메뉴 건너뛰기




Volumn 232, Issue , 2016, Pages 43-58

Emerging target families: Intractable targets

Author keywords

Druggability; Epigenetic reader domains; Phosphatases; Protein interaction inhibitors; RAS; Structure based design

Indexed keywords

4 (4 CHLOROPHENYL) 2,3,9 TRIMETHYL 6H THIENO[3,2 F][1,2,4]TRIAZOLO[4,3 A][1,4]DIAZEPINE 6 ACETIC ACID TERT BUTYL ESTER; BROMODOMAIN INHIBITOR; GUANOSINE TRIPHOSPHATASE; LONAFARNIB; NSC 87877; OICR 9429; PACLITAXEL; PHOSPHATASE; PROTEIN MDM2; PROTEIN P53; PROTEIN TYROSINE PHOSPHATASE; PROTEIN TYROSINE PHOSPHATASE 1B; PROTEIN TYROSINE PHOSPHATASE INHIBITOR; PROTEIN TYROSINE PHOSPHATASE SHP 2; PROTEIN TYROSINE PHOSPHATASE SHP 2 INHIBITOR; RAPAMYCIN; RAS PROTEIN; TIPIFARNIB; TRODUSQUEMINE; UNC 1215; UNCLASSIFIED DRUG;

EID: 84962743618     PISSN: 01712004     EISSN: 18650325     Source Type: Book Series    
DOI: 10.1007/164_2015_28     Document Type: Chapter
Times cited : (8)

