ICG Probes Publications

The following publications have benefited, directly or indirectly, from the National Cancer Institute's Initiative for Chemical Genetics (ICG). They represent some of the discoveries of probes made by the ICG or they have used probes discovered by the ICG.

ALx

Loregian, A., Coen, D.M. (2006). Selective anti-cytomegalovirus compounds discovered by screening for inhibitors of subunit interactions of the viral polymerase. Chem. Biol. 13(2), 191-200. [PubMed]

AMI-x

Billecke SS, Kitzmiller LA, Northrup JJ, Whitesall SE, Kimoto M, Hinz AV, D’Alecy LG (2006). Contribution of whole blood to the control of plasma asymmetrical dimethylarginine. Am J Physiol Heart Circ Physiol 291(4):H1788-96. [PubMed]

Scoumanne A, Chen X (2006). The epithelial cell transforming sequence 2, a guanine nucleotide exchange factor for Rho GTPases, is repressed by p53 via protein methyltransferases and is required for G1-S transition. Cancer Res 66(12):6271-9. [PubMed]

Huang S, Litt M, Felsenfeld G (2005). Methylation of histone H4 by arginine methyltransferase PRMT1 is essential in vivo for many subsequent histone modifications. Genes Dev 19(16):1885-93. PubMed

Saksouk N, Bhatti MM, Kieffer S, Smith AT, Musset K, Garin J, Sullivan WJ Jr, Cesbron-Delauw MF, Hakimi MA (2005). Histone-modifying complexes regulate gene expression pertinent to the differentiation of the protozoan parasite Toxoplasma gondii. Mol Cell Biol 25(23):10301-14. [PubMed]

Cheng D, Yadav N, King RW, Swanson MS, Weinstein EJ, Bedford MT (2004). Small molecule regulators of protein arginine methyltransferases. J Biol Chem 279(23):23892-9. [PubMed]

Binucleine

Eggert US, Kiger AA, Richter C, Perlman ZE, Perrimon N, Mitchison TJ, Field CM (2004). Parallel chemical genetic and genome-wide RNAi screens identify cytokinesis inhibitors and targets. PLoS Biol 2(12):e379. [PubMed]

Blebbistatin

Ahuja P, Perriard E, Trimble W, Perriard JC, Ehler E (2006). Probing the role of septins in cardiomyocytes. Exp Cell Res 312(9):1598-609. [PubMed]

Butler TM, Mooers SU, Siegman MJ (2006). Catch force links and the low to high force transition of myosin. Biophys J 90(9):3193-202. [PubMed]

Choi YO, Ryu HJ, Kim HR, Song YS, Kim C, Lee W, Choe H, Leem CH, Jang YJ (2006). Implication of phosphorylation of the myosin II regulatory light chain in insulin-stimulated GLUT4 translocation in 3T3-F442A adipocytes. Exp Mol Med 38(2):180-9. [PubMed]

Fukushima N, Morita Y (2006). Actomyosin-dependent microtubule rearrangement in lysophosphatidic acid-induced neurite remodeling of young cortical neurons. Brain Res 1094(1):65-75. [PubMed]

Hiratsuka T (2006). The interaction of Phe472 with a fluorescent inhibitor bound to the complex of myosin subfragment-1 with nucleotide. Biochemistry 45(4):1234-41. [PubMed]

Hotulainen P, Lappalainen P (2006). Stress fibers are generated by two distinct actin assembly mechanisms in motile cells. J Cell Biol 173(3):383-94. [PubMed]

Kolega J (2006). The role of myosin II motor activity in distributing myosin asymmetrically and coupling protrusive activity to cell translocation. Mol Biol Cell 17(10):4435-45. [PubMed]

Langevin HM, Bouffard NA, Badger GJ, Churchill DL, Howe AK (2006). Subcutaneous tissue fibroblast cytoskeletal remodeling induced by acupuncture: evidence for a mechanotransduction-based mechanism. J Cell Physiol 207(3):767-74. [PubMed]

Malek AM, Xu C, Kim ES, Alper SL (2006). Hypertonicity triggers RhoA-dependent assembly of myosin-containing striated polygonal actin networks in endothelial cells. Am J Physiol Cell Physiol (Epub ahead of print) [PubMed]

Matson S, Markoulaki S, Ducibella T (2006). Antagonists of myosin light chain kinase and of myosin II inhibit specific events of egg activation in fertilized mouse eggs. Biol Reprod 74(1):169-76. [PubMed]

Medeiros NA, Burnette DT, Forscher P (2006). Myosin II functions in actin-bundle turnover in neuronal growth cones. Nat Cell Biol 8(3):215-26. [PubMed]

