A REVIEW ON PROTEIN TYROSINE PHOSPHATASES - AN IMPORTANT TARGET FOR VARIOUS DISEASES
DOI:
https://doi.org/10.22159/ajpcr.2018.v11i7.25615Keywords:
Protein tyrosine phosphatase, Diabetes, Cancer, TuberculosisAbstract
The enzyme protein tyrosine phosphatase (PTP) is responsible for the regulation of cellular functions including cell growth, replication, and signal transduction. Dysregulation of this enzyme leads to various diseases including Type II diabetes and cancers as well. The PTP enzyme functions as a promising drug target for these diseases, leading to new innovations in developing new drug targets in the field of clinical studies and pharmacology. The PTP is considered as the next generation drug targets. The protein tyrosine drug targets can be targeted to cure the diseases caused due to its dysregulations. However, due to its complex structure and highly conserved active sites are the major challenges which block this strategy. Moreover, two enzyme proteins PTP A and PTP B of PTP enzyme family are essential for the survival of Mycobacterium in host macrophages and cause infection resulting in chronic tuberculosis. The novel drug-like properties of L335-M34 and L01Z08 compounds are selective inhibitors of this enzyme responsible for the tuberculosis virulence in mammals. Some of the commercial inhibitors such as ertiprotafib, arylbenzonaphthofurans, and arylbenzonaphthothiophenes have also proven to inhibit the enzyme's virulence. This review summarizes the latest innovations to lead a map for developing new innovative drugs against the various classes of target enzymes of tyrosine phosphatase.
Downloads
References
Dutta NK, He R, Pinn ML, He Y, Burrows F, Zhang ZY, et al. Mycobacterial protein tyrosine phosphatases A and B inhibitors augment the bactericidal activity of the standard anti-tuberculosis regimen. ACS Infect Dis 2016;2:231-9.
Cohen P, Alessi DR. Kinase drug discovery–what’s next in the field? ACS Chem Biol 2012;8:96-104.
Kempker RR, Kipiani M, Mirtskhulava V, Tukvadze N, Magee MJ, Blumberg HM, et al. Acquired drug resistance in Mycobacterium tuberculosis and poor outcomes among patients with multidrug-resistant tuberculosis. Emerg Infect Dis 2015;21:992-1001.
Clatworthy AE, Pierson E, Hung DT. Targeting virulence: A new paradigm for antimicrobial therapy. Nat Chem Biol 2007;3:541-8.
Silva AP, Tabernero L. New strategies in fighting TB: Targeting Mycobacterium tuberculosis-secreted phosphatases MptpA & MptpB. Future Med Chem 2010;2:1325-37.
Singh R, Rao V, Shakila H, Gupta R, Khera A, Dhar N, et al. Disruption of mptpB impairs the ability of Mycobacterium tuberculosis to survive in guinea pigs. Mol Microbiol 2003;50:751-62.
Wong D, Bach H, Sun J, Hmama Z, Av-Gay Y. Mycobacterium tuberculosis protein tyrosine phosphatase (PtpA) excludes host vacuolar-H+–ATPase to inhibit phagosome acidification. Proc Natl Acad Sci U S A 2011;108:19371-6.
Zeng LF, Xu J, He Y, He R, Wu L, Gunawan AM, et al. A facile hydroxyindole carboxylic acid based focused library approach for potent and selective inhibitors of mycobacterium protein tyrosine phosphatase B. ChemMedChem 2013;8:904-8.
He RJ, Yu ZH, Zhang RY, Zhang ZY. Protein tyrosine phosphatases as potential therapeutic targets. Acta Pharmacol Sin 2014;35:1227-46.
Yao ZJ, Ye B, Wu XW, Wang S, Wu L, Zhang ZY, et al. Structure-based design and synthesis of small molecule protein–tyrosine phosphatase 1B inhibitors1. Bioorg Med Chem 1998;6:1799-810.
Tobin JF, Tam S. Recent advances in the development of small molecule inhibitors of PTP1B for the treatment of insulin resistance and Type 2 diabetes. Curr Opin Drug Discov Devel 2002;5:500-12.
Tonks NK, Diltz CD, Fischer EH. Purification of the major protein-tyrosine-phosphatases of human placenta. J Biol Chem 1988;263:6722-30.