References (67)
  • 3
    • 77958056047 scopus 로고    scopus 로고
    • Protein tyrosine phosphatases as drug targets: Strategies and challenges of inhibitor development
    • Barr AJ (2010) Protein tyrosine phosphatases as drug targets: strategies and challenges of inhibitor development. Future Med Chem 2(10):1563-1576
    • (2010) Future Med Chem , vol.2 , Issue.10 , pp. 1563-1576
    • Barr, A.J.1
  • 5
    • 34249018367 scopus 로고    scopus 로고
    • GEFs and GAPs: Critical elements in the control of small G proteins
    • Bos JL, Rehmann H, Wittinghofer A (2007) GEFs and GAPs: critical elements in the control of small G proteins. Cell 129(5):865-877
    • (2007) Cell , vol.129 , Issue.5 , pp. 865-877
    • Bos, J.L.1    Rehmann, H.2    Wittinghofer, A.3
  • 8
    • 43049093663 scopus 로고    scopus 로고
    • The tyrosine phosphatase Shp2 (PTPN11) in cancer
    • Chan G, Kalaitzidis D, Neel BG (2008) The tyrosine phosphatase Shp2 (PTPN11) in cancer. Cancer Metastasis Rev 27(2):179-192
    • (2008) Cancer Metastasis Rev , vol.27 , Issue.2 , pp. 179-192
    • Chan, G.1    Kalaitzidis, D.2    Neel, B.G.3
  • 12
    • 0141726877 scopus 로고    scopus 로고
    • A 'rule of three' for fragment-based lead discovery?
    • Congreve M, Carr R, Murray C, Jhoti H (2003) A 'rule of three' for fragment-based lead discovery? Drug Discov Today 8(19):876-877
    • (2003) Drug Discov Today , vol.8 , Issue.19 , pp. 876-877
    • Congreve, M.1    Carr, R.2    Murray, C.3    Jhoti, H.4
  • 17
    • 84899973908 scopus 로고    scopus 로고
    • Targeting bromodomains: Epigenetic readers of lysine acetylation
    • Filippakopoulos P, Knapp S (2014) Targeting bromodomains: epigenetic readers of lysine acetylation. Nat Rev Drug Discov 13(5):337-356
    • (2014) Nat Rev Drug Discov , vol.13 , Issue.5 , pp. 337-356
    • Filippakopoulos, P.1    Knapp, S.2
  • 22
    • 17144373303 scopus 로고    scopus 로고
    • Druggability indices for protein targets derived from NMR-based screening data
    • Hajduk PJ, Huth JR, Fesik SW (2005) Druggability indices for protein targets derived from NMR-based screening data. J Med Chem 48(7):2518-2525
    • (2005) J Med Chem , vol.48 , Issue.7 , pp. 2518-2525
    • Hajduk, P.J.1    Huth, J.R.2    Fesik, S.W.3
  • 23
    • 65249117514 scopus 로고    scopus 로고
    • Identifying and characterizing binding sites and assessing druggability
    • Halgren TA (2009) Identifying and characterizing binding sites and assessing druggability. J Chem Inf Model 49(2):377-389
    • (2009) J Chem Inf Model , vol.49 , Issue.2 , pp. 377-389
    • Halgren, T.A.1
  • 25
    • 80455131079 scopus 로고    scopus 로고
    • Drug discovery toward antagonists of methyllysine binding proteins
    • Herold JM, Ingerman LA, Gao C, Frye SV (2011a) Drug discovery toward antagonists of methyllysine binding proteins. Curr Chem Genomics 5:51-61
    • (2011) Curr Chem Genomics , vol.5 , pp. 51-61
    • Herold, J.M.1    Ingerman, L.A.2    Gao, C.3    Frye, S.V.4
  • 28
  • 32
    • 33847202286 scopus 로고    scopus 로고
    • Protein tyrosine phosphatase 1B deficiency or inhibition delays ErbB2-induced mammary tumorigenesis and protects from lung metastasis
    • Julien SG, Dube N, Read M, Penney J, Paquet M, Han Y, Kennedy BP, Muller WJ, Tremblay ML (2007) Protein tyrosine phosphatase 1B deficiency or inhibition delays ErbB2-induced mammary tumorigenesis and protects from lung metastasis. Nat Genet 39(3):338-346
    • (2007) Nat Genet , vol.39 , Issue.3 , pp. 338-346
    • Julien, S.G.1    Dube, N.2    Read, M.3    Penney, J.4    Paquet, M.5    Han, Y.6    Kennedy, B.P.7    Muller, W.J.8    Tremblay, M.L.9
  • 36
    • 84890886196 scopus 로고    scopus 로고
    • Small-molecule modulators for epigenetics targets
    • Knapp S, Weinmann H (2013) Small-molecule modulators for epigenetics targets. ChemMedChem 8(11):1885-1891
    • (2013) ChemMedChem , vol.8 , Issue.11 , pp. 1885-1891
    • Knapp, S.1    Weinmann, H.2
  • 39
    • 0035289779 scopus 로고    scopus 로고
    • Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
    • Lipinski CA, Lombardo F, Dominy BW, Feeney PJ (2001) Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Deliv Rev 46(1-3):3-26
    • (2001) Adv Drug Deliv Rev , vol.46 , Issue.1-3 , pp. 3-26
    • Lipinski, C.A.1    Lombardo, F.2    Dominy, B.W.3    Feeney, P.J.4
  • 45
    • 84888639050 scopus 로고    scopus 로고
    • K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions
    • Ostrem JM, Peters U, Sos ML, Wells JA, Shokat KM (2013) K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions. Nature 503(7477):548-551
    • (2013) Nature , vol.503 , Issue.7477 , pp. 548-551
    • Ostrem, J.M.1    Peters, U.2    Sos, M.L.3    Wells, J.A.4    Shokat, K.M.5
  • 49
    • 0034507958 scopus 로고    scopus 로고
    • Molecular basis for the dephosphorylation of the activation segment of the insulin receptor by protein tyrosine phosphatase 1B
    • Salmeen A, Andersen JN, Myers MP, Tonks NK, Barford D (2000) Molecular basis for the dephosphorylation of the activation segment of the insulin receptor by protein tyrosine phosphatase 1B. Mol Cell 6(6):1401-1412
    • (2000) Mol Cell , vol.6 , Issue.6 , pp. 1401-1412
    • Salmeen, A.1    Andersen, J.N.2    Myers, M.P.3    Tonks, N.K.4    Barford, D.5
  • 50
  • 51
    • 0035861668 scopus 로고    scopus 로고
    • Acquisition of a specific and potent PTP1B inhibitor from a novel combinatorial library and screening procedure
