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Abstract：
BACKGROUND: The role played by phosphoprotein phosphatases (PPP) enzymes makes them of interest as therapeutic targets to treat pathologies including neurodegenerative diseases, cancer and autoimmune diseases, but also liable to cause severe side effects. This fact has hindered the study of PPP ligands as potential drugs. Fortunately, recent advances in the comprehension of PPP biochemistry have given rise to the development of refined pharmacological strategies to selectively target phosphatases and limit the possible generation of adverse reactions.
METHODS: This review summarizes the most relevant patents claiming the use of PPP ligands to treat human diseases in the last decade (2005-2015). It also includes some pharmacological strategies aiming to indirectly modulate PPP functionality by interacting with PPP-regulating enzymes.
CONCLUSIONS: There is still much work to be done to validate PPP enzymes as eligible targets for the development of new drugs. The most significant barrier is likely to be persuading the majority of the scientific community that PPP enzymes are not too unspecific. Few patents disclosed the rational design of direct PPP ligands, while many inventions relied on long chain peptides-based approaches. Overall, the future of ligands for PPP enzymes as therapeutics seems both challenging and exciting.
METHODS: This review summarizes the most relevant patents claiming the use of PPP ligands to treat human diseases in the last decade (2005-2015). It also includes some pharmacological strategies aiming to indirectly modulate PPP functionality by interacting with PPP-regulating enzymes.
CONCLUSIONS: There is still much work to be done to validate PPP enzymes as eligible targets for the development of new drugs. The most significant barrier is likely to be persuading the majority of the scientific community that PPP enzymes are not too unspecific. Few patents disclosed the rational design of direct PPP ligands, while many inventions relied on long chain peptides-based approaches. Overall, the future of ligands for PPP enzymes as therapeutics seems both challenging and exciting.
摘要：
背景：磷蛋白磷酸酶（PPP）酶的作用使它们成为治疗包括神经退行性疾病在内的病理的治疗靶标，癌症和自身免疫性疾病，但也容易引起严重的副作用。这一事实阻碍了PPP配体作为潜在药物的研究。幸运的是,对PPP生物化学的理解的最新进展引起了精细药理学策略的发展，以选择性地靶向磷酸酶并限制不良反应的可能产生。
方法：这篇综述总结了过去十年（2005-2015年）中使用PPP配体治疗人类疾病的最相关专利。它还包括一些旨在通过与PPP调节酶相互作用间接调节PPP功能的药理学策略。
结论：要验证PPP酶作为新药开发的合格靶标，还有很多工作要做。最重要的障碍可能是说服大多数科学界认为PPP酶不是太缺乏特异性。很少有专利公开了直接PPP配体的合理设计，而许多发明依赖于基于长链肽的方法。总的来说,PPP酶的配体作为治疗剂的未来似乎既具有挑战性又令人兴奋.
方法：这篇综述总结了过去十年（2005-2015年）中使用PPP配体治疗人类疾病的最相关专利。它还包括一些旨在通过与PPP调节酶相互作用间接调节PPP功能的药理学策略。
结论：要验证PPP酶作为新药开发的合格靶标，还有很多工作要做。最重要的障碍可能是说服大多数科学界认为PPP酶不是太缺乏特异性。很少有专利公开了直接PPP配体的合理设计，而许多发明依赖于基于长链肽的方法。总的来说,PPP酶的配体作为治疗剂的未来似乎既具有挑战性又令人兴奋.
