Organometallic Ligands

<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>Pemirolast is an antihistamine drug that is used for the treatment of allergies such as hay fever and allergic conjunctivitis. This drug binds to the histamine H1 receptor and blocks the action of histamine which results in the relief of allergic symptoms brought on by histamine. This drug is also a mast cell stabilizer.</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>Activates CFTR channels</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>Inhibitor of protein kinase CK2</p>

<p>NAP is a neuroprotective peptide, which is derived from activity-dependent neuroprotective protein (ADNP), with a mechanism involving microtubule stabilization and neuronal protection. It exhibits the ability to protect neurons from various types of damage, including oxidative stress and conditions mimicking neurodegenerative diseases. NAP enhances axonal transport and increases the resilience of neurons to insults that would typically result in cell death. This peptide has shown promise in preclinical studies for its potential to halt or reverse cognitive decline, making it a focal point for research into therapeutic strategies for disorders like Alzheimer's disease and other tauopathies. The peptide operates by binding to microtubules, promoting stability, and facilitating efficient transport of cellular components. Studies have highlighted its role in traversing the blood-brain barrier, which makes it a viable candidate for central nervous system-targeted therapies. Researchers continue to explore its efficacy and possible applications in improving cognitive function and providing neuroprotection in aging populations.</p>

<p>Pan-class I phosphatidylinositide 3-kinase (PI3K) inhibitor (IC50 = 3, 33, 3 and 75 nM at catalytic subunits p110α, p110β, p110δ and p110γ respectively). Inhibits proliferation in several cancer cell lines, such as glioblastoma, breast and prostate cancer cells. Has synergistic anti-cancer effect in combination with MEK/ERK kinase inhibitor GDC-0973 (cobimetinib).</p>

<p>An irreversible GSK-3β inhibitor that reduces phosphorylation of tau proteins, protects from neuronal loss and has cognitive and behavioural benefits in murine models. Studied for its potential as a therapeutic agent in Alzheimer’s disease and other neurodegenerative diseases. Tideglusib was also shown to inhibit the main protease Mpro from the SARS-CoV-2 virus with IC50 of 1.55 μM.</p>

<p>Imiquimod maleate is an immune response modifier, which is a synthetic compound sourced from chemical synthesis. Its mode of action involves the activation of the immune system through the stimulation of toll-like receptor 7 (TLR7), leading to the induction of various cytokines, such as interferon-alpha, that initiate an antiviral and anti-tumor response.</p>

<p>Inhibits YAP/Tead transcriptional activity. Has anti-tumour effects on oesophageal adenocarcinoma with therapeutic potential in combination with 5-FU. Involved in ferroptosis, mediated by iron-dependent ROS.</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>Inhibitor of glutathione peroxidase GPX4</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>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>Inhibits platelet glycoprotein IIb/IIIa receptors</p>

<p>Potent inhibitor of γ-secretase. LY 411575 inhibited production of amyloid β (Aβ) peptides with IC50 of 0.078 nM in vitro as well as decreased levels of Aβ40 and Aβ42 amyloids in brain of a mouse model for Alzheimer’s disease. In vitro studies confirmed that LY 411575 inhibited cleavage of Notch receptor at S3 site with IC50 of 0.39 nM, which blocked Notch activation and downstream signalling, leading to apoptosis in primary and immortalized Kaposi's sarcoma cells.</p>

<p>mGluR5 antagonist</p>

<p>Regaloside D is a natural product derived from plant sources, specifically isolated from certain species known for their bioactive properties. It functions as a glycoside, a compound in which a sugar is bound to a non-carbohydrate moiety, potentially influencing a variety of cellular processes through its interaction with specific molecular targets.</p>

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