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Volumn 57, Issue 23, 2014, Pages 9958-9970

Discovery of potent KIFC1 inhibitors using a method of integrated high-throughput synthesis and screening

Author keywords

[No Author keywords available]

Indexed keywords

AMIDE; CARBOXYLIC ACID; DIMETHYL SULFOXIDE; KINESIN INHIBITOR; MOLECULAR MOTOR; PHENYLALANINE; TRIETHYLAMINE; 5-METHYL-N-(1-OXO-1-(PYRROLIDIN-3-YLAMINO)-3-(6-(3-(TRIFLUOROMETHOXY)PHENYL)PYRIDIN-3-YL)PROPAN-2-YL)-4-PROPYLTHIOPHENE-2-CARBOXAMIDE; ALANINE; HUMAN SPLEEN, EMBRYO, AND TESTES EXPRESSED PROTEIN, HUMAN; KINESIN; PYRIDINE DERIVATIVE;

EID: 84918595366     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm501179r     Document Type: Article
Times cited : (31)

References (35)
  • 1
    • 50349090965 scopus 로고    scopus 로고
    • Intracellular transport and kinesin superfamily proteins, KIFs: Structure, function, and dynamics
    • Hirokawa, N.; Noda, Y. Intracellular transport and kinesin superfamily proteins, KIFs: structure, function, and dynamics Physiol. Rev. 2008, 88, 1089-1118
    • (2008) Physiol. Rev. , vol.88 , pp. 1089-1118
    • Hirokawa, N.1    Noda, Y.2
  • 2
    • 18344371892 scopus 로고    scopus 로고
    • The bipolar mitotic kinesin Eg5 moves on both microtubules that it crosslinks
    • Kapitein, L. C.; Peterman, E. J.; Kwok, B. H.; Kim, J. H.; Kapoor, T. M.; Schmidt, C. F. The bipolar mitotic kinesin Eg5 moves on both microtubules that it crosslinks Nature 2005, 435, 114-118
    • (2005) Nature , vol.435 , pp. 114-118
    • Kapitein, L.C.1    Peterman, E.J.2    Kwok, B.H.3    Kim, J.H.4    Kapoor, T.M.5    Schmidt, C.F.6
  • 3
    • 4644254479 scopus 로고    scopus 로고
    • The rate of bipolar spindle assembly depends on the microtubule-gliding velocity of the mitotic kinesin Eg5
    • Kwok, B. H.; Yang, J. G.; Kapoor, T. M. The rate of bipolar spindle assembly depends on the microtubule-gliding velocity of the mitotic kinesin Eg5 Curr. Biol. 2004, 14, 1783-1788
    • (2004) Curr. Biol. , vol.14 , pp. 1783-1788
    • Kwok, B.H.1    Yang, J.G.2    Kapoor, T.M.3
  • 4
    • 0034682703 scopus 로고    scopus 로고
    • Motor function in the mitotic spindle
    • Heald, R. Motor function in the mitotic spindle Cell 2000, 102, 399-402
    • (2000) Cell , vol.102 , pp. 399-402
    • Heald, R.1
  • 5
    • 0033615357 scopus 로고    scopus 로고
    • Small molecule inhibitor of mitotic spindle bipolarity identified in a phenotype-based screen
    • Mayer, T. U.; Kapoor, T. M.; Haggarty, S. J.; King, R. W.; Schreiber, S. L.; Mithison, T. J. Small molecule inhibitor of mitotic spindle bipolarity identified in a phenotype-based screen Science 1999, 286, 971-974
    • (1999) Science , vol.286 , pp. 971-974
    • Mayer, T.U.1    Kapoor, T.M.2    Haggarty, S.J.3    King, R.W.4    Schreiber, S.L.5    Mithison, T.J.6
  • 14
    • 0028040295 scopus 로고
    • Origins of reversed directionality in the NCD molecular motor
    • Lockhart, A.; Cross, R. A. Origins of reversed directionality in the NCD molecular motor EMBO J. 1994, 13, 751-757
    • (1994) EMBO J. , vol.13 , pp. 751-757
    • Lockhart, A.1    Cross, R.A.2
  • 15
    • 0031020735 scopus 로고    scopus 로고
    • XCTK2: A kinesin-related protein that promotes mitotic spindle assembly in Xenopus laevis egg extracts
    • Walczak, C. E.; Verma, S.; Mitchison, T. J. XCTK2: a kinesin-related protein that promotes mitotic spindle assembly in Xenopus laevis egg extracts J. Cell Biol. 1997, 136, 859-870
    • (1997) J. Cell Biol. , vol.136 , pp. 859-870
    • Walczak, C.E.1    Verma, S.2    Mitchison, T.J.3
  • 17
    • 0032702315 scopus 로고    scopus 로고
    • The kinesin-related protein, HSET, opposes the activity of Eg5 and cross-links microtubules in the mammalian mitotic spindle
    • Mountain, V.; Simerly, C.; Howard, L.; Andod, A.; Schatten, G.; Compton, D. A. The kinesin-related protein, HSET, opposes the activity of Eg5 and cross-links microtubules in the mammalian mitotic spindle J. Cell Biol. 1999, 147, 351-66
    • (1999) J. Cell Biol. , vol.147 , pp. 351-366
    • Mountain, V.1    Simerly, C.2    Howard, L.3    Andod, A.4    Schatten, G.5    Compton, D.A.6
  • 20
    • 23844500772 scopus 로고    scopus 로고
    • High-throughput assays for promiscuous inhibitors
    • 50 values from these two parallel KIFC1 MG assays was computed, and screening hits with a ratio greater than 3 were removed as promiscuous compounds. For reference, see: Feng, B. Y.; Shelat, A.; Doman, T. N.; Guy, R. K.; Shoichet, B. K. High-throughput assays for promiscuous inhibitors Nature Chem. Biol. 2005, 1, 146-148