Tonks NK, Diltz CD, Fischer EH. Characterization of the major protein-tyrosine-phosphatases of human placenta. J Biol Chem 1988;263:6731-7.
Zhang ZY, Lee SY. PTP1B inhibitors as potential therapeutics in the treatment of Type 2 diabetes and obesity. Expert Opin Investig Drugs 2003;12:223-33.
Kaszubska W, Falls HD, Schaefer VG, Haasch D, Frost L, Hessler P, et al. Protein tyrosine phosphatase 1B negatively regulates leptin signaling in a hypothalamic cell line. Mol Cell Endocrinol 2002;195:109-18.
Lund IK, Hansen JA, Andersen HS, Møller NP, Billestrup N. Mechanism of protein tyrosine phosphatase 1B-mediated inhibition of leptin signalling. J Mol Endocrinol 2005;34:339-51.
Combs AP. Recent advances in the discovery of competitive protein tyrosine phosphatase 1B inhibitors for the treatment of diabetes, obesity, and cancer. J Med Chem 2009;53:2333-44.
Lessard L, Stuible M, Tremblay ML. The two faces of PTP1B in cancer. Biochim Biophys Acta 2010;1804:613-9.
Wiener JR, Kerns BJ, Harvey EL, Conaway MR, Lglehart JD, Berchuck A, et al. Overexpression of the protien tyrosine phosphatase PTP1B in human breast cancer: Association with p185c-erbB-2 protein expression. J Natl Cancer Inst 1994;86:372-8.
Bentires-Alj M, Neel BG. Protein-tyrosine phosphatase 1B is required for HER2/Neu–induced breast cancer. Cancer Res 2007;67:2420-4.
He Y, Zeng LF, Yu ZH, He R, Liu S, Zhang ZY, et al. Bicyclic benzofuran and indole-based salicylic acids as protein tyrosine phosphatase inhibitors. Bioorg Med Chem 2012;20:1940-6.
Moreira W, Ngan GJ, Low JL, Poulsen A, Chia BC, Ang MJ, et al. Target mechanism-based whole-cell screening identifies bortezomib as an inhibitor of caseinolytic protease in mycobacteria. MBio 2015;6:e00253-15.
Bjorge JD, Pang A, Fujita DJ. Identification of protein-tyrosine phosphatase 1B as the major tyrosine phosphatase activity capable of dephosphorylating and activating c-src in several human breast cancer cell lines. J Biol Chem 2000;275:41439-46.
Arias-Romero LE, Saha S, Villamar-Cruz O, Yip SC, Ethier SP, Zhang ZY, et al. Activation of src by protein tyrosine phosphatase 1B is required for erbB2 transformation of human breast epithelial cells. Cancer Res 2009;69:4582-8.
Zhu S, Bjorge JD, Fujita DJ. PTP1B contributes to the oncogenic properties of colon cancer cells through src activation. Cancer Res 2007;67:10129-37.
Dubé N, Cheng A, Tremblay ML. The role of protein tyrosine phosphatase 1B in ras signaling. Proc Natl Acad Sci U S A 2004;101:1834-9.
Zhang Z, Lin SY, Neel BG, Haimovich B. Phosphorylated α-actinin and protein-tyrosine phosphatase 1B coregulate the disassembly of the focal adhesion kinase•Src complex and promote cell migration. J Biol Chem 2006;281:1746-54.
Wiener JR, Hurteau JA, Kerns BJ, Whitaker RS, Conaway MR, Berchuck A, et al. Overexpression of the tyrosine phosphatase PTP1B is associated with human ovarian carcinomas. Am J Obstet Gynecol 1994;170:1177-83.
Julien SG, Dubé N, Read M, Penney J, Paquet M, Han Y, et al. Protein tyrosine phosphatase 1B deficiency or inhibition delays erbB2-induced mammary tumorigenesis and protects from lung metastasis. Nat Genet 2007;39:338-46.
Han Y, Belley M, Bayly CI, Colucci J, Dufresne C, Giroux A, et al. Discovery of [(3-bromo-7-cyano-2-naphthyl)(difluoro) methyl] phosphonic acid, a potent and orally active small molecule PTP1B inhibitor. Bioorg Med Chem Lett 2008;18:3200-5.
