverse effects on non-cancerous cells and organ systems, necessitating precise dosage management and patient evaluation.</p>

<p>A potent inhibitor of EGFR with sensitizing and T790M resistance mutations, selective over the wild-type form of the receptor. Causes tumour regression in EGFR mutant T790M transgenic and xenograft models in vivo.</p>

<p>Gardos channel inhibitor</p>

<p>Astemizole is an antihistamine drug used to treat allergy symptoms. This drug is a histamine-1 receptor antagonist and does not cross the blood-brain barrier. Its binding to histamine receptors suppresses flare ups and pruritus.</p>

<p>Inhibitor of dopamine-?-hydroxylase</p>