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Chronological Index of : Targets & Mechanisms

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  • Covalent hits on KRAS

    UCSF- and Harvard Medical School-led teams have independently synthesized the first covalent inhibitors of a common oncogenic form of KRAS. Araxes has licensed the UCSF team's findings and has partnered with Johnson & …

    Published on 1/9/2014
  • The next battle line against melanoma

    Boston and Los Angeles researchers have reported mechanisms of resistance to BRAF and MEK inhibitors in melanoma. The work points to targets downstream of BRAF that could lead to combination therapies to forestall …

    Published on 1/9/2014
  • Balancing act in liver fibrosis

    U.S. researchers have shown that CXCR7 and CXCR4 play proregenerative and profibrotic roles following liver injury, making the proteins therapeutic targets to prevent or treat liver fibrosis.

    Published on 12/19/2013
  • Lipid kinase enters the malaria stage

    A Novartis-UCSD-led consortium has identified a new class of antimalarials that, unlike marketed drugs, eliminates Plasmodium at all stages of its infection cycle. The pharma is developing derivatives of the lead …

    Published on 12/19/2013
  • ClpPing persistence

    Northeastern University researchers have combined traditional antibiotics with compounds that activate bacterial clpP protease and cured mice with severe, highly drug-resistant Staphylococcus biofilm infections. Arietis…

    Published on 12/12/2013
  • Figure 1: The commensal bacteria-butyrate-Treg cell axis of inflammatory regulation in the gut

    Targets & Mechanisms: A gut feeling about butyrate Figure 1. The commensal bacteria-butyrate-Treg cell axis of inflammatory regulation in the gut. Certain commensal bacteria abundantly produce butyrate through …

    Published on 12/5/2013
  • A gut feeling about butyrate

    Inflammatory conditions of the gut have long been associated with imbalances in mucosal levels of microflora-produced short-chain fatty acids, but the underlying mechanisms were unknown. Two separate groups in the U.S. …

    Published on 12/5/2013
  • Getting to the root of periodontitis

    Current therapies do not target the underlying immune response that drives periodontitis. Looking to change that, a team from the U.S. and Brazil has shown that microparticles loaded with CCL22 recruited Treg cells to …

    Published on 11/21/2013
  • Riding the integrin wave in thrombosis

    The use of platelet integrin alpha(2b)beta(3) inhibitors in thrombosis, although clinically effective, has been limited by an associated high risk of bleeding. Now, researchers at the University of Illinois at Chicago …

    Published on 11/21/2013
  • Figure 1: Selective inhibition of integrin alpha(2b)beta(3) in thrombosis

    Targets & Mechanisms: Riding the integrin wave in thrombosis Figure 1. Selective inhibition of integrin a2bb3 in thrombosis. Findings published in Nature reveal two waves in integrin a2bb3 (GPIIb/IIIa; CD41/CD61) …

    Published on 11/21/2013
  • Table 1: RSV pipeline

    Targets & Mechanisms: RSVing for site zero Table 1. RSV pipeline. Only one product is marketed to prevent serious lower respiratory tract disease caused by respiratory syncytial virus (RSV). At least 12 other …

    Published on 11/14/2013
  • BETting on Th17 cells

    Constellation Pharmaceuticals has established a connection between BET bromodomain proteins and pathogenic T helper type 17 cells. The findings hint at potential therapeutic opportunities for this epigenetic target …

    Published on 11/14/2013
  • RSVing for site zero

    An NIH team has used structure-based design to generate an RSV vaccine that showed strong neutralizing activity in both mice and macaques. The next step is picking a candidate to advance into GMP production and clinical…

    Published on 11/14/2013
  • Pulse my heart

    VEGF-A to repair post-myocardial infarction heart damage has stumbled in the clinic because of delivery issues. Now, a multinational team thinks it has solved the delivery problem by using synthetic RNA. The molecule is…

    Published on 11/7/2013
  • Figure 1: VEGF-A promotes an endothelial cell fate in human cardiac progenitor cells

    Targets & Mechanisms: Pulse my heart Figure 1. VEGF-A promotes an endothelial cell fate in human cardiac progenitor cells. Lui et al. identified VEGF-A as a paracrine factor that promotes endothelial cell …

    Published on 11/7/2013
  • Benztropine for MS

    Although candidate compounds to treat secondary progressive multiple sclerosis abound, few lead to neuronal remyelination. A new study has suggested that an existing Parkinson's disease drug-benztropine-or a derivative …

    Published on 10/31/2013
  • KCC2 escape from neuropathic pain

    Researchers from Laval University have described an activator of the co-transporter KCC2 and shown its analgesic effect in mice. The group is developing next-generation compounds with better pharmacological properties.

    Published on 10/31/2013
  • Personal factors

    A multi-institute team collaborating with the FDA has determined why patients with a form of severe hemophilia rarely develop neutralizing antibodies against factor VIII replacement therapy. The group is developing an …

    Published on 10/31/2013
  • HER2's outside help

    An international team has found that neurokinin 1 substance P receptor, a known player in nausea, pain and inflammation, enhances HER2 signaling in breast cancer. The findings argue for combining antagonists against …

    Published on 10/17/2013
  • sFGFR for achondroplasia

    French researchers have designed a decoy version of fibroblast growth factor receptor 3 that increased bone length and decreased achondroplasia-associated complications in mice compared with vehicle. The molecule has a …

    Published on 10/17/2013
  • KIM-1 driving chronic kidney disease

    Harvard researchers have shown that KIM-1, a protein that helps overcome acute kidney injury, can also trigger chronic kidney disease. Companies modulating the target need to scrutinize the therapeutic window of their …

    Published on 10/10/2013
  • Alternative strategies in ALS

    Biogen Idec and Evotec are pursuing distinct strategies to find new therapies for ALS. Biogen Idec is forming partnerships to understand the basic biology, whereas Evotec is partnering for a phenotypic screening …

    Published on 10/3/2013
  • Hedgehog battles Down syndrome

    Researchers at Johns Hopkins have shown that a hedgehog pathway activator could help improve brain development, learning and memory in patients with Down syndrome. The team is trying to narrow the therapeutic window to …

    Published on 9/26/2013
  • Two respiratory viruses, one antibody

    Humabs and the Institute for Research in Biomedicine have identified an antibody that could be used to prevent as well as treat RSV, thus providing an advantage over the prophylactic Synagis. The mAb also could be …

    Published on 9/26/2013
  • Figure 1: A dual role for nociceptors

    Targets & Mechanisms: Bacteria's painful truth Figure 1. A dual role for nociceptors. Bacteria release factors, such as N-formyl-methionyl-isoleucyl-phenylalanine-leucine (FMIFL) and a-hemolysin (aHL), that directly …

    Published on 9/19/2013

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