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  • The Promise of Epigenetics in Early Stage Drug Discovery
    Epigenetic targets are exciting to drug discovery scientists because they hold great potential across a wide spectrum of therapeutic areas. The field of epigenetics focuses on the investigation of enzymes that alter gene expression through modification of their target substrates, usually through the addition or removal of methyl or acetyl groups. High-throughput assays to identify agents capable of modifying the action of such enzyme targets has, in the past, proven to be challenging due to the relatively small molecular alterations in addition to the possibility of sequential modifications, leading to multiple end products. As such, high-throughput bioassays that allow the direct, concurrent quantification of multiple modification states are attractive. The RapidFire platform enables high-throughput mass spectrometric analysis of native molecules from in vitro reactions by performing on-line desalting in seconds, as opposed to HPLC, which requires minutes. Moreover, the RapidFire system can be connected to any mass spectrometer providing unparalleled versatility in reaction detection.
  • Integrated Quant / Qual for In-vivo Discovery Bioanalysis using Hybrid Quadrupole-Time-of-Flight Mass Spectrometry
    Ultra high performance liquid chromatography (UHPLC) coupled with orthogonal acceleration hybrid quadrupole-time-of-flight (QqTOF) mass spectrometry is an emerging technique offering new strategies for the efficient screening of new chemical entities (NCE) and related molecules at the early discovery stage within the pharmaceutical industry.
  • Drug Delivery: enabling technology for discovery and development
    The integration of pharmacodynamic and pharmacokinetic parameters in non clinical pharmacology studies is a key aspect in drug discovery for efficacy and safety assessment, in the particular for the translation from the non clinical to the clinical field. Modeling the profile of plasma exposure achieved with the intended therapeutic route often requires the use of intravenous infusion. In addition, in most cases infusion parameters (infusion rate, volume, duration and sequences) need to be customized to achieve the appropriate pattern of plasma drug exposure. When pharmacodynamic parameters are recorded by telemetry, the use of implantable pumps rather than external pumps is necessary to preserve the improvement in physiological data recording offered by telemetry.
  • Part 2: How has HR-MS technology fundamentally changed the way we study drug biotransformation and disposition?
    AB SCIEX is proud to present the 2nd installment of a Global 4-Part Live Webinar Series exploring novel and dynamic workflows for Metabolite Identification & Drug Metabolism solutions as it pertains to the 4 main stages of the drug discovery and development paradigm, Lead Discovery, Late Stage Discovery, Early Development and Late Stage Development. Part 2 of this webinar series will focus on how HRMS technology has fundamentally changed the way metabolite biotransformations are investigated in Lead Discovery.
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  • Fungal Immunomodulatory Proteins: Characteristic, Potential Anti-Tumor Activities and Their Molecular Mechanisms
    We comment on the source and diversity of FIPs. • We provide a comparative analysis of structural and physicochemical properties of these proteins. • Antitumor effects of FIPs are discussed. • Molecular mechanisms involved in the antitumor activity of FIPs were analyzed. • FIPs offer enormous growth potential as future immunotherapeutics.
  • Cannabinoid receptors as therapeutic targets for autoimmune diseases – where do we stand?
    CB1 and CB2 receptors are essential for innate and adaptive immune responses. • The ECS and associated receptors are involved in autoimmune diseases. • CB2R agonists have emerged as new strategies for autoimmunity diseases. • ?9-THC and CBD showed immunosuppressive activity.
  • Optimizing Intracellular Signaling Domains for CAR NK Cells in HIV Immunotherapy: a Comprehensive Review
    • NK cells are key effectors of antiviral responses that become dysregulated during HIV infection. • CAR strategies can redirect T cell and NK cell functions towards HIV-infected cells. • CAR T cell strategies applied in NK cells are sub-optimal due to differences in signal transduction. • Understanding these differences in NK and T cell signaling may enhance NK-specific CAR design. • NK and T cell signal transduction are summarized and novel NK-specific CAR strategies are discussed.
  • Synthetic biology – reimagine drug discovery
    Synthetic biology is a term used to describe an approach by which novel artificial biological pathways, organisms or devices are designed and constructed. Bringing together skills from biology, chemistry, bioinformatics and engineering, it applies engineering-like techniques, at scale, to solve biological problems through a rational process of ‘biodesign’.
  • Therapy for Glioblastoma – is it working?
    As of July 2018, there were 759 ongoing or projected clinical trials for glioblastoma. • Drug therapies appear compromised by the need to combat tumour heterogeneity. • Immunotherapy approaches targeting multiple tumour antigens are showing promise in the clinic. • Improved understanding of glioblastoma tumour biology is paving the way for better drugs and integrated treatment strategies.
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