Ligands organométalliques

<p>Thyrotropin-releasing hormone (TRH) receptor agonist; TRH analogue</p>

<p>Inhibitor of proteaseγ‐secretase, which allows to modulate of the activity of γ‐secretase substrates Notch, E-cadherin, ErbB4, and amyloid precursor protein (APP). The compound can inhibit the growth of tongue carcinoma cells by arresting cell cycle in G0–G1 phase, modulate the activity of Notch1 receptor and Caspase-3 protease and induce apoptosis. It was also demonstrated that this inhibitor reduces the levels of β-amyloid peptide in the brain of mice model for Alzheimer’s disease. This compound also enhances the neuronal differentiation embryonic cells.</p>

<p>Antagonist of platelet activating factor</p>

<p>Endothelin A receptor antagonist</p>

<p>A potent small-molecule activator of UNC-51-like kinase 1 (ULK1), a serine-threonine kinase involved in autophagy. Promotes cytoprotective autophagy in MPP+-treated SH-SY5Y cells, via the ULK complex. Improves motor dysfunction and reduces loss of dopaminergic neurons, mediated by MPTP, in in vivo models of Parkinson’s disease.</p>

<p>GnRH super-agonist</p>

<p>Dexrazoxane is a cytoprotective drug that is used in chemotherapy to provide cardio-protection against anthracycline toxicity. It is an antimitotic agent with immunosuppressive properties. Dexrazoxane works by binding to iron in the cell, preventing it from being released. Dexrazoxane is also a catalytic inhibitor of topoisomerase II.</p>

<p>Selective antagonist of the serotonin receptors 5-HT2A with subnanomolar affinity. The compound has clozapine-like anti-psychotic properties and more favourable CNS safety profile than traditional anti-psychotics. MDL 100907 has been used in studies on antisocial behaviour in mice and shown that the blockage of 5-HT2A receptors leads to decreased post-traumatic aggression and bradycardia.</p>

<p>Inhibitor of protein kinase CK1</p>

<p>Azilsartan is an angiotensin II receptor blocker that is used to treat hypertension. It blocks the binding of angiotensin II receptors to the AT1 receptor by selectively binding to AT1 receptors as an antagonist, blocking the vasoconstrictor and aldosterone-secreting effects of angiotensin II.</p>

<p>Selective vasopressin receptor V2 agonist</p>

<p>Selective inhibitor of the transforming growth factor beta receptor TGFβ1. RepSox can replace Sox, a transcriptional factor required for cell self-renewal, in reprogramming of adult cells to induced pluripotent stem cells (iPSCs). In the cloned interspecies embryos, RepSox induced expression of pluripotency regulatory genes Oct4 and Nanog, improved viability and developmental potential of embryos in the pre-implantation stage.</p>

<p>Tandospirone is a psychotropic drug that acts as a selective serotonin receptor partial agonist. It is derived from a synthetic source, specifically targeting the 5-HT1A receptors in the brain. Tandospirone modulates serotonergic neurotransmission by binding to these receptors, which are associated with mood regulation. This action results in the anxiolytic and antidepressant effects observed with the drug.</p>

<p>Eltrombopag is an agonist of thrombopoietin receptor TpoR, which triggers activation of the JAK2/STAT5 signalling pathway. This drug is indicated in individuals with thrombocytopenia since it leads to increased proliferation of megakaryocyte progenitor cells and increased production of platelets. Eltrombopag also enhances expansion of human umbilical cord blood hematopoietic stem/primitive progenitor cells and promotes hematopoiesis.</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>RIPK2 protein kinase inhibitor; EGFR inhibitor</p>

<p>Inhibitor of poly (ADP-ribose) polymerase enzyme; antineoplastic</p>

<p>Pidotimod is a small molecule (dipeptide) that acts as immunomodulator. It activates the immune system by binding to Toll-like receptor (TLR) 4 and TLR2 and it is involved in the regulation of TLRs signaling pathways. Pidotimod has chemokine activity on CXC chemokine receptor 3 (CXCR3) that triggers monocyte adhesion and migration by activation of tyrosine phosphorylation-based cell signaling. Recent studies showed that pidotimod can be used to treat acute respiratory tract infections (RTIs) and its pharmacokinetic studies has shown its ability to boost the immunoresponse and favouring the increase in the level of immunoglobulins (IgA, IgM, IgG) and T-lymphocytes (CD3+, CD4+). Pidotimod also exhibits anti-inflammatory properties by inhibiting the production of pro-inflammatory molecules such as IL-6 and TNF-α, which are linked to autoimmune diseases.</p>

<p>Inhibitor of PDE4 enzyme</p>

<p>Amoxapine is a dibenzoxazepine- derivative tricyclic antidepressant or TCA. It is used in the treatment of depressive disorders and psychotic depression. Amoxapine is a potent serotonin and norepinephrine reuptake inhibitor. It works on the central nervous system to increase levels of the chemicals in the brain.</p>