Miyake Y, Inoue N, Nishimura K, Kinoshita N, Hosoya H, Yonemura S. Actomyosin tension is required for correct recruitment of adherens junction components and zonula occludens formation. Exp Cell Res. 2006 May 15;312(9):1637-50. Epub 2006 Mar 7. [PubMed]

Miyauchi K, Yamamoto Y, Kosaka T, Hosoya H (2006). Myosin II activity is not essential for recruitment of myosin II to the furrow in dividing HeLa cells. Biochem Biophys Res Commun 350(3):543-8. [PubMed]

Miyoshi H, Satoh SK, Yamada E, Hamaguchi Y (2006). Temporal change in local forces and total force all over the surface of the sea urchin egg during cytokinesis. Cell Motil Cytoskeleton 63(4):208-21. [PubMed]

Niggli V, Schmid M, Nievergelt A (2006). Differential roles of Rho-kinase and myosin light chain kinase in regulating shape, adhesion, and migration of HT1080 fibrosarcoma cells. Biochem Biophys Res Commun 343(2):602-8. [PubMed]

Orlando KA, Stone NL, Pittman RN (2006). Rho kinase regulates fragmentation and phagocytosis of apoptotic cells. Exp Cell Res 312(1):5-15. [PubMed]

Rah SY, Park KH, Nam TS, Kim SJ, Kim H, Im MJ, Kim UH (2006). Association of CD38 with nonmuscle myosin heavy chain IIA and Lck is essential for the internalization and activation of CD38. J Biol Chem (Epub ahead of print) [PubMed]

Remond MC, Fee JA, Elson EL, Taber LA (2006). Myosin-based contraction is not necessary for cardiac c-looping in the chick embryo. Anat Embryol (Berl) 443-54. [PubMed]

Rhee AY, Ogut O, Brozovich FV (2006). Nonmuscle myosin, force maintenance, and the tonic contractile phenotype in smooth muscle. Pflugers Arch 452(6):766-74. [PubMed]

Ryu J, Liu L, Wong TP, Wu DC, Burette A, Weinberg R, Wang YT, Sheng M (2006). A critical role for myosin IIb in dendritic spine morphology and synaptic function. Neuron 49(2):175-82. [PubMed]

Suzuki J, Jin ZG, Meoli DF, Matoba T, Berk BC (2006). Cyclophilin A is secreted by a vesicular pathway in vascular smooth muscle cells. Circ Res 98(6):811-7. [PubMed]

Szczepanowska J, Korn ED, Brzeska H (2006). Activation of myosin in HeLa cells causes redistribution of focal adhesions and F-actin from cell center to cell periphery. Cell Motil Cytoskeleton 63(6):356-74. [PubMed]

Tornieri K, Welshhans K, Geddis MS, Rehder V (2006). Control of neurite outgrowth and growth cone motility by phosphatidylinositol-3-kinase. Cell Motil Cytoskeleton 63(4):173-92. [PubMed]

Yoshida K, Soldati T (2006). Dissection of amoeboid movement into two mechanically distinct modes. J Cell Sci 119(Pt 18):3833-44. [PubMed]

Allingham JS, Smith R, Rayment I (2005). The structural basis of blebbistatin inhibition and specificity for myosin II. Nat Struct Mol Biol 12(4):378-9. [PubMed]

Balland M, Richert A, Gallet F (2005). The dissipative contribution of myosin II in the cytoskeleton dynamics of myoblasts. Eur Biophys J 34(3):255-61. [PubMed]

Bastian P, Lang K, Niggemann B, Zaenker KS, Entschladen F (2005). Myosin regulation in the migration of tumor cells and leukocytes within a three-dimensional collagen matrix. Cell Mol Life Sci 62(1):65-76. [PubMed]

Bellion A, Baudoin JP, Alvarez C, Bornens M, Metin C (2005). Nucleokinesis in tangentially migrating neurons comprises two alternating phases: forward migration of the Golgi/centrosome associated with centrosome splitting and myosin contraction at the rear. J Neurosci 25(24):5691-9. [PubMed]

Chan W, Calderon G, Swift AL, Moseley J, Li S, Hosoya H, Arias IM, Ortiz DF (2005). Myosin II regulatory light chain is required for trafficking of bile salt export protein to the apical membrane in Madin-Darby canine kidney cells. J Biol Chem 280(25):23741-7. [PubMed]

Di Ciano-Oliveira C, Lodyga M, Fan L, Szaszi K, Hosoya H, Rotstein OD, Kapus A (2005). Is myosin light-chain phosphorylation a regulatory signal for the osmotic activation of the Na+-K+-2Cl- cotransporter? Am J Physiol Cell Physiol 289(1):C68-81. [PubMed]

