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Showing 1–7 of 7 results
Advanced filters: Author: Adrian Whitty Clear advanced filters
  • Macrocycles have the potential to act on currently undruggable targets, but their discovery thus far has been unsystematic. A physicochemical analysis of all nonredundant co-crystal structures now sets out guidelines for macrocycle development.

    • Elizabeth A Villar
    • Dmitri Beglov
    • Adrian Whitty
    Research
    Nature Chemical Biology
    Volume: 10, P: 723-731
  • Compounds that exhibit a covalent mechanism of action are typically avoided in drug discovery programmes, largely owing to safety concerns. Here, Singh and colleagues present the pharmacological advantages offered by covalent drugs and discuss strategies to address the potential risks and challenges that have been associated with these agents.

    • Juswinder Singh
    • Russell C. Petter
    • Adrian Whitty
    Reviews
    Nature Reviews Drug Discovery
    Volume: 10, P: 307-317
  • Cooperative binding effects pervade biology. Only a few basic principles are at play, but in different biological contexts cooperativity appears in distinct guises to achieve different ends. Here I discuss some of the manifestations of cooperativity that are most important in biology and drug discovery as they pertain to systems at different levels of complexity and also highlight aspects of this broadly important phenomenon that remain poorly understood.

    • Adrian Whitty
    Comments & Opinion
    Nature Chemical Biology
    Volume: 4, P: 435-439
  • Developing small-molecule inhibitors against protein-protein interaction targets is among the most difficult challenges in contemporary drug discovery. Recent developments in our understanding of this problem, and in the knowledge and tools available to address it, give cause for renewed hope, but substantial challenges remain.

    • Adrian Whitty
    • Gnanasambandam Kumaravel
    Comments & Opinion
    Nature Chemical Biology
    Volume: 2, P: 112-118