title: Novel pharmacological modulators of autophagy: an updated patent review (2012-2015).
abstract: Autophagy is a lysosome-dependent degradation pathway that maintains cellular homeostasis in response to a variety of cellular stresses. Accumulating reports based on animal models have indicated the importance of this catabolic program in many human pathophysiological conditions, including diabetes, neurodegenerative diseases, aging, and cancers. Therefore, autophagy has been highlighted as a novel therapeutic target with a wide range of beneficial effects on human diseases. Here, we review the recent advances of our knowledge toward autophagy, as well as the efforts for developing autophagy modulators. Areas covered: The relevant patents (published at 2012-2015) and the research literature claiming the pharmacological modulation of autophagy are reviewed. Also, their molecular mechanisms and potential therapeutic utilities are discussed. Expert opinion: Considering the molecular machinery involved in autophagy induction, the targeting of autophagy-specific protein is very important to design the therapeutic interventions for specifically treating a variety of autophagy-associated disorders. Many patents and the research literature described in this review have shown promising applications of the relevant autophagy modulators for cancer or neurodegeneration treatments, a few of which are already being considered for clinical evaluation. However, most patents have claimed the modulators of autophagy with little information regarding their mechanisms of action. To design highly potent therapeutics, further work, such as developing compounds that specifically target the autophagy-specific machinery, are required.
authors.affiliation: a Department of Biochemistry and Molecular Biology , School of Medicine, Kyung Hee University , Seoul , Korea.
authors.forename: Joohun
authors.initials: J
authors.lastname: Ha
authors.affiliation: b Department of Oral Biochemistry and Molecular Biology , School of Dentistry, Kyung Hee University , Seoul , Korea.
authors.forename: Joungmok
authors.initials: J
authors.lastname: Kim
mesh_terms: D000375:Aging / Q000187:drug effects / Q000502:physiology; D000818:Animals; D001343:Autophagy / Q000187:drug effects*; D003920:Diabetes Mellitus / Q000188:drug therapy / Q000503:physiopathology; D015195:Drug Design; D006706:Homeostasis; D006801:Humans; D008247:Lysosomes / Q000378:metabolism*; D009369:Neoplasms / Q000188:drug therapy / Q000473:pathology; D019636:Neurodegenerative Diseases / Q000188:drug therapy / Q000503:physiopathology; D010330:Patents as Topic
keywords: AMPK/mTORC1; Autophagy; Beclin 1; PIK3C3/VPS34; ULK1; autophagy modulators; cancer; neurodegenerative diseases