Ligas Organometálicas

<p>Prostaglandin F2α receptor agonist</p>

<p>VE 822 is a potent and selective inhibitor of ATR protein kinase, which is derived through chemical synthesis with a high specificity for ATR over related kinases. ATR, or ataxia telangiectasia and Rad3-related kinase, plays a critical role in the cellular response to DNA damage and replication stress. VE 822 achieves its mode of action by interfering with ATR’s catalytic activity, thereby halting the DNA damage response and rendering cancer cells more susceptible to DNA-damaging agents.</p>

<p>Inhibitor of the intracellular copper chaperones ATOX1 and CCS</p>

<p>Selective and potent inhibitor of lysine acetyltransferases KAT6A and KAT6B with IC50 values of 8 nM and 28 nM, respectively. The compound is a reversible competitor of acetyl coenzyme A domain of KAT6A/B enzymes. It inhibits MYST-catalysed histone acetylation and potentiates senescence in vitro and in zebrafish model of hepatocellular carcinoma. The compound opened the door to a new class of cancer therapeutics that could potentially direct the cancer cells in senescence or permanent dormancy.</p>

<p>COX-2 inhibitor; anti-inflammatory</p>

<p>Saha Chloroalkane T1 is a specialized chemical compound, typically categorized as a chloroalkane. It emerges from a synthetic process involving the chlorination of hydrocarbons, specifically alkanes, which serves as its primary source. The mode of action for chloroalkanes like Saha Chloroalkane T1 involves the stable incorporation of chlorine atoms, enhancing reactivity and providing versatility in chemical reactions.</p>

<p>Idelalisib is a pharmaceutical drug that functions as a PI3Kδ inhibitor, developed through synthetic chemical processes. Its mode of action involves selectively targeting and inhibiting phosphatidylinositol 3-kinase delta (PI3Kδ), a lipid kinase that plays a crucial role in the signaling pathways responsible for cell proliferation, survival, and differentiation. By inhibiting this enzyme, Idelalisib effectively impedes pathways that are often hyperactivated in certain hematologic malignancies, thereby exerting antitumor effects.</p>

<p>Bexarotene is a retinoid and antineoplastic agent that is used for the treatment of solid tumours and t-cell lymphomas. It inhibits the growth in vitro of some tumor cell lines of hematopoietic and squamous cell origin and research has shown that it induces tumor regression in vivo in some animal models.</p>

<p>Afatinib is a small molecule that inhibits the activity of cellular kinases that are involved in the progression of cancer. It is an Irreversible inhibitor of three members of the ErbB family. This molecule binds covalently to cysteine 797 residue in HER2 and blocks downstream cellular signalling which inhibits cellular growth and promotes apoptosis. It has been researched for the treatment of non-small cell lung cancer (NSCLC), breast cancer, pancreatic cancer and colorectal cancer.</p>

<p>Phosphodiesterase 5 inhibitor; anti-impotence drug</p>

<p>Carmustine is a DNA alkylating agent which also cross-links DNA. As a result, Carmustine disrupts the function of DNA, resulting in the arrest the cell cycle and apoptosis. Consequently these properties of Carmustine, in addition to its ability to easily transmit through the blood-brain barrier, means it can be used as a cancer treatment, treating cancers such as, breast, ovarian and pancreatic as well as lymphomas and leukemias. Furthermore Carmustine can contribute to cytotoxic effects through its ability to carbamoylate DNA repair enzymes and proteins.</p>

<p>Agonist of μ opioid receptor; irritable bowel disease treatment</p>

<p>Antirheumatic; immunosuppressant; neuroprotective; neuroregenerative</p>

<p>A specific inhibitor of Bone Morphogenetic Protein (BMP) type 1 receptors ALK2 and ALK3 (IC50  &lt; 0.5 µM). Dorsomorphin analog that exclusively targets the BMP but not VEGF signaling. It is able to inhibit the BMP-induced Smad1/5/8 activation but not the p38/MAP kinase signaling or Activin A-induced Smad2 activation.</p>