Erbe DV, Wang S, Zhang YL, Harding K, Kung L, Tam M, et al. Ertiprotafib improves glycemic control and lowers lipids via multiple mechanisms. Mol Pharmacol 2005;67:69-77.
Lantz KA, Hart SG, Planey SL, Roitman MF, Ruiz-White IA, Wolfe HR, et al. Inhibition of PTP1B by trodusquemine (MSI-1436) causes fat-specific weight loss in diet-induced obese mice. Obesity 2010;18:1516-23.
Scott LM, Lawrence HR, Sebti SM, Lawrence NJ, Wu J. Targeting protein tyrosine phosphatases for anticancer drug discovery. Curr Pharm Des 2010;16:1843-62.
Bibi SH, Kalsoom SA, Rashid HA. Ligand based approach for pharmacophore generation for identification of novel compounds having antidiabetic activity. Int J Pharm Pharm Sci 2013;5:303-14.
Fantus IG, Kadota S, Deragon G, Foster B, Posner BI. Pervanadate [peroxide(s) of vanadate] mimics insulin action in rat adipocytes via activation of the insulin receptor tyrosine kinase. Biochemistry 1989;28:8864-71.
Posner BI, Faure R, Burgess JW, Bevan AP, Lachance D, Zhang- Sun G, et al. Peroxovanadium compounds. A new class of potent phosphotyrosine phosphatase inhibitors which are insulin mimetics. J Biol Chem 1994;269:4596-604.
Cohen N, Halberstam M, Shlimovich P, Chang CJ, Shamoon H, Rossetti L, et al. Oral vanadyl sulfate improves hepatic and peripheral insulin sensitivity in patients with non-insulin-dependent diabetes mellitus. J Clin Invest 1995;95:2501-9.
Sarmiento M, Puius YA, Vetter SW, Keng YF, Wu L, Zhao Y, et al. Structural basis of plasticity in protein tyrosine phosphatase 1B substrate recognition. Biochemistry 2000;39:8171-9.
Wrobel J, Sredy J, Moxham C, Dietrich A, Li Z, Sawicki DR, et al. PTP1B inhibition and antihyperglycemic activity in the ob/ob mouse model of novel 11-arylbenzo[b]naphtho[2,3-d]furans and 11-arylbenzo[b] naphtho[2,3-d]thiophenes. J Med Chem 1999;42:3199-202.
Peterson RL, Casciotti L, Block L, Goad ME, Tong Z, Meehan JT, et al. Mechanistic toxicogenomic analysis of WAY-144122 administration in sprague–dawley rats. Toxicol Appl Pharmacol 2004;196:80-94.
Bialy L, Waldmann H. Inhibitors of protein tyrosine phosphatases: Next-generation drugs? Angew Chem Int Ed 2005;44:3814-39.
Wiesmann C, Barr KJ, Kung J, Zhu J, Erlanson DA, Shen W, et al. Allosteric inhibition of protein tyrosine phosphatase 1B. Nat Struct Mol Biol 2004;11:730-7.
Bolton JL, Trush MA, Penning TM, Dryhurst G, Monks TJ. Role of quinones in toxicology. Chem Res Toxicol 2000;13:135-60.
Monks TJ, Jones DC. The metabolism and toxicity of quinones, quinonimines, quinone methides, and quinone-thioethers. Curr Drug Metab 2002;3:425-38.
Barf T, Kaptein A. Irreversible protein kinase inhibitors: Balancing the benefits and risks. J Med Chem 2012;55:6243-62.
Sanderson K. Irreversible kinase inhibitors gain traction. Nat Rev Drug Discov 2013;12:649-51.
Pandey SK, Yu XX, Watts LM, Michael MD, Sloop KW, Rivard AR, et al. Reduction of low molecular weight protein-tyrosine phosphatase expression improves hyperglycemia and insulin sensitivity in obese mice. J Biol Chem 2007;282:14291-9.
Rondinone CM, Trevillyan JM, Clampit J, Gum RJ, Berg C, Kroeger P, et al. Protein tyrosine phosphatase 1B reduction regulates adiposity and expression of genes involved in lipogenesis. Diabetes 2002;51:2405-11.