    • (2005) Nature Chem. Biol. , vol.1 , pp. 146-148
    • Feng, B.Y.1    Shelat, A.2    Doman, T.N.3    Guy, R.K.4    Shoichet, B.K.5
  • 21
    • 17144405643 scopus 로고    scopus 로고
    • Mitotic kinesins: Prospects for antimitotic drug discovery
    • Bergnes, G.; Brejc, K.; Belmont, L. Mitotic kinesins: prospects for antimitotic drug discovery Curr. Top. Med. Chem. 2005, 5, 127-145
    • (2005) Curr. Top. Med. Chem. , vol.5 , pp. 127-145
    • Bergnes, G.1    Brejc, K.2    Belmont, L.3
  • 23
    • 3242771433 scopus 로고    scopus 로고
    • Crystal structure of the motor domain of the human kinetochore protein CENP-E
    • Garcia-Saez, I.; Yen, T.; Wade, R. H.; Kozielski, F. Crystal structure of the motor domain of the human kinetochore protein CENP-E J. Mol. Biol. 2004, 340, 1107-1116
    • (2004) J. Mol. Biol. , vol.340 , pp. 1107-1116
    • Garcia-Saez, I.1    Yen, T.2    Wade, R.H.3    Kozielski, F.4
  • 27
    • 84888297107 scopus 로고    scopus 로고
    • Design, synthesis, and biological evaluation of an allosteric inhibitor of HSET that targets cancer cells with supernumerary centrosomes
    • Following the publication of ref 14, another group has since disclosed structurally different KIFC1 inhibitors.
    • Following the publication of ref 14, another group has since disclosed structurally different KIFC1 inhibitors. Watts, C. A.; Richards, F. M.; Bender, A.; Bond, P. J.; Korb, O.; Kern, O.; Riddick, M.; Owen, P.; Myers, R. M.; Raff, J.; Gergely, F.; Jodrell, D. I.; Ley, S. V. Design, synthesis, and biological evaluation of an allosteric inhibitor of HSET that targets cancer cells with supernumerary centrosomes Chem. Biol. 2013, 20, 1399-1410
    • (2013) Chem. Biol. , vol.20 , pp. 1399-1410
    • Watts, C.A.1    Richards, F.M.2    Bender, A.3    Bond, P.J.4    Korb, O.5    Kern, O.6    Riddick, M.7    Owen, P.8    Myers, R.M.9    Raff, J.10    Gergely, F.11    Jodrell, D.I.12    Ley, S.V.13
  • 28
    • 0026419319 scopus 로고
    • Generation and use of synthetic peptide combinatorial libraries for basic research and drug discovery
    • Houghten, R. A.; Pinilla, C.; Blondelle, S. E.; Appel, J. R.; Dooley, C. T.; Cuervo, J. H. Generation and use of synthetic peptide combinatorial libraries for basic research and drug discovery Nature 1991, 354, 84-86
    • (1991) Nature , vol.354 , pp. 84-86
    • Houghten, R.A.1    Pinilla, C.2    Blondelle, S.E.3    Appel, J.R.4    Dooley, C.T.5    Cuervo, J.H.6
  • 29
    • 0026419328 scopus 로고
    • A new type of synthetic peptide library for identifying ligand-binding activity
    • Lam, K. S.; Salmon, S. E.; Hersh, E. M.; Hruby, V. J.; Kazmierski, W. M.; Knapp, R. J. A new type of synthetic peptide library for identifying ligand-binding activity Nature 1991, 354, 82-84
    • (1991) Nature , vol.354 , pp. 82-84
    • Lam, K.S.1    Salmon, S.E.2    Hersh, E.M.3    Hruby, V.J.4    Kazmierski, W.M.5    Knapp, R.J.6
  • 30
    • 0037321729 scopus 로고    scopus 로고
    • Purification strategies for combinatorial and parallel chemistry
    • Edward, P. J. Purification strategies for combinatorial and parallel chemistry Comb. Chem. High Throughput Screening 2003, 6, 11-27
    • (2003) Comb. Chem. High Throughput Screening , vol.6 , pp. 11-27
    • Edward, P.J.1
  • 32
    • 0035339061 scopus 로고    scopus 로고
    • High-throughput purification of compound libraries
    • Ripka, W. C.; Barker, G.; Krakover, J. High-throughput purification of compound libraries Drug Discovery Today 2001, 6, 471-477
    • (2001) Drug Discovery Today , vol.6 , pp. 471-477
    • Ripka, W.C.1    Barker, G.2    Krakover, J.3
  • 33
    • 40149107624 scopus 로고    scopus 로고
    • A combinatorial method for solution-phase synthesis of labeled bivalent beta-turn mimics
    • Angell, Y.; Chen, D.; Brahimi, F.; Saragovi, H. U.; Burgess, K. A combinatorial method for solution-phase synthesis of labeled bivalent beta-turn mimics J. Am. Chem. Soc. 2008, 130, 556-565
    • (2008) J. Am. Chem. Soc. , vol.130 , pp. 556-565
    • Angell, Y.1    Chen, D.2    Brahimi, F.3    Saragovi, H.U.4    Burgess, K.5
  • 35
    • 3343018903 scopus 로고    scopus 로고
    • Comparative analysis of two C-terminal kinesin motor proteins: KIFC1 and KIFC5A
    • Zhang, Y.; Sperry, A. O. Comparative analysis of two C-terminal kinesin motor proteins: KIFC1 and KIFC5A Cell Motil. Cytoskeleton 2004, 58, 213-230
    • (2004) Cell Motil. Cytoskeleton , vol.58 , pp. 213-230
    • Zhang, Y.1    Sperry, A.O.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.