KD025 (SLx-2119) suppresses adipogenesis at intermediate stage in human adipose-derived stem cells

References

• Coelho M, Oliveira T, Fernandes R. Biochemistry of adipose tissue: an endocrine organ. Arch Med Sci. 2013;9:191–200.
   PubMed Web of Science ®Google Scholar
• Galic S, Oakhill JS, Steinberg GR. Adipose tissue as an endocrine organ. Mol Cell Endocrinol. 2010;316:129–139.
   PubMed Web of Science ®Google Scholar
• Lowe CE, O’Rahilly S, Rochford JJ. Adipogenesis at a glance. J Cell Sci. 2011;124:2681–2686.
   PubMed Web of Science ®Google Scholar
• Rosen ED, MacDougald OA. Adipocyte differentiation from the inside out. Nat Rev Mol Cell Biol. 2006;7:885–896.
   PubMed Web of Science ®Google Scholar
• Rosen ED, Hsu C-H, Wang X, et al. C/EBPα induces adipogenesis through PPARγ: a unified pathway. Genes Dev. 2002;16:22–26.
   PubMed Web of Science ®Google Scholar
• Cristancho AG, Lazar MA. Forming functional fat: a growing understanding of adipocyte differentiation. Nat Rev Mol Cell Biol. 2011;12:722–734.
   PubMed Web of Science ®Google Scholar
• Rosen ED, Walkey CJ, Puigserver P, et al. Transcriptional regulation of adipogenesis. Genes Dev. 2000;14:1293–1307.
   PubMed Web of Science ®Google Scholar
• Amano M, Nakayama M, Kaibuchi K. Rho-kinase/ROCK: a key regulator of the cytoskeleton and cell polarity. Cytoskeleton (Hoboken, NJ) 2010; 67:545–554.
   PubMed Web of Science ®Google Scholar
• Feng Y, LoGrasso PV, Defert O, et al. (ROCK) inhibitors and their therapeutic potential. J Med Chem. 2016;59:2269–2300.
   PubMed Web of Science ®Google Scholar
• Riento K, Ridley AJ. ROCKs: multifunctional kinases in cell behaviour. Nat Rev Mol Cell Biol. 2003;4:446–456.
   PubMed Web of Science ®Google Scholar
• Sordella R, Jiang W, Chen G-C, et al. Modulation of Rho GTPase signaling regulates a switch between adipogenesis and myogenesis. Cell. 2003;113:147–158.
   PubMed Web of Science ®Google Scholar
• Jaffe AB, Hall A. RHO GTPASES: biochemistry and biology. Annu Rev Cell Dev Biol. 2005;21:247–269.
   PubMed Web of Science ®Google Scholar
• McBeath R, Pirone DM, Nelson CM, et al. Cell shape, cytoskeletal tension, and RhoA regulate stem cell lineage commitment. Dev Cell. 2004;6:483–495.
   PubMed Web of Science ®Google Scholar
• Noguchi M, Hosoda K, Fujikura J, et al. Genetic and pharmacological inhibition of Rho-associated kinase II enhances adipogenesis. J Biol Chem. 2007;282:29574–29583.
   PubMed Web of Science ®Google Scholar
• Boerma M, Fu Q, Wang J, et al. Comparative gene expression profiling in three primary human cell lines after treatment with a novel inhibitor of Rho kinase or atorvastatin. Blood Coagul Fibrinolysis. 2008;19:709–718.
   PubMed Web of Science ®Google Scholar
• De Silva TM, Kinzenbaw DA, Modrick ML, et al. Heterogeneous impact of ROCK2 on carotid and cerebrovascular function. Hypertension. 2016;68:809–817.
   PubMed Web of Science ®Google Scholar
• Zanin-Zhorov A, Weiss JM, Nyuydzefe MS, et al. Selective oral ROCK2 inhibitor down-regulates IL-21 and IL-17 secretion in human T cells via STAT3-dependent mechanism. Proc Natl Acad Sci U S A. 2014;111:16814–16819.