Zinker BA, Rondinone CM, Trevillyan JM, Gum RJ, Clampit JE, Waring JF, et al. PTP1B antisense oligonucleotide lowers PTP1B protein, normalizes blood glucose, and improves insulin sensitivity in diabetic mice. Proc Natl Acad Sci U S A 2002;99:11357-62.
Barr AJ. Protein tyrosine phosphatases as drug targets: Strategies and challenges of inhibitor development. Future Med Chem 2010;2:1563-76.
He R, Zeng LF, He Y, Zhang S, Zhang ZY. Small molecule tools for functional interrogation of protein tyrosine phosphatases. FEBS J 2013;280:731-50.
Kennedy BP. Role of protein tyrosine phosphatase-1B in diabetes and obesity. Biomed Pharmacother 1999;53:466-70.
McGuire MC, Fields RM, Nyomba BL, Raz I, Bogardus C, Tonks NK, et al. Abnormal regulation of protein tyrosine phosphatase activities in skeletal muscle of insulin-resistant humans. Diabetes 1991;40:939-42.
Worm D, Vinten J, Staehr P, Henriksen JE, Handberg A, Beck- Nielsen H, et al. Altered basal and insulin-stimulated phosphotyrosine phosphatase (PTPase) activity in skeletal muscle from NIDDM patients compared with control subjects. Diabetologia 1996;39:1208-14.
Møller NP, Iversen LF, Andersen HS, McCormack JG. Protein tyrosine phosphatases (PTPs) as drug targets: Inhibitors of PTP-1B for the treatment of diabetes. Curr Opin Drug Discov Devel 2000;3:527-40.
Grundner C, Ng HL, Alber T. Mycobacterium tuberculosis protein tyrosine phosphatase ptpB structure reveals a diverged fold and a buried active site. Structure 2005;13:1625-34.
Kolmodin K, Aqvist J. The catalytic mechanism of protein tyrosine phosphatases revisited. FEBS Lett 2001;498:208-13.
Zhang ZY. Protein tyrosine phosphatases: Prospects for therapeutics. Curr Opin Chem Biol 2001;5:416-23.
Hooft van Huijsduijnen R, Bombrun A, Swinnen D. Selecting protein tyrosine phosphatases as drug targets. Drug Discov Today 2002;7:1013-9.
Murillo AC, Li HY, Alber T, Baker EN, Berger JM, Cherney LT, et al. High throughput crystallography of TB drug targets. Infect Disord Drug Targets 2007;7:127-39.
Alonso A, Sasin J, Bottini N, Friedberg I, Friedberg I, Osterman A, et al. Protein tyrosine phosphatases in the human genome. Cell 2004;117:699-711.
Jiang CS, Liang LF, Guo YW. Natural products possessing protein tyrosine phosphatase 1B (PTP1B) inhibitory activity found in the last decades. Acta Pharmacol Sin 2012;33:1217-45.
Thareja S, Aggarwal S, Bhardwaj TR, Kumar M. Protein tyrosine phosphatase 1B inhibitors: A molecular level legitimate approach for the management of diabetes mellitus. Med Res Rev 2012;32:459-517.
Oh WK, Lee CH, Lee MS, Bae EY, Sohn CB, Oh H, et al. Antidiabetic effects of extracts from Psidium guajava. J Ethnopharmacol 2005;96:411-5.
Inbathamizh L, Padmini E. Moringa oleifera flower compounds as potent ligands to drug targets in PC3 cell lines–an in silico analysis. Int J Pharm Pharm Sci 2013;5:377-83.
Singh AN, Baruah MM, Sharma N. Structure based docking studies towards exploring the potential anti-androgen activity of selected phytochemicals against prostate cancer. Sci Rep 2017;7:1955.
Na M, Kim BY, Osada H, Ahn JS. Inhibition of protein tyrosine phosphatase 1B by lupeol and lupenone isolated from Sorbus commixta. J Enzyme Inhib Med Chem 2009;24:1056-9.
Salmeen A, Andersen JN, Myers MP, Tonks NK, Barford D. Molecular basis for the dephosphorylation of the activation segment of the insulin receptor by protein tyrosine phosphatase 1B. Mol cell 2000 Dec 1;6(6):1401-12.
Published
How to Cite
Issue
Section
The publication is licensed under CC By and is open access. Copyright is with author and allowed to retain publishing rights without restrictions.