<p>6-OAU is a chemical compound categorized as a cytokinin-like molecule, which is derived from natural plant sources. It functions by modulating gene expression and hormone pathways involved in various plant growth and developmental processes. The mode of action of 6-OAU largely revolves around mimicking the activity of cytokinins, essential plant hormones that regulate cell division, shoot and root growth, as well as delay senescence.</p>

<p>Platinum-based anti-tumor drug</p>

<p>Carmofur is an antineoplastic agent that is used to treat various cancers such as breast and colorectal cancer. This drug is a derivative of fluorouracil. Carmofur is an inhibitor of the human acid ceramidase, a lysosomal amidase involved in the development of cancer cells.</p>

<p>Inhibits actin polymerization</p>

<p>A metabolite of arachidonic acid, synthesised by COX enzymes and prostaglandin E synthases (PGEs). Binds to EP1, EP2, EP3 and EP4 receptors with high affinity (Kd &lt; 10 nM). Therapeutic potential for analgesia, pain relief and arthritic diseases. Enhances differentiation and expansion of iPSC-derived hematopoietic progenitor cells.</p>

<p>Inhibitor of BACE1 protease</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>Sorafenib is a drug that belongs to the class of multikinase inhibitors. It inhibits a number of kinases, including the Mcl-1 protein, which is involved in apoptosis along with blocking picolinic acid (PA), an endogenous metabolite involved in apoptosis signal transduction. Sorafenib also binds to epidermal growth factor receptor (EGFR) on the surface of cancer cells, inhibiting the production of proteins that are required for angiogenesis, thus blocking the formation of new blood vessels. Sorafenib may also inhibit P-glycoprotein (Pgp) activity. Overall, these cytotoxic effects give Sorafenib anti-tumor properties, inhibiting angiogenesis and cellular transformation, which are the two main processes of tumor growth and metastasis. Sorafenib tosylate has been shown to be effective against a range of solid tumors such as breast, prostate and lung cancers and is also used for the treatment of metastatic colorectal cancer and renal cell carcinoma. A combination therapy group found that sorafenib was more effective when used with interferon alfa-2b for the treatment of advanced renal cell carcinoma. Sorafenib also has the potential for drug interactions with other drugs that are metabolized by cytochrome P450 enzymes.</p>

<p>Inhibitor of pan-class I PI3K family of lipid kinases; antineoplastic</p>

<p>Inhibitor of TGF-α, CTGF, ERK1/2, NF-κB and FasL; anti-inflammatory</p>

<p>Melatonin is a neurotransmitter produced by the pineal gland that is involved in the regulation of sleep-wake cycles. It can be used to treat several conditions like shift work disorders, insomnia, jet lag, and alterations of the circadian rhythm. Some authors also proposed the use of melatonin against cognitive disorders. In an interesting research conducted on zebrafish, it was found that memory formation occurs better during daytime compared to nighttime, suggesting a role of melatonin in this process. When melatonin was administered during the daytime it caused reduced memory formation. On the contrary, removing the pineal gland or treating the fish with a melatonin antagonist significantly improves nighttime memory formation.</p>

<p>Ivabradine is a HCN channel blocker that is used to reduce the risk of hospitalization for worsening heart failure and used in the treatment of symptomatic heart failure. This drug acts by inhibiting the “funny” channel pacemaker current (If) which results in a lower heart rate and allows for more blood flow to the myocardium.</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>Troxipide is a gastric cytoprotective agent that is used for the treatment of gastroesophageal reflux disease (GERD). It has anti-inflammatory, anti-ulcer and mucus secreting properties. This drug inhibits proinflammatory mediators in order to restore the normal gastric mucosa.</p>

<p>Dual inhibitor of the adaptor protein 2-associated kinase 1 (AAK1) and BMP2-inducible kinase (BMP2K) with IC50 values of 270 nM and 1 μM, respectively. In a recent study, SGC AAK1 1 stabilised β-catenin, inhibited phosphorylation of the AP2 complex subunit mu protein (AP2M1) and activated Wnt signalling in in vitro experiments._x000D_</p>

<p>Inhibits interaction between small GTPase Rab27a and its effector JFC1 (synaptotagmin-like protein1, Slp1). These proteins regulate neutrophil exocytosis, decrease neutrophil infiltration in liver and kidneys and reduce extracellular ROS production by NAPDH oxidase. Thus, nexinhibib20 suppresses systemic inflammation.</p>

