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Analytical techniques

 

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Conformational Bias: A key concept for protein kinase inhibition

28 February 2012 | By Henrik Möbitz, Global Discovery Chemistry, Computer Aided Drug Design, Novartis Institutes for Biomedical Research and Doriano Fabbro, Expertise Platform Kinases, Novartis Institutes for Biomedical Research

Protein kinases act as molecular switches with remarkable plasticity and dynamics upon interaction with specific regulatory domains as well as modulators. Conformation provides a conceptual framework for understanding many aspects of kinase biology. The kinase domain has precise structural prerequisites for signal transfer and can oscillate between two major conformations:…

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Recent developments in the use of LCMS in process pharmaceutical chemistry

28 February 2012 | By Dr. Florence O. McCarthy, Department of Chemistry, Analytical and Biological Chemistry Research Facility, University College Cork

Liquid Chromatography Mass Spectrometry (LCMS) is a powerful technique that has recently undergone exponential growth in its application to pharmaceutical synthesis. This perspective will outline the general principles of LCMS, detail some recent approaches and the benefits to be derived from its use at an early stage of process development.…

Near Infrared NIR supplement 2012
Near Infrared NIR supplement 2012
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Near Infrared supplement 2012

27 February 2012 | By

In this Near Infrared supplement: Understanding external factor influences and the right use of chemometrics; Recent advances in spectroscopic measurements applied to pharmaceutical testing; Discover what vendor companies are discussing in our Near Infrared Spectroscopy Leaders Roundtable...

PAT supplement 2011
PAT supplement 2011
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PAT supplement 2011

15 December 2011 | By

In this PAT supplement: The historical development of the FDA's PAT initiative and its present course; Implementation of modelling approaches in the QbD framework: Examples from the Novartis experience; Challenges in development and implementation of spectroscopic techniques as PAT Analysers...

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Under the Microscope: Philip Irving, FOSS NIRSystems Inc.

13 December 2011 | By Philip Irving, President, FOSS NIRSystems, Inc.

FOSS NIRSystems, Inc. has a long, complicated and rich history tracing back to 1966 when NEOTEC Corporation was founded. Through a number of acquisitions and mergers, NIRSystems was trademarked in 1989 and bought by Perstorp Analytical, before the company was bought by FOSS in 1997, strengthening the company’s pharmaceutical division.…

Abbott logo
Abbott logo
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Abbott receives CE Mark for new hepatitis test

9 November 2011 | By

Abbott announced it has received CE Marking (Conformité Européenne) in the European Union to market a new, highly sensitive diagnostic test for detection of hepatitis B surface antigen (HBsAg). The test is performed on Abbott’s ARCHITECT® system. Hepatitis B is an inflammatory liver disease caused by the hepatitis B virus…

Raman supplement 2011
Raman supplement 2011
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Raman supplement 2011

24 October 2011 | By

In this Raman supplement: Solid state transformations of APIS during manufacturing by Raman analysis of pharmaceutical molecules and dosage forms; Detection, determination of chemical composition and chemical profiling of counterfeit medicines...

FIGURE 1 Schematic overview of the MALDI-MSI process as applied to imaging compound and metabolite distributions in a whole body rat sample. From one section of an animal dosed with the unlabelled compound, the substance and metabolite distributions can be acquired
FIGURE 1 Schematic overview of the MALDI-MSI process as applied to imaging compound and metabolite distributions in a whole body rat sample. From one section of an animal dosed with the unlabelled compound, the substance and metabolite distributions can be acquired
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MALDI-mass spectrometry imaging applied to drug discovery and development

19 October 2011 | By Brendan Prideaux, Dieter Staab, Gregory Morandi, Nicole Ehrhard and Markus Stoeckli, Novartis Institutes for BioMedical Research

Since its introduction in the field of biomedical imaging over 10 years ago1, matrixassisted laser desorption/ionisation mass spectrometry imaging (MALDI-MSI) has played an ever increasing role in drug discovery and development and is now utilised in laboratories of many leading pharmaceutical companies and collaborating academic institutions.

Detection of microorganisms using cellular component-based rapid method technologies
Detection of microorganisms using cellular component-based rapid method technologies
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Detection of microorganisms using optical spectroscopic-based rapid method technologies

31 August 2011 | By Michael J. Miller, President, Microbiology Consultants, LLC

This is the fourth in a series of articles on rapid microbiological methods that will appear in European Pharmaceutical Review during 2011. Previously, we discussed a number of cellular-component rapid microbiological methods (RMMs), such as ATP bioluminescence, fatty acid analysis, MALDI and SELDI time of flight mass spectrometry, Fourier transform-infrared…

Figure 1 Free energy diagram for a single step binding interaction between protein (P) and ligand (L). For a binding reaction of this type increasing affinity is achieved by lowering the free energy of the PL complex. Increasing residence (decreasing koff) time is achieved by lowering the free energy of the PL complex and/or destabilizing the transition state
Figure 1 Free energy diagram for a single step binding interaction between protein (P) and ligand (L). For a binding reaction of this type increasing affinity is achieved by lowering the free energy of the PL complex. Increasing residence (decreasing koff) time is achieved by lowering the free energy of the PL complex and/or destabilizing the transition state
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Thermodynamics and kinetics driving quality in drug discovery

31 August 2011 | By Geoff Holdgate, AstraZeneca

Recently, there has been renewed interest in using thermodynamic and kinetic data, alongside empirical rules (particularly focused upon cLogP and molecular weight) and guiding metrics such as ligand efficiency and lipophilic ligand efficiency developed for fragments, leads and drugs in order to facilitate the design of compounds with a greater…