    • Shen K, Keng YF, Wu L, Guo XL, Lawrence DS, Zhang ZY (2001) Acquisition of a specific and potent PTP1B inhibitor from a novel combinatorial library and screening procedure. J Biol Chem 276(50):47311-47319
    • (2001) J Biol Chem , vol.276 , Issue.50 , pp. 47311-47319
    • Shen, K.1    Keng, Y.F.2    Wu, L.3    Guo, X.L.4    Lawrence, D.S.5    Zhang, Z.Y.6
  • 52
    • 78649523910 scopus 로고    scopus 로고
    • Drug-like density: A method of quantifying the "bindability" of a protein target based on a very large set of pockets and drug-like ligands from the Protein Data Bank
    • Sheridan RP, Maiorov VN, Holloway MK, Cornell WD, Gao YD (2010) Drug-like density: a method of quantifying the "bindability" of a protein target based on a very large set of pockets and drug-like ligands from the Protein Data Bank. J Chem Inf Model 50(11):2029-2040
    • (2010) J Chem Inf Model , vol.50 , Issue.11 , pp. 2029-2040
    • Sheridan, R.P.1    Maiorov, V.N.2    Holloway, M.K.3    Cornell, W.D.4    Gao, Y.D.5
  • 53
    • 0030764557 scopus 로고    scopus 로고
    • Severe defects in immunity and hematopoiesis caused by SHP-1 protein-tyrosine-phosphatase deficiency
    • Shultz LD, Rajan TV, Greiner DL (1997) Severe defects in immunity and hematopoiesis caused by SHP-1 protein-tyrosine-phosphatase deficiency. Trends Biotechnol 15(8):302-307
    • (1997) Trends Biotechnol , vol.15 , Issue.8 , pp. 302-307
    • Shultz, L.D.1    Rajan, T.V.2    Greiner, D.L.3
  • 54
    • 79959444149 scopus 로고    scopus 로고
    • Analysis of in vitro bioactivity data extracted from drug discovery literature and patents: Ranking 1654 human protein targets by assayed compounds and molecular scaffolds
    • Southan C, Boppana K, Jagarlapudi SA, Muresan S (2011) Analysis of in vitro bioactivity data extracted from drug discovery literature and patents: ranking 1654 human protein targets by assayed compounds and molecular scaffolds. J Cheminform 3(1):14
    • (2011) J Cheminform , vol.3 , Issue.1 , pp. 14
    • Southan, C.1    Boppana, K.2    Jagarlapudi, S.A.3    Muresan, S.4
  • 56
    • 33845901313 scopus 로고    scopus 로고
    • MDM2 inhibitors for cancer therapy
    • Vassilev LT (2007) MDM2 inhibitors for cancer therapy. Trends Mol Med 13(1):23-31
    • (2007) Trends Mol Med , vol.13 , Issue.1 , pp. 23-31
    • Vassilev, L.T.1
  • 57
    • 0037030653 scopus 로고    scopus 로고
    • Molecular properties that influence the oral bioavailability of drug candidates
    • Veber DF, Johnson SR, Cheng HY, Smith BR, Ward KW, Kopple KD (2002) Molecular properties that influence the oral bioavailability of drug candidates. J Med Chem 45(12):2615-2623
    • (2002) J Med Chem , vol.45 , Issue.12 , pp. 2615-2623
    • Veber, D.F.1    Johnson, S.R.2    Cheng, H.Y.3    Smith, B.R.4    Ward, K.W.5    Kopple, K.D.6
  • 58
    • 84866338076 scopus 로고    scopus 로고
    • Druggability analysis and structural classification of bromodomain acetyl-lysine binding sites
    • Vidler LR, Brown N, Knapp S, Hoelder S (2012) Druggability analysis and structural classification of bromodomain acetyl-lysine binding sites. J Med Chem 55(17):7346-7359
    • (2012) J Med Chem , vol.55 , Issue.17 , pp. 7346-7359
    • Vidler, L.R.1    Brown, N.2    Knapp, S.3    Hoelder, S.4
  • 60
    • 84865463399 scopus 로고    scopus 로고
    • Ras inhibition via direct Ras binding-is there a path forward?
    • Wang W, Fang G, Rudolph J (2012) Ras inhibition via direct Ras binding-is there a path forward? Bioorg Med Chem Lett 22(18):5766-5776
    • (2012) Bioorg Med Chem Lett , vol.22 , Issue.18 , pp. 5766-5776
    • Wang, W.1    Fang, G.2    Rudolph, J.3
  • 63
    • 27644483149 scopus 로고    scopus 로고
    • Overexpression of Shp2 tyrosine phosphatase is implicated in leukemogenesis in adult human leukemia
    • Xu R, Yu Y, Zheng S, Zhao X, Dong Q, He Z, Liang Y, Lu Q, Fang Y, Gan X et al (2005) Overexpression of Shp2 tyrosine phosphatase is implicated in leukemogenesis in adult human leukemia. Blood 106(9):3142-3149
    • (2005) Blood , vol.106 , Issue.9 , pp. 3142-3149
    • Xu, R.1    Yu, Y.2    Zheng, S.3    Zhao, X.4    Dong, Q.5    He, Z.6    Liang, Y.7    Lu, Q.8    Fang, Y.9    Gan, X.10
  • 64
    • 0030769147 scopus 로고    scopus 로고
    • Impaired bone marrow microenvironment and immune function in T cell protein tyrosine phosphatase-deficient mice
    • You-Ten KE, Muise ES, Itie A, Michaliszyn E, Wagner J, Jothy S, Lapp WS, Tremblay ML (1997) Impaired bone marrow microenvironment and immune function in T cell protein tyrosine phosphatase-deficient mice. J Exp Med 186(5):683-693
    • (1997) J Exp Med , vol.186 , Issue.5 , pp. 683-693
    • You-Ten, K.E.1    Muise, E.S.2    Itie, A.3    Michaliszyn, E.4    Wagner, J.5    Jothy, S.6    Lapp, W.S.7    Tremblay, M.L.8
  • 67
    • 44049086087 scopus 로고    scopus 로고
    • SHP2 is up-regulated in breast cancer cells and in infiltrating ductal carcinoma of the breast, implying its involvement in breast oncogenesis
    • Zhou X, Coad J, Ducatman B, Agazie YM (2008) SHP2 is up-regulated in breast cancer cells and in infiltrating ductal carcinoma of the breast, implying its involvement in breast oncogenesis. Histopathology 53(4):389-402
    • (2008) Histopathology , vol.53 , Issue.4 , pp. 389-402
    • Zhou, X.1    Coad, J.2    Ducatman, B.3    Agazie, Y.M.4


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.