Designing Drug

Question: Discuss about theDesigning Drug. Answer: Introduction The disorder due to the continuous nerve action is caused due to the disturbance in the process of neurotransmission. In this essay, the action of the drug, which is designed to stop the action of the neurotransmitter release in the pre-synaptic cleft is discussed, which helps in the prevention of disorder due to the continuous nerve movement. The mechanism of endocytosis is used as to design the drug. The endocytosis is a process of active transport, where cell engulfs particles from the extracellular fluid. As it is an active form of transport, energy is required in this form of transport, and it helps in the transportation of the major polar molecules, which are not possible to pass through the hydrophobic layer of the cell membrane (Sigismund et al. 2012). On the other hand, exocytosis is another form of active transport, in which molecules are transported out of the cell to the extracellular fluid (Refer to Appendix). Both endocytosis and exocytosis form the vesicle pathway for the cell. The neurotransmitters are the chemical messengers that help in the process neurotransmission. The chemical messages are passed from one cell to another through the synaptic cleft. These neurotransmitters are small or large-sized proteins that are passed through the endoplasmic reticulum. If the KEDL sequence of peptide is present within the ER, it prevents the protein from leaving the ER. Neve rtheless, if the concentration of the soluble protein within the ER is high, the process of vesicle pathway is carried out and the proteins are transported to the Golgi complex. The soluble proteins are bounded to the KEDL receptor and are transported to Golgi body. From the Golgi body, the protein enters the lysosome and thereby reaching the stage of late endosomes. From lysosome, the particles are sent to the extracellular fluid, with the help of hydrolytic enzyme (Giannotta et al. 2012). Many drugs have the capability to inhibit the action of the neurotransmitter. These drugs are able to inhibit the function of neurotransmitter by binding on the particular target site of the, where the neurotransmitter is supposed to bind. The drug can attach directly to the binding site of the neurotransmitter, which is called the competitive binding. It can also attach to the alternative site, and it is called non-competitive binding (Silverman and Holladay 2014). The precursor enzymes of the neurotransmitter can be inhibited, when the drug binds to the active site of the enzymes. Vesicles are the medium through which, the neurotransmitter are transported. Drugs like dopamine and serotonin are the able to fill the vesicles and thereby preventing the protein from being transported using the mechanism of endocytosis. The calcium ions, which are responsible for the release of neurotransmitter, can be blocked by the release of the docked vesicules. Botulinum is the drug that is responsible for the inhibiting the action of the calcium ion by binding with the proteins present in the neuron membrane (Changingminds.org, 2016). The action of the neurotransmitter can be prevented with the help of the drugs that have the ability to prevent the process of endocytosis. The drug that is designed to prevent the continuous nerve disorder needs to have the characteristics to replicate the property of the neurotransmitter protein. Reference Changingminds.org. (2016). Drug action in neurons. [online] Available at: https://changingminds.org/explanations/brain/brain_chemistry/drug_neuron.htm [Accessed 28 Sep. 2016]. Giannotta, M., Ruggiero, C., Grossi, M., Cancino, J., Capitani, M., Pulvirenti, T., Consoli, G.M.L., Geraci, C., Fanelli, F., Luini, A. and Sallese, M., 2012. The KDEL receptor couples to Gq/11 to activate Src kinases and regulate transport through the Golgi.The EMBO journal,31(13), pp.2869-2881. Sigismund, S., Confalonieri, S., Ciliberto, A., Polo, S., Scita, G. and Di Fiore, P.P., 2012. Endocytosis and signaling: cell logistics shape the eukaryotic cell plan.Physiological reviews,92(1), pp.273-366. Silverman, R.B. and Holladay, M.W., 2014.The organic chemistry of drug design and drug action. Academic press.