Figures & data
Table 1. Inhibition parameters of CGA, UA and SUR compounds using the three PTP1B constructs.
Table 2. Previously reported inhibition and kinetic parameters using short and full PTP1B constructs.
Table 3. Kinetic parameters of inhibition and type of inhibition of different compounds using hPTP1B1-400.
Table 4. Theoretical binding properties of hPTP1B1-400 inhibitor complex.
Liu G, Xin Z, Liang H, Abad-Zapatero C, Hajduk PJ, Janowick DA, Szczepankiewicz BG, Pei Z, Hutchins CW, Ballaron SJ, et al. Selective protein tyrosine phosphatase 1B inhibitors: Targeting the second phosphotyrosine binding site with non-carboxylic acid-containing ligands. J Med Chem. 2003;46(16):3437–3440. Kyriakou E, Schmidt S, Dodd GT, Pfuhlmann K, Simonds SE, Lenhart D, Geerlof A, Schriever SC, De Angelis M, Schramm KW, et al. Celastrol promotes weight loss in diet-induced obesity by inhibiting the protein tyrosine phosphatases PTP1B and TCPTP in the hypothalamus. J Med Chem. 2018;61(24):11144–11157. Zhang XY, Li W, Wang J, Li N, Cheng MS, Koike K. Protein tyrosine phosphatase 1B inhibitory activities of ursane-type triterpenes from Chinese raspberry, fruits of Rubus chingii. Chin J Nat Med. 2019;17(1):15–21. Zhao BT, Nguyen DH, Le DD, Choi JS, Min BS, Woo MH. Protein tyrosine phosphatase 1B inhibitors from natural sources. Arch Pharm Res. 2018;41(2):130–161. Zhang W, Hong D, Zhou Y, Zhang Y, Shen Q, Li J. y, Hu L. h, Li J. Ursolic acid and its derivative inhibit protein tyrosine phosphatase 1B, enhancing insulin receptor phosphorylation and stimulating glucose uptake. Biochim Biophys Acta. 2006;1760(10):1505–1512. De-La-Cruz-Martínez L, Duran-Becerra C, González-Andrade M, Páez-Franco JC, Germán-Acacio JM, Espinosa-Chávez J, Torres-Valencia JM, Pérez-Villanueva J, Palacios-Espinosa JF, Soria-Arteche O, et al. Indole- and pyrazole-glycyrrhetinic acid derivatives as PTP1B inhibitors: synthesis, in vitro and in silico studies. Molecules. 2021;26(14):4375. Erbe DV, Wang S, Zhang YL, Harding K, Kung L, Tam M, Stolz L, Xing Y, Furey S, Qadri A, et al. Ertiprotafib improves glycemic control and lowers lipids via multiple mechanisms. Mol Pharmacol. 2005;67(1):69–77. Kumar GS, Page R, Petiid W. The mode of action of the Protein tyrosine phosphatase 1B inhibitor ertiprotafib; 2020. Available from: Lipchock JM, Hendrickson HP, Douglas BB, Bird KE, Ginther PS, Rivalta I, Ten NS, Batista VS, Loria JP. Characterization of protein tyrosine phosphatase 1B inhibition by chlorogenic acid and cichoric acid. Biochemistry. 2017;56(1):96–106. Baskaran SK, Goswami N, Selvaraj S, Muthusamy VS, Lakshmi BS. Molecular dynamics approach to probe the allosteric inhibition of PTP1B by chlorogenic and cichoric acid. J Chem Inf Model. 2012;52(8):2004–2012. Luo J, Zheng M, Jiang B, Li C, Guo S, Wang L, Li X, Yu R, Shi D. Antidiabetic activity in vitro and in vivo of BDB, a selective inhibitor of protein tyrosine phosphatase 1B, from Rhodomela confervoides. Br J Pharmacol. 2020;177(19):4464–4480. Krishnan N, Konidaris KF, Gasser G, Tonks NK. A potent, selective, and orally bioavailable inhibitor of the protein-tyrosine phosphatase PTP1B improves insulin and leptin signaling in animal models. J Biol Chem. 2018;293(5):1517–1525. Andersen HS, Iversen LF, Jeppesen CB, Branner S, Norris K, Rasmussen HB, Moller KB, Møller NPH. 2-(oxalylamino)-benzoic acid is a general, competitive inhibitor of protein-tyrosine phosphatases. J Biol Chem. 2000;275(10):7101–7108. Xin Z, Liu G, Abad-Zapatero C, Pei Z, Szczepankiewicz BG, Li X, Zhang T, Hutchins CW, Hajduk PJ, Ballaron SJ, et al. Identification of a monoacid-based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B. Bioorg Med Chem Lett. 2003;13(22):3947–3950. Tian Zhao B, Hung Nguyen D, Mi Lee B, Hui Seong S, Sue Choi J, Sun Min B, Hee Woo M. PTP1B inhibitory and cytotoxic activities of triterpenoids from the aerial parts of Agrimonia pilosa. Med Chem Res. 2017;26(11):2870–2878. Zhang YL, Keng YF, Zhao Y, Wu L, Zhang ZY. Suramin is an active site-directed, reversible, and tight-binding inhibitor of protein-tyrosine phosphatases. J Biol Chem. 1998;273(20):12281–12287. McCain DF, Wu L, Nickel P, Kassack MU, Kreimeyer A, Gagliardi A, Collins DC, Zhang ZY. Suramin derivatives as inhibitors and activators of protein-tyrosine phosphatases. J Biol Chem. 2004;279(15):14713–14725. Krishnan N, Koveal D, Miller DH, Xue B, Akshinthala SD, Kragelj J, Jensen MR, Gauss CM, Page R, Blackledge M, et al. Targeting the disordered C terminus of PTP1B with an allosteric inhibitor. Nat Chem Biol. 2014;10(7):558–566. Lantz KA, Hart SGE, Planey SL, Roitman MF, Ruiz-White IA, Wolfe HR, McLane MP. Inhibition of PTP1B by trodusquemine (MSI-1436) causes fat-specific weight loss in diet-induced obese mice. Obesity. 2010;18(8):1516–1523.