<p>Selective inhibitor of the platelet derived growth factor receptor PDGFRβ with IC50 value of 4.2 nM. JNJ 10198409 inhibits the PDGFRβ kinase activity and its downstream signalling leading to anti-proliferative and anti-angiogenic effects, which were confirmed in various tumoral cell lines.</p>

<p>Inhibitor of CDK4/6 serine/threonine kinases; antineoplastic</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>Brimonidine-D-tartrate is a selective alpha-2 adrenergic agonist, which is a pharmacological compound derived synthetically, targeting specific receptor subtypes in the adrenergic receptor family. Its mode of action involves reducing aqueous humor production and increasing uveoscleral outflow in the eye, thereby lowering intraocular pressure. Additionally, it induces peripheral vasoconstriction, playing a role in reducing redness in rosacea.</p>

<p>Dapoxetine is a drug that belongs to the group of selective serotonin reuptake inhibitors (SSRIs). It is used to treat premature ejaculation. This drug inhibits the serotonin transporter allowing for an increased action of serotonin at the postsynaptic cleft, thus promoting ejaculatory delay.</p>

<p>Vipivotide tetraxetan is a radioactive therapeutic agent, which is a radioligand conjugate composed of a DOTA chelator linked to a targeting moiety. The source of this compound lies in its synthesis, where the DOTA ligand is conjugated to a peptide or small molecule that targets specific cell surface antigens expressed on cancer cells.</p>

<p>Ziprasidone is an atypical antipsychotic drug that is used to manage schizophrenia, bipolar mania, and agitation. This drug binds to serotonin and dopamine receptors. As a result it enhances modulation of mood and improves overall cognition.</p>

<p>Inhibitor of stearoyl-CoA desaturase SCD1 with IC50 of 6.3 nM, as measured in the SCD1-expressing human microsomes.  A 939572 exhibited anticancer activity as it reduced cell proliferation and triggered cell killing in human non-small cell lung carcinoma cells. A 939572 inhibited tumour growth in an in vivo model for gastric carcinoma and reduced the oleic acid:stearic acid ratio in mouse liver and plasma.</p>

<p>Ebselen is a non-toxic organoselenium compound with antioxidant, anti-inflammatory and cytoprotective properties. Ebselen is an inhibitor of lipoxygenases, nitric oxide (NO) synthases, protein kinase C, H+/K+-ATPase, thioredoxin reductase and NADPH oxidase. Recently, ebselen has been identified by several studies as a covalent inhibitor of the main protease Mpro from coronaviruses. For the SARS-CoV-2 main protease Mpro, the IC50 value is 0.67 μM and EC50 is 4.57 μM.</p>

<p>Inhibits mTORC1 and mTORC2 serine/threonine kinases</p>

<p>Piracetam analog; AMPA receptor allosteric modulator</p>

<p>Leflunomide is a pyrimidine synthesis inhibitor drug that is used to treat rheumatoid arthritis. Although its mechanism of action is not fully determined, this drug has shown to interfere with cell cycle progression by inhibiting dihydroorotate dehydrogenase and has shown antiproliferative activity. As a result of this, it interferes with the expansion of activated autoimmune lymphocytes. Additionally, Leflunomide is a tyrosine kinase inhibitor.</p>

<p>Clomipramine is a tricyclic antidepressant drug that inhibits the reuptake of serotonin, norepinephrine, and dopamine. It is used to treat obsessive compulsive disorder, panic disorders and cataplexy. Additionally, Clomipramine is shown to modulate immune activation and shows constant anti-inflammatory properties at therapeutic concentrations by consistently decreasing pro-inflammatory cytokines.</p>

<p>Inhibitor of glucose uptake via GLUT1 and GLUT4 transporters, promoting intracellular glucose deprivation. The compound is a chemical sensitizer to the FAS cell death receptor and is able to break down the resistance of caspase activation. It has potential for anti-cancer therapy as it modulates the Warburg effect in cancer cell lines.</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>Modulator of RBP protein; activator of sphingomyelinase; pro-apoptotic</p>