Ekman M, Fagher K, Wede M, Stakeberg K, Arner A (2005). Decreased phosphatase activity, increased Ca2+ sensitivity, and myosin light chain phosphorylation in urinary bladder smooth muscle of newborn mice. J Gen Physiol 125(2):187-96. [PubMed]

Fabian L, Forer A (2005). Redundant mechanisms for anaphase chromosome movements: crane-fly spermatocyte spindles normally use actin filaments but also can function without them. Protoplasma 225(3-4):169-84. [PubMed]

Guha M, Zhou M, Wang YL (2005). Cortical actin turnover during cytokinesis requires myosin II. Curr Biol 15(8):732-6. [PubMed]

Gutjahr MC, Rossy J, Niggli V (2005). Role of Rho, Rac, and Rho-kinase in phosphorylation of myosin light chain, development of polarity, and spontaneous migration of Walker 256 carcinosarcoma cells. Exp Cell Res 308(2):422-38. [PubMed]

Ivanov AI, Hunt D, Utech M, Nusrat A, Parkos CA (2005). Differential roles for actin polymerization and a myosin II motor in assembly of the epithelial apical junctional complex. Mol Biol Cell 16(6):2636-50. [PubMed]

Kanada M, Nagasaki A, Uyeda TQ (2005). Adhesion-dependent and contractile ring-independent equatorial furrowing during cytokinesis in mammalian cells. Mol Biol Cell 16(8):3865-72. [PubMed]

Lehmann MJ, Sherer NM, Marks CB, Pypaert M, Mothes W (2005). Actin- and myosin-driven movement of viruses along filopodia precedes their entry into cells. J Cell Biol 170(2):317-25. [PubMed]

Maddala R, Rao VP (2005). α-Crystallin localizes to the leading edges of migrating lens epithelial cells. Exp Cell Res 306(1):203-15. [PubMed]

Murthy K, Wadsworth P (2005). Myosin-II-dependent localization and dynamics of F-actin during cytokinesis. Curr Biol 15(8):724-31. [PubMed]

Nakayama M, Amano M, Katsumi A, Kaneko T, Kawabata S, Takefuji M, Kaibuchi K (2005). Rho-kinase and myosin II activities are required for cell type and environment specific migration. Genes Cells 10(2):107-17. [PubMed]

Polo-Parada L, Plattner F, Bose C, Landmesser LT (2005). NCAM 180 acting via a conserved C-terminal domain and MLCK is essential for effective transmission with repetitive stimulation. Neuron 46(6):917-31. [PubMed]

Sakamoto T, Limouze J, Combs CA, Straight AF, Sellers JR (2005). Blebbistatin, a myosin II inhibitor, is photoinactivated by blue light. Biochemistry 44(2):584-8. [PubMed]

Shewan AM, Maddugoda M, Kraemer A, Stehbens SJ, Verma S, Kovacs EM, Yap AS (2005). Myosin 2 is a key Rho kinase target necessary for the local concentration of E-cadherin at cell-cell contacts. Mol Biol Cell 16(10):4531-42. [PubMed]

Shu S, Liu X, Korn ED (2005). Blebbistatin and blebbistatin-inactivated myosin II inhibit myosin II-independent processes in Dictyostelium. Proc Natl Acad Sci U S A 102(5):1472-7. [PubMed]

Steimle PA, Fulcher FK, Patel YM (2005). A novel role for myosin II in insulin-stimulated glucose uptake in 3T3-L1 adipocytes. Biochem Biophys Res Commun 331(4):1560-5. [PubMed]

Wilkinson S, Paterson HF, Marshall CJ (2005). Cdc42-MRCK and Rho-ROCK signalling cooperate in myosin phosphorylation and cell invasion. Nat Cell Biol 7(3):255-61. [PubMed]

Wong C, Stearns T (2005). Mammalian cells lack checkpoints for tetraploidy, aberrant centrosome number, and cytokinesis failure. BMC Cell Biol 6(1):6. [PubMed]

Xia D, Stull JT, Kamm KE (2005). Myosin phosphatase targeting subunit 1 affects cell migration by regulating myosin phosphorylation and actin assembly. Exp Cell Res 304(2):506-17. [PubMed]

Zhang H, Webb DJ, Asmussen H, Niu S, Horwitz AF (2005). A GIT1/PIX/Rac/PAK signaling module regulates spine morphogenesis and synapse formation through MLC. J Neurosci 25(13):3379-88. [PubMed]

Zhang M, Rao PV (2005). Blebbistatin, a novel inhibitor of myosin II ATPase activity, increases aqueous humor outflow facility in perfused enucleated porcine eyes. Invest Ophthalmol Vis Sci 46(11):4130-8. [PubMed]

