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Chronological Index of : Targets & Mechanisms

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  • Targets & Mechanisms: Unearthing antibiotics

    New antimicrobial peptides from soil bacteria

    Two new techniques for exploiting soil bacteria to find antibiotics have uncovered compound classes and targets that could impact the field even more than the pair of antimicrobials discovered.

    Published on 1/22/2015
  • Pseudo-allergy exposed

    One receptor could help screen out allergy-inducing compounds during discovery

    A single receptor found to mediate allergic drug reactions could lead to an antidote and allow compounds to be screened out early during drug discovery.

    Published on 1/22/2015
  • Figure: The THIQ IQ

    Pseudo-allergy exposed Targets & Mechanisms The THIQ IQ Structures of the classic basic secretagogue 48/80, its cyclized monomer and representative members of neuromuscular blocking or anti-microbial drugs that …

    Published on 1/22/2015
  • Box: Dirt Silk Road

    Unearthing antibiotics Targets & Mechanisms Dirt silk road Historically, soil-based bacteria were routinely mined for antibiotics, but the practice has lost ground to synthetic approaches involving structure-based …

    Published on 1/22/2015
  • Resurrecting a magic bullet

    Heidelberg Pharma has resuscitated a long-dead ADC toxin with updated conjugation techniques, and its partner Roche has thrown the company a lifeline that could help validate the platform.

    Published on 12/18/2014
  • Lysin in wait

    Micreos and ContraFect are separately developing phage lysins, which are not prone to bacterial resistance, as complements to antibiotics.

    Published on 12/11/2014
  • PIEZO de resistance

    A Duke team has found a new role for PIEZO calcium channels in cartilage damage, suggesting channel inhibitors could be developed for joint injury or osteoarthritis.

    Published on 12/11/2014
  • Terazosin reborn

    Chinese researchers have found that the generic alpha-blocker terazosin prevents apoptosis and want to pursue it for stroke, but they will need to navigate a landscape of difficult preclinical models.

    Published on 12/11/2014
  • Greasing insulin

    The once discarded target GPR120 has led to the discovery of an entirely new class of fatty acids that could restore insulin sensitivity in patients with diabetes.

    Published on 11/6/2014
  • Branching out in pancreatic cancer

    Changes in circulating levels of branched-chain amino acids detectable 2-5 years before the onset of pancreatic cancer could lead to diagnostic markers for the indication.

    Published on 10/23/2014
  • Alnylam interrupts preeclampsia

    Alnylam has generated an siRNA conjugate that blocks angiotensin-induced hypertension without causing fetal toxicity in a rat model of preeclampsia.

    Published on 10/16/2014
  • BetaLogics' in vitro beta cells

    BetaLogics and University of British Columbia researchers have developed an in vitro protocol to generate mature insulin-producing beta-like cells from human pluripotent stem cells - a major milestone in the development…

    Published on 10/9/2014
  • MIDAS touch vaccine

    A vaccine against the fibrinogen-binding MIDAS domain in the ebpA protein of Enterococcus faecalis could provide a solution to the widespread problem of catheter-associated urinary tract infections.

    Published on 10/9/2014
  • Ral-lying around Ras

    A University of Colorado-led team has demonstrated anticancer efficacy for new small molecule inhibitors of Ral proteins - a family of Ras-like GTPases often overlooked in favor of their Ras cousins.

    Published on 10/9/2014
  • ALK7's obese functions

    Researchers have shown that inhibiting ALK7 can increase energy expenditure in fat cells and suggest the protein could be a target for obesity. Acceleron Pharma has licensed the findings and is pursuing a discovery …

    Published on 9/25/2014
  • A chromatin target for ALL

    An NYU School of Medicine-GSK collaboration has shown that an inhibitor of the chromatin regulator JMJD3 could help treat T cell acute lymphoblastic leukemia and might avoid the safety pitfalls of other notch 1-targeted…

    Published on 9/11/2014
  • Destabilizing data in CF

    In vitro data from two academic labs show combinations of Kalydeco ivacaftor and lumacaftor destabilize the CFTR channel. Although the new findings are at odds with Vertex's positive clinical results, they are prompting…

    Published on 9/4/2014
  • A cultured approach to ALS therapy

    The mechanisms by which dysfunctional glial cells contribute to ALS have remained poorly defined. Now, Harvard University researchers have identified a therapeutic target-prostaglandin D2 receptor subtype DP1-and shown …

    Published on 8/28/2014
  • PAX6 drives differentiation of skin epithelial stem cells to limbal stem cells

    Targets & Mechanisms: Corneal perspectives Figure 1. PAX6 drives differentiation of skin epithelial stem cells to limbal stem cells. Two new approaches that promote regenerative therapies for corneal transplants have…

    Published on 8/21/2014
  • Corneal perspectives

    Two independent findings could increase the availability of tissue for corneal transplants. A UCSD team has identified key factors needed to culture the limbal stem cells necessary for clear vision. A Harvard team has …

    Published on 8/21/2014
  • Figure 1: Controlling insulin secretion via the adipose tissue-islet connection

    Targets & Mechanisms: Adipsin meets beta cells Figure 1. Controlling insulin secretion via the adipose tissue-islet connection. Lipids derived from ingested nutrients are metabolized to fatty acids that trigger an …

    Published on 8/7/2014
  • Adipsin meets beta cells

    A Harvard-led team has shown that adipsin increases insulin secretion by generating the complement peptide C3a. Its therapeutic potential might hinge on whether the effects persist with chronic dosing without triggering…

    Published on 8/7/2014
  • Neo enough in glioma

    A peptide containing a mutation in IDH1 could join the race for a cancer vaccine for glioma. The next question is whether the vaccine can jump-start an immune response in patients.

    Published on 7/31/2014
  • Taking a BET on hedgehog

    U.S. researchers show that BET bromodomain inhibition could open up a new therapeutic strategy for hedgehog-driven cancers that fail to respond to smoothened inhibitors.

    Published on 7/31/2014
  • Selecting CDK7

    A Harvard Medical School team has found a cyclin dependent kinase 7 inhibitor that covalently binds a cysteine outside the enzyme's kinase domain and suppresses leukemia in mice. Syros Pharmaceuticals has licensed the …

    Published on 7/24/2014

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