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

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

<p>Trkc active human is a bioengineered protein, which is a synthetic derivative of the TRKC (tropomyosin receptor kinase C) receptor. This product is derived from recombinant DNA technology, utilizing expression systems to produce a functionally active protein that mimics the natural receptor found in human cells. Its mode of action involves the specific binding and activation of neurotrophin-3 (NT-3), a critical signaling molecule in the nervous system.</p>

<p>(2R)-Arimoclomol maleate is an investigational pharmaceutical compound, which is an orally bioavailable small molecule with pharmacological activity primarily targeting cellular protein homeostasis mechanisms. This therapeutic agent is derived from molecular chaperones and operates by selectively enhancing the expression of heat shock proteins (HSPs). The mechanism of action involves the modulation of the heat shock response, wherein (2R)-Arimoclomol maleate amplifies the natural cellular defense pathways against protein misfolding and aggregation.</p>

<p>Inhibitor of VEGFR, PDGR, c-Kit and Ret; inhibitor of angiogenesis</p>

<p>5-Fluoro-1-(tetrahydro-2-furyl)uracil is a chemotherapeutic agent, which is a synthetic derivative of uracil. This compound is developed from modified nucleosides with the aim of enhancing antitumor efficacy. Its mechanism of action involves the inhibition of thymidylate synthase, leading to a disruption in DNA synthesis. By integrating into RNA and DNA, it ultimately impedes tumor cell proliferation due to RNA processing interference and DNA damage.</p>

<p>Diphenidol is an antiemetic agent used for the treatment and prevention of nausea and vomiting associated with various conditions. Its mechanism of action is not well known but it is thought to diminish vestibular stimulation and depress labyrinthine function.</p>

<p>Inhibitor of EIF2AK3/PERK kinases</p>

<p>Wee1 inhibitor with an IC50 of 5.2 nM</p>

<p>AZD-7648 is a selective inhibitor of DNA-dependent protein kinase (DNA-PK), which is a pivotal enzyme involved in the non-homologous end joining (NHEJ) pathway of DNA repair. This product is derived from extensive chemical synthesis and optimization, designed for its specificity and efficacy in inhibiting DNA-PK activity. The mode of action involves binding to the ATP-binding site of DNA-PK, thereby obstructing its ability to facilitate the repair of double-strand DNA breaks.</p>

<p>Fibroblast growth factor receptor inhibitor</p>

<p>Agomelatine is a potent agonist at melatonin receptors and an antagonist at serotonin receptors. It was designed to treat mood disorders, such as depression. It has been shown to improve mood by increasing the levels of certain neurotransmitters in the brain such as dopamine and noradrenaline. Agomelatine has beneficial phase-shifting effects in humans; it causes a sleep phase advance, a drop in body temperature, and an initial release of melatonin. According to controlled human studies, Agomelatine is equally effective at treating severe depression as the SSRI antidepressants paroxetine and sertraline.</p>

<p>Inhibits non-receptor tyrosine kinase BTK; antineoplastic</p>

<p>Inhibits p38 MAP kinase; anti-inflammatory; neuroprotective</p>

<p>Microtubule disrupter; anti-mitotic drug; anti-cancer alkaloid</p>

<p>Zileuton is an inhibitor of the 5-lipoxygenase enzyme, thus preventing the leukotrienes LTE4, LDT4, LTB4 and LTC4 from being formed. This in turn reduces inflammation, bronchoconstriction and mucus secretion in the airways. As a result, Zileuton can be used in the treatment and management of asthma and allergic rhinitis. Studies have shown that Zileuton has the potential to reverse dementia-related brain damage.</p>

<p>Vasopressin analog; vasoactive agent</p>

<p>17:0-20:4Pi (4) P is a synthetic phosphoinositide, which is a type of phospholipid. It is typically sourced from laboratory synthesis, often incorporating stable isotopes or specific fatty acid chains to mimic natural compounds found in cell membranes. This product functions primarily as a probe in biochemical experiments, particularly for studying lipid signaling pathways within cells.</p>

<p>Fexofenadine is a selective histamine-1 receptor antagonist that is used to treat the symptoms of seasonal allergies. It does not cross the blood-brain barrier and carries little-to-no activity at off targets. This drug binds to the inactive form of the H1 receptor and inhibits its activation and downstream effects.</p>

