Ligand

New Trends and Future Developments of Platinum-Based Antitumor Drugs (Oxaliplatin) Introduction: The purpose of this report is to go through the recent studies and scenarios to get an understanding of future developments of platinum-based antitumor drugs. Cisplatin was discovered in 1845 by an M Peyrone, which lead the molecule to be known as 'Peyrone 's salt '. However the authorization for cisplatin for the cures of ovarian and testicular cancer was given in 1978. Currently in cancer…

ABSTRACT N-Myristoyltransferase (NMT) is an attractive target for the development of novel antimalarial drugs. In this paper, we report a hologram quantitative structure-activity relationship (HQSAR), a comparative molecular field analysis (CoMFA), and a comparative molecular similarity indices analysis (CoMSIA) studies on a series of benzo[b]thiophene-containing selective inhibitors of plasmodial NMT. Two QSAR models were constructed, one for Plasmodium falciparum NMT and another for Homo…

Examine the forced swim test and sucrose preference test as simple tests of behavioural despair in a rodent animal model of depression, and evaluate the efficacy of nAChR agonists, antagonists, and ligand agonists as a supplement to the commonly prescribed antidepressant fluoxetine. 1.1 Rationale & specific goals The forced swim test (FST) and sucrose preference test (SPT) are commonly used behavioural experiments that are low cost, simple to implement, require no training of subjects, and can…

Kaempferol is a natural polyphenol, secondary metabolite (flavonol), a type of flavonoid, found in a variety of plant-derived foods. Kaempferol is a yellow crystalline solid with a melting point of 276–278 °C. It is slightly soluble in water and highly soluble in hot ethanol, ethers, and DMSO. Kaempferol acts as an antioxidant by reducing oxidative stress. Many studies suggest that consuming kaempferol may reduce the risk of various cancers, and it is currently under consideration as a possible…

microorganism via phagocytic receptors on the surface of the macrophage and ligands on the surface of the microorganism. When a macrophage binds to a microorganism via phagocytic receptors, there are cell surface receptors and plasma proteins that recognize the properties such as carbohydrate, lipid,or nucleic acid of the surface of the microorganism. There are also complement receptors (C3/CR4) that recognize the ligands on the microbial surface. The macrophage captures pathogens by…

INTRODUCTION Ca2+ as an intracellular second messenger is indispensable for the physiology of organisms and the molecular regulation of cells. The cytosolic free Ca2+ concentration is a crucial signal for a variety of neuronal processes including neurotransmitter release, control of membrane excitability, synaptic plasticity, and cognition. Ca2+ homeostasis in neurons is accurate controlled by several types of Ca2+ channels or the activity of Ca2+ transporters with either locate on the plasma…

Glucocorticoid are primarily used therapeutically as anti-inflammatory and immunosuppressive agent. They are secreted from the adrenal cortex of the adrenal gland in a circadian manner or in response to stress perceived by the brain. They are able to modulate physiological homeostasis and coordinate those adaptive responses to stressors. An imbalance in glucocorticoid levels, specifically chronic glucocorticoid has been associated with a number of neuropsychiatric disorders, specifically…

This means finding proteins that express affinity and specificity for the respective ligand. According to Ewald (2011) there are three good options, CitX (periplasmic binding protein from Salmonella typhimurium) and the binding domains of DpiB (sensor histidine kinase from E. coli) and CitA (sensor histidine kinase from Klebsiella pneumoniae)…

Interpretation of the NOESY: (Nuclear Overhauser Effect) spectrum of 1-(2-methyl-1,2,3,4-tetrahydroquinolin-4-yl)azepan-2-one (3a) is as follows. Strong coupling interaction of protons of 2nd and 4th position in 1-(2-methyl-1,2,3,4-tetrahydroquinolin-4-yl)azepan-2-one (3a), was not so strongly observed in COSY because it involves long range coupling i.e. protons attached between 2nd and 4th carbon atom. Hence, we studied NOESY to know the spacial interaction between these two protons. Thus, the…

Observe Ligand Protein Interaction using Gel Filtration (Phenol Red Binding to Serum Albumin) Introduction: Serum albumin is often known as blood albumin, it is the most abundant plasma protein in humans and other mammals. Serum albumin is essential for maintaining the osmotic pressure that is needed for distribution of body fluids between body tissues and intravascular compartments. It is also a carrier protein by non specifically binding several biomolecules. Ligand is a molecule can bind…