Ligands organométalliques

<p>Finasteride is an antiandrogenic drug that belongs to the group of 5-alpha reductase inhibitors, which are used for the treatment of benign prostatic hyperplasia and male pattern baldness. The conversion of testosterone to 5α-dihydrotestosterone (DHT) is blocked by type II 5α-reductase inhibition, which then results in significant increase in prostatic testosterone concentrations and minimal to moderate increases in serum and tissue DHT concentrations. A reduction in DHT concentration will cause a reduction in prostatic volume as DHT appears to be the main androgen responsible for stimulating prostatic growth.</p>

<p>Partial inverse agonist of benzodiazepine sites of the GABAA receptors with anxiogenic properties. FG 7142 is a pharmacological stressor which generates anxiety in humans and in experimental animals such as rhesus monkeys and rodents. FG 7142 also reduces food intake and frequency of feeding in male and female rats.</p>

<p>Farnesyl pyrophosphate synthase inhibitor</p>

<p>Increases VEGF via heme oxygenase-1 modulation; anti-ulcer agent</p>

<p>Fondaparinux sodium is an anticoagulant, which is a synthetic pentasaccharide based on the antithrombin-binding sequence of heparin. As a meticulously engineered compound, it is derived by chemical synthesis. Its mode of action involves the selective inhibition of factor Xa, a critical enzyme in the coagulation cascade. By binding specifically to antithrombin III, it enhances the inactivation of factor Xa, thereby interrupting the pathway that leads to thrombin formation and ultimately preventing fibrin clot formation.</p>

<p>Rofecoxib is a non-steroidal anti-inflammatory drug that is used to treat osteoarthritis, acute pain and migraine attacks. This drug is also a COX-2 inhibitor. As a result, it reduces inflammation and pain.</p>

<p>Apo-D human is a glycosylated lipocalin protein, which is primarily derived from human plasma. It plays a pivotal role in the regulation of lipid-related metabolic processes due to its ability to bind and transport various ligands, including steroids and lipids. The protein's mode of action involves its function as a shuttle for small hydrophobic molecules, impacting cholesterol metabolism and potentially influencing lipid-related signaling pathways.</p>

<p>Inhibitor of metalloendopeptidase neprilysin</p>

<p>Beta-adrenoceptor antagonist; anti-hypertensive</p>

Olanzapine is an antipsychotic drug present in formulations of certain medications used for the management of schizophrenia, bipolar disorder and agitation. This drug is an antagonist of 5-HT2A serotonin and dopamine (D1/2) receptors.

<p>Azelastine is an antihistamine drug that is used to treat allergic rhinitis. It inhibits the production of inflammatory mediators such as histamine and leukotrienes. It antagonizes the actions of histamine, resulting in relief of allergy symptoms. Azelastine has been shown to inhibit mediators of mast cell degranulation like leukotrienes in the nasal lavage of patients with rhinitis and possesses mast cell-stabilizing qualities that limit the production of interleukin-6, tryptase, histamine, and TNF-alpha2 from mast cells.</p>

<p>Inhibitor of the histone methyltransferase SETD8 that supresses methylation of the K20 residue in histone 4. UNC 0379 treatment of human glioma reduced recruitment of 53BP1 protein to double strand breaks and sensitised cells to radiotherapy without altering cell cycle kinetics.</p>

<p>Muscarinic acetylcholine receptor agonist</p>

<p>N-Desmethyl ibandronate sodium is a white crystalline solid with a melting point of 238-240 °C. It has versatile building block, complex compound and research chemicals applications. It is an intermediate used in the synthesis of other compounds, such as speciality chemicals, useful intermediates and useful scaffolds. N-Desmethyl ibandronate sodium can be used in reactions that require high quality and high purity products.</p>

<p>VEGFR2 a tyrosine kinase receptor inhibitor; antineoplastic</p>

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

<p>Antagonist of dopamine (D2), serotonin (5-HT2A) and histamine H1 receptors</p>

Lestaurtinib is a multitarget tyrosine kinase inhibitor of the JAK, FLT-3 and TrkA families of tyrosine kinases at nanomolar concentrations. It inhibits proliferation and induces apoptosis in vitro. Lestaurtinib is a FDA approved orphan drug for acute myeloid leukemia.

<p>Inhibitor of vacuolar-type proton pump</p>

<p>Selective inhibitor of the mutated RET variant RETV804M, which is the anticipated drug-resistant RET mutant that can occur in tumours treated with kinase inhibitors. The compound has a biochemical IC50 of 0.02 µM and selectivity for purified RETV804M over purified RET and KDR of 3.7 and 110, respectively. The efficacy of the compound was shown also in cell cultures with IC50 of 4.4 µM, and cell assay selectivity for RETV804M over RET and KDR of 0.89 and 2.3, respectively.</p>