<p>Promotes binding of vWf to glycoproteins on platelets, inducing aggregation</p>

<p>Positive allosteric modulator (PAM) of cannabinoid receptors CB2. The C2 modulator is the first synthetic PAM of CB2 receptors with antinociceptive properties, which were observed in a mouse model of neuropathic pain.</p>

<p>Antagonist of cardiac potassium channel HERG; anti-psychotic</p>

<p>Ondansetron is a serotonin 5-HT3 receptor antagonist that has been shown to inhibit the effects of serotonin in the gastrointestinal tract, thereby preventing nausea and vomiting that is caused by cancer chemotherapy. Chemotherapy and radiotherapy are associated with the release of serotonin (5-HT) from enterochromaffin cells of the small intestine, initiating a vomiting reflex through stimulation of 5-HT3 receptors located on vagal afferents. Ondansetron blocks the initiation of this reflex. The drug binds to receptors on cells in the gastrointestinal tract that are normally activated by serotonin, thereby blocking its effect.</p>

<p>Montelukast is a leukotriene receptor antagonist that blocks the binding of leukotrienes to their receptors. It is used for the treatment of chronic cough, as well as for the relief of symptoms of seasonal and perennial allergic rhinitis. Montelukast binds to leukotriene receptors on cells in the airways, preventing them from attaching to leukotrienes and triggering an inflammatory response. This drug has been shown to be effective in controlling asthma symptoms by reducing bronchial hyperresponsiveness and relieving respiratory obstruction due to inflammation. Montelukast also has anti-inflammatory properties, which are thought to be due to its ability to inhibit production of pro-inflammatory cytokines such as IL-6.</p>

<p>Agonist of β3-adrenoreceptors with thermogenic properties and potential to control diet-induced obesity. The compound reversed obesity in adult rats and was effective even in animals that continued to feed on high-fat food. It caused the enlarged white adipocytes to shrink and triggered remodelling of the white adipose tissue.</p>

<p>Inhibitor of ABC transporters; oral bioenhancer for anti-cancer therapy</p>

<p>Potent and selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 of 2.4 nM. Its anti-inflammatory activity was examined in a mouse model for acute colitis. The compound protected from intestinal inflammation by prevention of infiltration of CD19+ B-cells into the lamina propria of colonic epithelium and attenuated neutrophil activation. Its broad anti-inflammatory response involved decrease in 24 inflammatory chemokines and cytokines. Also, it is a potent inhibitor of cell proliferation in pancreatic cancer cell lines.</p>

<p>Palonosetron is a selective serotonin 5-HT3 receptor antagonist. It is an antinauseant and antiemetic agent that has been shown to be effective in preventing nausea and vomiting induced by cancer chemotherapy, radiotherapy, or surgery. By directly inhibiting serotonin activity in the region postrema and the chemoreceptor trigger zone, the inhibition of 5-HT3 receptors also prevents the visceral afferent stimulation of the vomiting center.</p>

<p>Inhibits MEK1 and MEK2 kinases; targeted therapy for melanoma</p>

<p>(R)-Phenylephrine is a non-selective α1-adrenoceptor agonist that can be used as a bronchodilator or vasopressor. The biological effects of this compound are due to its ability to cause relaxation of smooth muscle cells and increase blood pressure by stimulating alpha-adrenergic receptors in the body. Also, this drug is used to relieve nasal discomfort caused by colds and allergies and is used to relieve sinus congestion and pressure.</p>

<p>Clebopride is a dopamine antagonist drug that is used in the treatment of symptoms associated with gastrointestinal disorders. This drug is also used to treat nausea and vomiting. Clebopride blocks dopamine to allow an increase in the release of acetylcholine so that muscle movement in the digestive system is increased.</p>

<p>Potent and selective positive allosteric modulator (PAM) of metabotropic glutamate receptor mGlu4. Valiglurax is orally bioavailable and CNS-penetrant mGlu4 PAM in preclinical development for the Parkinson’s disease therapy and alleviation of the motor symptoms.</p>