   PubMed Web of Science ®Google Scholar
• Zanin-Zhorov A, Weiss JM, Trzeciak A, et al. Cutting edge: selective oral ROCK2 inhibitor reduces clinical scores in patients with psoriasis vulgaris and Normalizes skin pathology via concurrent regulation of IL-17 and IL-10. J Immunol. 2017;198:3809–3814.
   PubMed Web of Science ®Google Scholar
• Diep DTV, Hong K, Khun T, et al. Anti-adipogenic effects of KD025 (SLx-2119), a ROCK2-specific inhibitor, in 3T3-L1 cells. Sci Rep. 2018;8:2477.
   PubMed Web of Science ®Google Scholar
• Sasaki Y, Suzuki M, Hidaka H. The novel and specific Rho-kinase inhibitor (S)-(+)-2-methyl-1-[(4-methyl-5-isoquinoline)sulfonyl]-homopiperazine as a probing molecule for Rho-kinase-involved pathway. Pharmacol Ther. 2002;93:225–232.
   PubMed Web of Science ®Google Scholar
• Rodriguez A-M, Elabd C, Delteil F, et al. Adipocyte differentiation of multipotent cells established from human adipose tissue. Biochem Biophys Res Commun. 2004;315:255–263.
   PubMed Web of Science ®Google Scholar
• Wang T, Kang W, Du L, et al. Rho-kinase inhibitor Y-27632 facilitates the proliferation, migration and pluripotency of human periodontal ligament stem cells. J Cell Mol Med. 2017;21:3100–3112.
   PubMed Web of Science ®Google Scholar
• Liao JK, Seto M, Noma K. Rho kinase (ROCK) inhibitors. J Cardiovasc Pharmacol. 2007;50:17–24.
   PubMed Web of Science ®Google Scholar
• Lee S-H, Huang H, Choi K, et al. ROCK1 isoform-specific deletion reveals a role for diet-induced insulin resistance. Am J Physiol Endocrinol Metab. 2014;306:E332–E343.
   PubMed Web of Science ®Google Scholar
• Chun KH, Araki K, Jee Y, et al. Regulation of glucose transport by ROCK1 differs from that of ROCK2 and is controlled by actin polymerization. Endocrinology. 2012;153:1649–1662.
   PubMed Web of Science ®Google Scholar
• Chun KH, Choi KD, Lee DH, et al. In vivo activation of ROCK1 by insulin is impaired in skeletal muscle of humans with type 2 diabetes. Am J Physiol Endocrinol Metab. 2011;300:E536–E542.
   PubMed Web of Science ®Google Scholar
• Soliman H, Varela JN, Nyamandi V, et al. Attenuation of obesity-induced insulin resistance in mice with heterozygous deletion of ROCK2. Int J Obes (Lond). 2016;40:1435–1443.
   PubMed Web of Science ®Google Scholar
• Santos R, Ursu O, Gaulton A, et al. A comprehensive map of molecular drug targets. Nat Rev Drug Discov. 2016;16:19–34.
   PubMed Web of Science ®Google Scholar
• Otto TC, Lane MD. Adipose development: from stem cell to adipocyte. Crit Rev Biochem Mol Biol. 2005;40:229–242.
   PubMed Web of Science ®Google Scholar
• Bunnell BA, Flaat M, Gagliardi C, et al. Adipose-derived stem cells: isolation, expansion and differentiation. Methods. 2008;45:115–120.
   PubMed Web of Science ®Google Scholar
• Zuk PA, Zhu M, Ashjian P, et al. Human adipose tissue is a source of multipotent stem cells. Mol Biol Cell. 2002;13:4279–4295.
   PubMed Web of Science ®Google Scholar
• Moseti D, Regassa A, Kim W-K. Molecular regulation of adipogenesis and potential anti-adipogenic bioactive molecules. Int J Mol Sci. 2016;17:124.
   PubMed Web of Science ®Google Scholar
• Summers SA, Whiteman EL, Birnbaum MJ. Insulin signaling in the adipocyte. Int J Obesity. 2000;24:SS67–S70.
   Web of Science ®Google Scholar
• Zhang HH, Huang J, Düvel K, et al. Insulin stimulates adipogenesis through the Akt-TSC2-mTORC1 pathway. PLOS ONE. 2009;4:e6189.
   PubMed Web of Science ®Google Scholar