Drug discovery and development articles within Nature

Featured

  • Article
    | Open Access

    Unimolecular integration of NMDA receptor antagonism with GLP-1 receptor agonism effectively reverses obesity, hyperglycaemia and dyslipidaemia in rodent models of metabolic disease.

    • Jonas Petersen
    • , Mette Q. Ludwig
    •  & Christoffer Clemmensen

  • Article
    | Open Access

    Accuracy of free-energy calculations can be improved by constructing an experimental benchmark for solid–solid free-energy differences, quantifying statistical errors for the computed free energies and placing both hydrate and anhydrate crystal structures on the same energy landscape.

    • Dzmitry Firaha
    • , Yifei Michelle Liu
    •  & Marcus A. Neumann

  • Article |

    A new type of transformation converting a heteroaromatic carbon atom into a nitrogen atom, turning quinolines into quinazolines to enable manipulation of molecular properties, is reported.

    • Jisoo Woo
    • , Colin Stein
    •  & Mark D. Levin

  • Article |

    A lead-optimization strategy combining porin permeation properties and biochemical potency leads to development of a new class of antibiotic based on broad inhibition of penicillin-binding proteins from Gram-negative bacteria.

    • Thomas F. Durand-Reville
    • , Alita A. Miller
    •  & Ruben A. Tommasi

  • Article |

    Modular synthesis and structural biology are used to design and characterize group A streptogramin antibiotics, one of which has activity against streptogramin-resistant strains and demonstrates efficacy in a mouse model of bacterial infection.

    • Qi Li
    • , Jenna Pellegrino
    •  & Ian B. Seiple

  • Article |

    A manganese-catalysed oxidative C(sp3)–H methylation method allows a methyl group to be selectively installed into medicinally important heterocycles, providing a way to improve pharmaceuticals and better understand the ‘magic methyl effect’.

    • Kaibo Feng
    • , Raundi E. Quevedo
    •  & M. Christina White

  • Letter |

    A system that combines nanoscale synthesis and affinity ranking enables high-throughput screening of reaction conditions and bioactivity for a given protein target, accelerating the process of drug discovery.

    • Nathan J. Gesmundo
    • , Bérengère Sauvagnat
    •  & Tim Cernak

  • Outlook |

    In 2006, pharmaceutical innovation consultant Bernard Munos helped to launch a lively public discussion about how open innovation can bring novel drugs to market with his paper 'Can opensource R&D reinvigorate drug research? He tells Nature how things have changed since then.

    • Eric Bender

  • Outlook |

    A growing appreciation that cooperation and competition can coexist is transforming the life-sciences innovation landscape. Development was once shrouded in secrecy, but now organizations are coming together.

    • David Holmes

  • Outlook |

    Open initiatives are promising, but we have much further to go if research data are to be as publicly accessible as they should be, says Aled Edwards.

    • Aled Edwards

  • Outlook |

    Drug discovery is time-consuming and full of blind alleys. Pharmaceutical rivals are cooperating in the early stages to accelerate and improve the efficiency of the process.

    • Neil Savage

  • Outlook |

    In a pioneering move, the compound JQ1 was released to the community for free. The impact that this has had on research and development is slowly coming into focus.

    • Andrew R. Scott

  • Article |

    The description of a compound (DDD107498) with antimalarial activity against multiple life-cycle stages of Plasmodium falciparum and good pharmacokinetic and safety properties, with potential for single-dose treatment, chemoprotection and prevention of transmission.

    • Beatriz Baragaña
    • , Irene Hallyburton
    •  & Ian H. Gilbert

  • Article |

    An automated approach designing drug ligands to multi-target profiles (with a 75% prediction success rate) is experimentally validated by the invention of novel ligands tailored to the complex and physiologically-relevant goal of identifying drugs that can specifically target profiles of multiple proteins.

    • Jérémy Besnard
    • , Gian Filippo Ruda
    •  & Andrew L. Hopkins

  • News & Views |

    Reagents have been developed that allow carbon—hydrogen bonds on benzene-like compounds called heterocycles to be converted directly into carbon—carbon bonds. The finding will be a boon to medicinal chemists. See Letter p.95

    • William J. Pitts

  • Outlook |

    Several new drugs for treating chronic obstructive pulmonary disease are about to hit the market, with more in the pipeline.

    • Duncan Graham-Rowe

  • Editorial |

    Legal actions and oversight are necessary to keep the drug industry in line.

  • News |

    As approvals for engineered food animals stall, pigs may be US regulators’ next challenge.

    • Amy Maxmen

  • Article |

    A large-scale computational effort is used to predict the activity of 656 drugs against 73 protein targets that have been associated with adverse drug reactions; the abdominal pain side effect of the synthetic oestrogen chlorotrianisene is shown to be mediated through its inhibition of cyclooxygenase-1.

    • Eugen Lounkine
    • , Michael J. Keiser
    •  & Laszlo Urban

  • News & Views |

    Alterations in brain blood vessels in mice precede the neural dysfunction associated with Alzheimer's disease. The finding highlights potential targets for drug development. See Letter p.512

    • Peter Carmeliet
    •  & Bart De Strooper

  • Letter |

    Although IL-2 has been studied for its immune-stimulating activity against metastatic cancer, its side effects have limited its clinical use; here, an engineered IL-2 ‘superkine’ is shown to have increased activity, particularly in inducing antitumour T cells, but fewer side effects.

    • Aron M. Levin
    • , Darren L. Bates
    •  & K. Christopher Garcia

  • News |

    First treatment to tackle protein behind the disease wins approval — but only a small fraction of patients will benefit.

    • Heidi Ledford

  • News & Views |

    Mutations in the maternal copy of the UBE3A gene cause a neurodevelopmental disorder known as Angelman syndrome. Drugs that activate the normally silenced paternal copy of this gene may be of therapeutic value. See Letter p.185

    • Arthur L. Beaudet

  • Outlook |

    The repertoire of traditional Chinese medicine could offer rich pickings for modern drug developers, but researchers must first define and test herbal concoctions.

    • Zhiguo Xu

  • News |

    Pharmaceutical industry anxiously struggles to retool as Lipitor patent expires.

    • Heidi Ledford

  • Outlook |

    The United States publishes more biomedical research papers than ever before, yet drug development is stagnating. Several new initiatives aim to turn this knowledge into new remedies.

    • Amy Maxmen

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