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Drug targets
For the past decade, the number of molecular targets for approved drugs has been debated. A chemical with a certain reactivity or binding property is used as a drug because of its clinical effects. A clinically relevant 'target' might consist not only of a single biochemical entity, but the simultaneous interference of a number of receptors (pathways, enzymes and so on). Only this will give a net clinical effect that might be considered beneficial. Reflections on molecular targets are very important because drugs are molecules, but it is important not to be too simplistic. A target derived from the net effect rather than the direct chemical interaction will require input from systems biology, a nascent research field that promises to significantly affect the drug discovery process. Target is primarily dependent on the amount of knowledge available about the target and its interactions with a drug. If the target structure has already been determined, it could still be that the molecular effect of the drug cannot be fully described by the interactions with one target protein alone. An effective drug target comprises a biochemical system rather than a single molecule. Drug Targets focuses on the biochemical and molecular aspects of the signaling mechanisms which are known targets for important classes of clinically useful drugs. Drug targets are large molecules – macromolecules generally much smaller than their targets it interacts with their targets by binding to binding sites. The Binding sites are typically hydrophobic pockets on the surface of macromolecules. Binding interactions typically involve intermolecular bonds. Functional groups on the drug are involved in binding interactions and are called binding groups. Specific regions within the binding site are involved in binding interactions are called binding regions. Most drugs are in equilibrium between being bound and unbound to their target. The idea behind molecular targeting is to design drugs that specifically attack the molecular pathways that cause disease, without disrupting the normal functions in our cells and tissues. Drugs developed using this approach can be less toxic and more effective than current medicines. A molecular target is chosen which is believed to influence a particular disease when affected by a drug. The greater the selectivity can be achieved the less chance of side effects. Most of the drugs work by binding to the target receptor site; they can either block the physiological function of the protein, or mimics its effect. The discovery and exploitation of new drug targets is a key focus for both the pharmaceutical industry and academic biomedical research. Understanding the identity of drug targets that are encoded by the human genome is of great importance for the development of new pharmaceutical products and the allocation of resources within academic and industrial biomedical research. Currently marketed drugs mediate their effects through only a small number of the potential human target proteins. The initial curation of the data set involved the identification of drugs without known protein targets, such as drugs that act directly on DNA, dietary supplements and drugs that do not have known protein targets. Drug target is a key molecule involved in a particular metabolic or signaling pathway that is specific to a disease condition or pathology or to the infectivity or survival of a microbial pathogen. Some approaches attempt to inhibit the functioning of the pathway in the diseased state by causing a key molecule to stop functioning. Drugs may be designed that bind to the active region and inhibit this key molecule.

DRUG DISCOVERY OF THE MONTH

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Horizant (Gabapentin Enacarbil) for postherpetic Neuralgia

Brithvi V

Horizant (gabapentin enacarbil) is an extended-release formulation of gabapentin enacarbil, a prodrug of gabapentin. Horizant is specifically indicated for the management of postherpetic neuralgia (PHN) in adults

Drug Discovery, 2012, 2(4), 3-4

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FDA APPROVED DRUGS

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FDA approved drugs - August 2012

Brithvi V

Lucentis (ranibizumab) is a therapeutic antibody fragment designed to inhibit vascular endothelial growth factor A (VEGF-A), a protein that plays a critical role in ocular angiogenesis. Blocking VEGF-A can decrease abnormal new blood vessel formation and the resultant leaking of serum into the retina.

Drug Discovery, 2012, 2(4), 5-7

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RESEARCH

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Evaluation of Antidepressant activity of Bacopa monnieri in rat: A study in Animal Model of Depression

Somoday Hazra, Ritabrata Banerjee, Biplab K. Das, Anup K. Ghosh, Tarit K. Banerjee, Uday S. Hazra, Susanta K. Biswas, Amal C. Mondal

Major depression is a common and potentially life threatening condition. Stress induced helplessness in rodents constitutes a well-defined model to investigate physiological attributes of depression.

Drug Discovery, 2012, 2(4), 8-13

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DRUG DISCOVERY OF THE MONTH

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Current panorama on Camptothecin in Cancer treatment

Balasubramanian J

This paper is a review on Camptothecin and its solubility, QSAR; release effects while combining with various polymers, DNA damage, Programmed cell death and MMR effect in cells. Camptothecin (CPT) is an effective chemotherapeutic agent for treatment of patients with cancer.

Drug Discovery, 2012, 2(5), 16-18

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FDA APPROVED DRUGS

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FDA approved drugs - September 2012

Brithvi V

Stivarga (regorafenib) is a small molecule inhibitor of multiple membrane-bound and intracellular kinases involved in normal cellular functions and in pathologic processes such as oncogenesis, tumor angiogenesis, and maintenance of the tumor microenvironment

Drug Discovery, 2012, 2(5), 19-20

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PERSPECTIVES

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A Pharmacological Characterization of Adenosine Receptors

Nouh MH. Aljarari, Dhastagir Sultan Sheriff

Adenosine receptors (AR) are member of the G-protein Coupled Receptors (GPCR) superfamily, with four subtypes currently recognised, A1, A2A, A2B and A3 receptors. Because of various potential physiological implications of stimulating AR, the main purpose of the present review was to briefly describe the pharmacological properties of these receptors and how they could be activated

Drug Discovery, 2012, 2(5), 21-27

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DRUG DISCOVERY OF THE MONTH

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Resealed Erythrocytes: A Novel drug Carrier in drug

Balasubramanian J, Narayanan N, Vijayakumar

Resealed erythrocyte has got several advantages over the other drug delivery system which makes it superior than other systems. Resealed erythrocytes, as a drug delivery system has excellent capacity to enhance the therapeutic index and patient compliance.

Drug Discovery, 2012, 2(6), 30-32

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FDA APPROVED DRUGS

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FDA approved drugs - October 2012

Brithvi V

Synribo (omacetaxine mepesuccinate) is a cephalotaxine ester. It is specifically approved for the treatment of adults with chronic or accelerated phase chronic myeloid leukemia with resistance and/or intolerance to two or more tyrosine kinase inhibitors

Drug Discovery, 2012, 2(6), 33-35

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RESEARCH

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Larvicidal activity of various solvent extracts of Lichen Roccella Montagnei against Filarial Vector Culex Quinquefasciatus

Balaji P, Sakthivadivel M, Bharath P, Hariharan GN

Polarity based different solvent extracts (at four different conc.) of lichen, Roccella montagnei Bél. emend. Awas. (Roccellaceae) were screened for mosquito larvicidal activity against the 3rd instar larvae of the filarial vector, Culex quinquefasciatus Say (Diptera: Culicidae).

Drug Discovery, 2012, 2(6), 36-39

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