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Researchers from UCSF San Francisco have discovered an injection with a chemical to improve the memory of mice to study the respond of cells to biological stress. The chemicals injected were screened for their potential to perturb a protective biochemical pathway within cells that is activated when cells are unable to keep up with the need to fold proteins into their working forms. The chemical acts within the cell beyond the biochemical pathway that activates this folded protein response, though. It broadly impacts the integrated stress response. In this response, several biochemical pathways converge on a single molecular lynchpin is a protein called elF2 alpha. The inactivation of eIF2 alpha is a brake on memory consolidation (Ref: Brithvi V, ISRIB: a new chemical entity targets elF2 alpha for memory boosting, Drug discovery, 2013, 5(13), 3), (Image: loyalkng.com).



DRUG DISCOVERY OF THE MONTH

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ISRIB: a new chemical entity targets elF2 alpha for memory boosting

Brithvi V

Researchers from UCSF San Francisco have discovered an injection with a chemical to improve the memory of mice to study the respond of cells to biological stress.

Drug Discovery, 2013, 5(13), 3

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FDA APPROVED DRUGS

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FDA approved drugs - May 2013

Brithvi V

Liptruzet (ezetimibe and atorvastatin) treats two sources of cholesterol by inhibiting both the absorption of cholesterol in the digestive tract - through ezetimibe - and the production of cholesterol in the liver - through atorvastatin.

Drug Discovery, 2013, 5(13), 4-7

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DRUG DISCOVERY OF THE MONTH

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Diacylglycerol kinase alpha: A promising target for Glioblastoma

Brithvi V

Diacylglycerol kinase alpha is an enzyme in humans is encoded by the DGKA gene. The protein encoded by this gene belongs to the eukaryotic diacylglycerol kinase family. It acts as a modulator that competes with protein kinase C for the second messenger diacylglycerol in intracellular signaling pathways.

Drug Discovery, 2013, 5(14), 10

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FDA APPROVED DRUGS

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FDA approved drugs – June 2013

Brithvi V

Revlimid (lenalidomide), a thalidomide analogue, is an immunomodulatory agent specifically indicated for the treatment of patients with mantle cell lymphoma (MCL) whose disease has relapsed or progressed after two prior therapies, one of which included bortezomib.

Drug Discovery, 2013, 5(14), 11-12

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RESEARCH

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Subtractive genomics approach for identification of drug targets against Chlamydophila pneumonia J138

Kumaraswamy Naidu C, Trinath D, Suneetha Y

Pneumonia is an inflammatory condition affecting the lung alveoli. Approximately 450 million people around the world were infected with pneumonia with an estimated mortality of 4 million. Chlamydophila pneumoniae is an obligate intracellular bacterium that infects humans and is a major cause of pneumonia.

Drug Discovery, 2013, 5(14), 13-15

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DRUG DISCOVERY OF THE MONTH

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Halogen bonds: novel tools for drug discovery

Brithvi V

Halogen bonding is the non-covalent interaction that occurs between a halogen atom (Lewis acid) and a Lewis base. The first reported use of halogen bonding in liquid crystal formation was by H. Loc Nguyen. On the bio-molecular level, halogen bonding is important for substrate specificity, binding and molecular folding. Depending on the structural and chemical environment, halogen bonding interactions can be weak or strong. For molecular recognition and binding, halogen bonding can be significant. A halogen bond in Biomolecules can be defined as a short C X···O Y interaction (C X is a carbon-bonded chlorine, bromine, or iodine, and O Y is a carbonyl, hydroxyl, charged carboxylate, or phosphate group), where the X···O distance is less than or equal to the sums of the respective van der Waals radii (3.27 Å for Cl···O, 3.37Å for Br···O, and 3.50 Å for I···O) and can conform to the geometry seen in small molecules, with the C X···O angle ≈165° (consistent with a strong directional polarization of the halogen) and the X···O Y angle ≈120°. The concept of the halogen bond (or Xbond) has become recognized as contributing significantly to the specificity in recognition of a large class of halogenated compounds.

Drug Discovery, 2013, 5(15), 19

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FDA APPROVED DRUGS

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FDA approved drugs – July 2013

Brithvi V

Zubsolv is a sublingual tablet formulation of buprenorphine, an opioid analgesic, and naloxone, an opioid antagonist. It was designed to counteract the high effect that may arise following the intravenous injection of a disolved tablet. Combining buprenorphine and naloxone in a single tablet reduces the risk of intravenous abuse. It is specifically indicated for the maintenance treatment of opioid dependence and should be used as part of a complete treatment plan to include counseling and psychosocial support. It is supplied as a tablet for sublingual administration. The recommended target dosage of Zubsolv sublingual tablet is 11.4 mg/2.8 mg buprenorphine/naloxone/day (two 5.7/1.4 mg tablets) as a single daily dose. The dosage of Zubsolv should be progressively adjusted in increments/decrements of 1.4 mg/0.36 mg or 2.8 mg/0.72 mg buprenorphine/naloxone to a level that holds the patient in treatment and suppresses opioid withdrawal signs and symptoms.

Drug Discovery, 2013, 5(15), 20-22

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RESEARCH

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Anti-inflammatory effect of a methanolic extract of leaves of Ocimum Sanctum

Basak P, Mallick P, Mazumder S, Verma AS

Aim of study: The aim of this study was to establish the anti-inflammatory activity of the methanolic extract of Ocimum sanctum leaves (MEOS) with its fractions and to delineate the possible mechanism of action for MEOS. Materials and methods: The anti-inflammatory activities of MEOS along with its petroleum ether and chloroform fractions were evaluated in a Carrageenan induced model of acute inflammation. The effect of MEOS on lipopolysaccharide induced production of nitric oxide (NO) in macrophages was also studied. Results: MEOS (100, 200 and 400 mg/kg body weight) significantly reduced Carrageenan induced paw edema; chloroform fraction was most potent (66%, p < 0.001). MEOS was non-toxic up to 125microgm/ml in mouse peritoneal macrophages wherein it (0–100microgm/ml) reduced lipopolysaccharide induced NO production. Conclusion: MEOS possesses significant anti-inflammatory activity. Chloroform fraction of MEOS showed best anti-inflammatory activity.

Drug Discovery, 2013, 5(15), 23-26

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