Mathuram Theodore Lemuel, Reece Lisa M, Cherian Kotturathu Mammen
Department of Stem Cell and Tissue Engineering, Frontier Mediville (A Unit of Frontier Lifeline and Dr. K. M. Cherian Heart Foundation), Affiliated to University of Madras, Chennai, Tamil Nadu, India.
Sealy Center for Vaccine Development, World Health Organization Collaborating Center for Vaccine Research, Evaluation and Training on Emerging Infectious Diseases, University of Texas Medical Branch, Galveston, TX, USA.
Drug Res (Stuttg). 2018 Aug;68(8):436-443. doi: 10.1055/s-0044-100186. Epub 2018 Jan 31.
GSK-3 inhibitors are an emerging tool for clinical interventions in human diseases and represent a niche area in combinational therapy. They possess diverse facets in applications of nervous system disorders, Type 2 diabetes, regenerative medicine and cancer. However, conflicting reports suggest the controversial role of GSK-3 inhibitors in cancers. This review aims to highlight the rise of GSK-3 inhibitors as tools for molecular-targeted research and its shift to a promising drug candidate. The review also focuses on key GSK-3 inhibitors and their roles in cancer and regenerative medicine with special emphasis to tideglusib. In addition, the decisive roles of GSK-3 in various molecular pathways will be concisely reviewed. Finally, this review concludes the emergence of GSK-3 inhibitors as a 'double-edged sword' in the treatment against human diseases cautioning researchers about the potential ramifications of off-target pharmacological effects.
糖原合成酶激酶-3（GSK-3）抑制剂是用于人类疾病临床干预的一种新兴工具，也是联合治疗领域的一个细分领域。它们在神经系统疾病、2型糖尿病、再生医学和癌症的应用中具有多方面作用。然而，相互矛盾的报道表明GSK-3抑制剂在癌症中的作用存在争议。本综述旨在强调GSK-3抑制剂作为分子靶向研究工具的兴起及其向有前景的候选药物的转变。该综述还聚焦于关键的GSK-3抑制剂及其在癌症和再生医学中的作用，特别强调了替格列净。此外，还将简要回顾GSK-3在各种分子途径中的决定性作用。最后，本综述总结了GSK-3抑制剂在治疗人类疾病中作为“双刃剑”的出现，提醒研究人员注意脱靶药理效应的潜在影响。
