Pharmacology articles within Nature Communications

Featured

• Article | 19 February 2013

  Single-cell and subcellular pharmacokinetic imaging allows insight into drug action in vivo

  Current pharmacokinetic models describe the distribution of drugs within tissues but usually lack single-cell resolution. Here Weissleder and colleagues visualize the subcellular distribution of an anticancer drug in real time in living animals and develop a model to extrapolate these findings to humans.

  • Greg M. Thurber
  • , Katy S. Yang
  •  & Ralph Weissleder

• Article | 08 January 2013

  A safe lithium mimetic for bipolar disorder

  Lithium is commonly used to treat bipolar disorder, but it exerts side effects at doses close to the therapeutic range. Singh and colleagues screen a collection of clinical compounds and find that ebselen induces lithium-like effects on mouse models of bipolar disorder by inhibiting inositol monophosphatase.

  • Nisha Singh
  • , Amy C. Halliday
  •  & Grant C. Churchill

• Article | 18 December 2012

  Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors

  Selective inhibitors of protein methyltransferases are anticancer drug candidates. Yu et al. report the structural changes that occur when selective inhibitors bind to the protein methyltransferase DOT1L.

  • Wenyu Yu
  • , Emma J. Chory
  •  & Matthieu Schapira

• Article | 13 November 2012

  Structural modelling and mutant cycle analysis predict pharmacoresponsiveness of a Na_v1.7 mutant channel

  Mutations of the Na_V1.7 voltage-gated sodium channel are implicated in abnormal pain signal transduction. Yang and colleagues perform structural modeling, mutant cycle analysis and electrophysiology on specific mutants and find that they can accurately predict their response profiles to channel blockers.

  • Yang Yang
  • , Sulayman D. Dib-Hajj
  •  & Stephen G. Waxman

• Article
  12 June 2012 | Open Access

  The translation inhibitor pateamine A prevents cachexia-induced muscle wasting in mice

  Cachexia, or muscle-wasting syndrome, is often observed in patients with cancer or sepsis, and no specific treatment of cachexia is currently available. In this study, Di Marcoet al.show that low doses of pateamine A, an inhibitor of translation initiation, prevent cachexia in a mouse model of the disease.

  • Sergio Di Marco
  • , Anne Cammas
  •  & Imed Eddine Gallouzi

• Article | 29 May 2012

  Metformin elicits anticancer effects through the sequential modulation of DICER and c-MYC

  Metformin is used to treat diabetes and its use has been associated with reduced cancer incidence, but the mechanism is unclear. In this study, metformin is shown to alter microRNA expression including an increase in mir-33a, which decreases the expression of the oncogenec-Myc.

  • Giovanni Blandino
  • , Mariacristina Valerio
  •  & Sabrina Strano

• Article
  14 February 2012 | Open Access

  PPARγ contributes to PKM2 and HK2 expression in fatty liver

  Molecular factors, regulating the expression of specific glycolytic enzymes that favour biosynthetic processes, have remained unknown. Panasyuket al. identify PPARγ as a novel transcription factor turning on pyruvate kinase M2 and hexokinase 2, which are frequently upregulated in pathophysiological growth.

  • Ganna Panasyuk
  • , Catherine Espeillac
  •  & Mario Pende

• Article | 10 January 2012

  Programmable multivalent display of receptor ligands using peptide nucleic acid nanoscaffolds

  Multivalent display of integrin antagonists enhances their efficacy, but current synthetic scaffolds used to display ligands are limited in range and precision. Englundet al. develop a new scaffold to study the multivalent effects of integrin antagonists across wide ranges of ligand number, density, and 3D arrangement.

  • Ethan A. Englund
  • , Deyun Wang
  •  & Daniel H. Appella

• Article
  16 November 2010 | Open Access

  Drug export and allosteric coupling in a multidrug transporter revealed by molecular simulations

  The drug transporter AcrB is a component of the tripartite efflux system AcrB–AcrA–TolC, which is important in multidrug-resistantEscherichia coli. Takada and co-workers used molecular simulations to further reveal the mechanism of drug export.

  • Xin-Qiu Yao
  • , Hiroo Kenzaki
  •  & Shoji Takada