<p>Ifosfamide is an alkylating agent and immunosuppressive drug used in chemotherapy for the treatment of various cancers such as ovarian, testicular, cervical and bladder. This drug interferes with the normal process of DNA replication causing damage to the DNA in cancer cells hence preventing them from growing and dividing.</p>

<p>Inhibitor of DNA topoisomerase I</p>

<p>Spla2-X Inhibitor 31 is a chemical inhibitor specifically targeting the human secreted phospholipase A2 group X (sPLA2-X), which is derived synthetically through chemical synthesis. Its mode of action involves binding to the active site of sPLA2-X, effectively blocking its enzymatic activity. This enzyme catalyzes the hydrolysis of phospholipids, leading to the release of arachidonic acid, a precursor for bioactive lipids involved in inflammation and other cellular processes.</p>

<p>Competitive antagonist of ionotropic glutamate receptors of AMPA and kainate subfamilies. Reported anti-convulsant activity in seizures models induced by electrostimulation, drugs or genetic predisposition. Pro-convulsant effects in Theiler's murine encephalomyelitis virus-induced (TMEV) seizure model.</p>

<p>Cetirizine is a selective histamine-1 antagonist drug used for the treatment of allergies. One of the common uses is for a condition called allergic rhinitis. As Cetirizine is an antihistamine, its main mode of action is by selectively inhibiting H1 receptors. In vivo and ex vivo animal models have shown insignificant anticholinergic and antiserotonergic effects.</p>

<p>Activates muscarinic GPCR DREADDs, which are unaffected by the endogenous ligand acetycholamine of the parent receptor. Clozapine is metabolized to clozapine N oxide in the liver, mainly by CYP3A4. Has anti-seizure effects, when induced by chemoconvulsants pilocarpine and picrotoxin.</p>

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

<p>CMX 001 is an antiviral medication that is a prodrug of cidofovir, which is derived from nucleoside analogs with direct inhibition of viral DNA polymerase. This mechanism of action allows CMX 001 to effectively disrupt viral replication by integrating into viral DNA and halting its synthesis. Designed to target a broad range of DNA viruses, this drug offers a robust means of controlling viral infections.</p>

<p>Crizotinib is a drug that belongs to the group of tyrosine kinase inhibitors. It is used in the treatment of cancers, including non-small cell lung cancer, small cell lung cancer, and other types of solid tumours. Crizotinib inhibits the activity of the tyrosine kinase ALK or anaplastic lymphoma kinase, which is involved in many signalling pathways and biological processes. The inhibition of this enzyme leads to decreased energy metabolism, reduced mitochondrial membrane potential and increased susceptibility to apoptosis.</p>

<p>Bicuculline is a phthalide-isoquinoline compound and is a competitive GABA receptor antagonist. It blocks GABA’s inhibitory action, mimicking epilepsy. This compound is used in research to better study epilepsy.</p>

<p>Inhibits urate anion exchanger 1 (URAT1); therapeutic use in gout</p>

<p>Eplerenone is a drug known as an aldosterone antagonist. It is a type of potassium-sparing diuretic that is used to treat chronic heart failure and high blood pressure, particularly for patients with resistant hypertension due to elevated aldosterone. It does this by blocking the activity of the enzyme that produces aldosterone, which increases levels of sodium and water in the body. This leads to a decrease in blood pressure.</p>

<p>Etodolac is a non-steroidal anti-inflammatory drug (NSAID) used to treat osteoarthritis and rheumatoid arthritis. It is also used to treat acute pain. This drug works by inhibiting prostaglandin synthesis from the inhibition of the enzyme cyclooxygenase.</p>

<p>Agonist of ghrelin receptor; growth hormone secretagog</p>

<p>Inhibitor of protein kinase CK2</p>

<p>Selective and potent inhibitor of 8-oxoguanine DNA glycosylase OGG1 with IC50 of 0.6 μM. OGG1 is a key enzyme in DNA repair mechanism called base excision repair (BER). The compound inhibits the hydrolysis of glycosidic bond required for the excision of 8-oxoguanine from double stranded DNA, which leads to accumulation of mutations. It has been proposed as monotherapy for certain types of cancers as well as adjuvant for cancer therapy with DNA damaging agents. It has potential to sensitize tumours for chemotherapy and inhibit development of drug resistance mechanisms.</p>