Featured
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Article |
Structural basis of GABA reuptake inhibition
Structural determination of GAT1 using cryo-electron microscopy provides insights into the biology and pharmacology of this GABA transporter.
- Zenia Motiwala
- , Nanda Gowtham Aduri
- & Cornelius Gati
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Letter |
Vaccine-driven pharmacodynamic dissection and mitigation of fenethylline psychoactivity
A vaccine-driven approach shows that the prominent stimulant features of the psychoactive profile of fenethylline can be attributed to amphetamine, with synergistic support from theophylline, and no direct contributions from the parent drug molecule.
- Cody J. Wenthur
- , Bin Zhou
- & Kim D. Janda
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Letter |
The allosteric inhibitor ABL001 enables dual targeting of BCR–ABL1
The selective allosteric ABL1 inhibitor ABL001 (asciminib) represents a new inhibitory mechanism for BCR–ABL1-driven malignancies, and its efficacy and evolving mechanisms of resistance do not overlap with those of other BCR–ABL1 kinase inhibitors.
- Andrew A. Wylie
- , Joseph Schoepfer
- & William R. Sellers
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Research Highlights |
Molecule blocks sperm production
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Research Highlights |
Antidepressants' cellular target
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News |
A wake-up call for dormant genes
Anti-cancer drug holds potential as a treatment for genetic-imprinting disorder.
- Rebecca Hill
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Letter |
Digoxin and its derivatives suppress TH17 cell differentiation by antagonizing RORγt activity
- Jun R. Huh
- , Monica W. L. Leung
- & Dan R. Littman
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Letter |
DHODH modulates transcriptional elongation in the neural crest and melanoma
In a zebrafish model of melanoma driven by activated BRAF, this study finds expression of a gene signature indicative of disrupted terminal differentiation of neural crest progenitors. A chemical screen led to the identification of leflunomide as an inhibitor of neural crest stem cells. Leflunomide inhibits dihydroorotate dehydrogenase and thereby transcriptional elongation, including genes involved in neural crest development and melanoma growth. Leflunomide has anti-melanoma activity in the zebrafish model and human melanoma xenografts, and might prove useful as an anticancer drug.
- Richard Mark White
- , Jennifer Cech
- & Leonard I. Zon
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News & Views |
Closing in on an oral treatment
At present, only injectable drugs are available for treating multiple sclerosis. So clinical trials indicating that the drug fingolimod might be a step towards an oral treatment for the disease are exciting indeed.
- Roland Martin
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News |
Health benefits of red-wine chemical unclear
Sceptics continue to ask whether resveratrol really can delay the effects of ageing.
- Lizzie Buchen
