Organometallic Ligands

<p>Temozolomide is an imidazotetrazine alkylating agent. It has anti-tumor activity against a broad spectrum of tumors, such as leukemias, lymphomas and solid tumors. Temozolomide induces G2/M arrest, preventing cells from entering mitosis and, therefore, apoptosis. As a drug resistance-modifying agent it is used for studying drug resistance mechanisms in glioblastoma cell lines.</p>

<p>AP 1903 is a synthetic small molecule, which acts as a dimerizer ligand. It is derived from the modification of the macrolide antibiotic rapamycin to remove its immunosuppressive effects, thus enabling targeted control of cellular processes. The mode of action involves binding to engineered receptors on the cell surface that contain drug-dependent domains. This binding triggers the dimerization of these receptors, leading to downstream signaling and subsequent cellular responses.</p>

<p>A highly potent antagonist of group II metabotropic glutamate receptors (IC50 values = 21 nM and 14 nM at human mGluR2 and mGluR3 respectively). LY 341495 also inhibits group I and III mGluRs with lower potencies (IC50 values = 0.17, 7.8 and 8.2 µM at mGluR8, mGluR1a and mGluR5a respectively). There has been contradicting findings on the antidepressant and anxiolytic activities of this compound. Enhanced cognitive function and locomotor activity have also been described for LY 341495.</p>

<p>Inhibits FGFR family of kinases; antineoplastic; anti-angiogenic</p>

<p>Nisoldipine is a calcium channel blocker that is used to treat hypertension. It acts on vascular smooth muscle cells by blocking voltage-gated L-type calcium channels. By inhibiting the influx of calcium in smooth muscle cells, Nisoldipine prevents calcium-dependent smooth muscle contraction and subsequent vasoconstriction.</p>

<p>Pravastatin is an HMG-CoA reductase inhibitor that is used to lower lipid levels and manage cardiovascular events such as strokes and myocardial infarction. This drug inhibits HMG-CoA reductase allowing for a reduction in the level of cholesterol.</p>

<p>KBU2046 is an antimicrobial peptide, which is derived from natural or synthetic peptide sequences with potential therapeutic properties. It exerts its effects by disrupting the structure and integrity of bacterial cell membranes through the formation of pores or micelles. This action alters membrane permeability, ultimately leading to cell lysis and death.</p>

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

<p>Fenpiverinium is an anticholinergic and antispasmodic agent that is used to treat muscle spasms and pain. Fenpiverinium inhibits the production of acetylcholine at muscarinic receptors by inhibiting cholinesterase enzymes. Also it has an effect on autoimmune diseases and non-immune-related diseases such as lupus erythematosus, rheumatoid arthritis, psoriasis, and Crohn's disease. It is also effective against pain caused by diabetes mellitus.</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>Dopamine reuptake inhibitor; ligand of sigma receptors</p>

<p>Glucocorticoid receptor agonist; anti-inflammatory</p>

<p>17:0-20:4 Pi (4,5) P2 is a synthetic phosphoinositide, which is a chemically defined lipid derived from laboratory synthesis. It features a specific acyl chain composition with a heptadecanoic acid (17:0) at the sn-1 position and an arachidonic acid (20:4) at the sn-2 position. This phosphoinositide mimics naturally occurring phosphatidylinositol 4,5-bisphosphate (PI(4,5)P2), an essential component of cellular membranes.</p>

<p>Inhibitor of CDK2, JAK2 and FLT3; anticancer</p>

<p>Inhibits MET, VEGFR1-3, Tie and Ron tyrosine kinases; antineoplastic</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>Aniracetam is a nootropic drug that is used to alleviate memory disturbances caused by cerebrovascular disease and brain disorders. This drug has anti-depressive and anxiolytic properties and is said to target serotonin and dopamine receptors.</p>

<p>Inhibitor of the transient receptor vanilloid channel, specific for the TRPV2 subtype with IC50 value of 0.46 μM. In human prostate cancer cells, SET2 inhibited cell migration but did not affect cell survival. SET2 has been proposed as a potential anti-cancer and anti-metastatic agent.</p>

<p>Hispolon is a naturally occurring polyketide compound, which is derived from the mushroom Phellinus linteus, commonly found in Asia. This compound is known for its diverse biological activities, primarily functioning as an antioxidant, anti-inflammatory, and antitumor agent. The mode of action of hispolon involves the modulation of multiple cellular pathways. It has been shown to induce apoptosis in cancer cells by triggering intrinsic and extrinsic apoptotic pathways. Additionally, hispolon exhibits the ability to inhibit the NF-κB pathway, subsequently decreasing the expression of pro-inflammatory cytokines and leading to an anti-inflammatory effect.</p>

<p>Dimenhydrinate is a drug that was initially used as an antihistamine to treat symptoms of allergies such as watery eyes, sneezing and a runny nose, however it is now used for the treatment and prevention of nausea, vertigo and motion sickness. Dimenhydrinate is a combination of diphenhydramine and 8-chlorotheophylline. Its antiemetic properties are thought to be produced from diphenhydramine’s antagonism of H1 histamine receptors. Also, it is believed to have antimuscarinic effects that minimize disturbances to the body’s equilibrium.</p>