Duxbury MS, Ashley SW, Whang EE (2004). Inhibition of pancreatic adenocarcinoma cellular invasiveness by blebbistatin: a novel myosin II inhibitor. Biochem Biophys Res Commun 313(4):992-7. [PubMed]

Gallo G. (2004). Myosin II activity is required for severing-induced axon retraction in vitro. Exp Neurol 189(1):112-21. [PubMed]

Gehler S, Shaw AE, Sarmiere PD, Bamburg JR, Letourneau PC (2004). Brain-derived neurotrophic factor regulation of retinal growth cone filopodial dynamics is mediated through actin depolymerizing factor/cofilin. J Neurosci 24(47):10741-9. [PubMed]

Griffin MA, Sen S, Sweeney HL, Discher DE (2004). Adhesion-contractile balance in myocyte differentiation. J Cell Sci 117(Pt 24):5855-63. [PubMed]

Ivanov AI, McCall IC, Parkos CA, Nusrat A (2004). Role for actin filament turnover and a myosin II motor in cytoskeleton-driven disassembly of the epithelial apical junctional complex. Mol Biol Cell 15(6):2639-51. [PubMed]

Kolega J (2004). Phototoxicity and photoinactivation of blebbistatin in UV and visible light. Biochem Biophys Res Commun 320(3):1020-5. [PubMed]

Kovacs M, Toth J, Hetenyi C, Malnasi-Csizmadia A, Sellers JR (2004). Mechanism of blebbistatin inhibition of myosin II. J Biol Chem 279(34):35557-63. [PubMed]

Limouze J, Straight AF, Mitchison T, Sellers JR (2004). Specificity of blebbistatin, an inhibitor of myosin II. J Muscle Res Cell Motil 25(4-5):337-41. [PubMed]

Pielak RM, Gaysinskaya VA, Cohen WD (2004). Formation and function of the polar body contractile ring in Spisula. Dev Biol 269(2):421-32. [PubMed]

Ponti A, Machacek M, Gupton SL, Waterman-Storer CM, Danuser G (2004). Two distinct actin networks drive the protrusion of migrating cells. Science 305(5691):1782-6. [PubMed]

Ramamurthy B, Yengo CM, Straight AF, Mitchison TJ, Sweeney HL (2004). Kinetic mechanism of blebbistatin inhibition of nonmuscle myosin IIb. Biochemistry 43(46):14832-9. [PubMed]

Rosenblatt J, Cramer LP, Baum B, McGee KM (2004). Myosin II-dependent cortical movement is required for centrosome separation and positioning during mitotic spindle assembly. Cell 117(3):361-72. [PubMed]

Uetake Y, Sluder G (2004). Cell cycle progression after cleavage failure: mammalian somatic cells do not possess a “tetraploidy checkpoint”. J Cell Biol 165(5):609-15. [PubMed]

Yoshizaki H, Ohba Y, Parrini MC, Dulyaninova NG, Bresnick AR, Mochizuki N, Matsuda M (2004). Cell type-specific regulation of RhoA activity during cytokinesis. J Biol Chem 279(43):44756-62. [PubMed]

Abe M, Ho CH, Kamm KE, Grinnell F (2003). Different molecular motors mediate platelet-derived growth factor and lysophosphatidic acid-stimulated floating collagen matrix contraction. J Biol Chem 278(48):47707-12. [PubMed]

Straight AF, Cheung A, Limouze J, Chen I, Westwood NJ, Sellers JR, Mitchison TJ (2003). Dissecting temporal and spatial control of cytokinesis with a myosin II inhibitor. Science 299(5613):1743-7. [PubMed]

BLT-1

Duong M, Collins HL, Jin W, Zanotti I, Favari E, Rothblat GH (2006). Relative contributions of ABCA1 and SR-BI to cholesterol efflux to serum from fibroblasts and macrophages. Arterioscler Thromb Vasc Biol 26(3):541-7. [PubMed]

Ortegren U, Yin L, Ost A, Karlsson H, Nystrom FH, Stralfors P (2006). Separation and characterization of caveolae subclasses in the plasma membrane of primary adipocytes; segregation of specific proteins and functions. FEBS J 273(14):3381-92. [PubMed]

Reboul E, Klein A, Bietrix F, Gleize B, Malezet-Desmoulins C, Schneider M, Margotat A, Lagrost L, Collet X, Borel P (2006). Scavenger receptor class B type I (SR-BI) is involved in vitamin E transport across the enterocyte. J Biol Chem 281(8):4739-45. [PubMed]

Sahoo D, Darlington YF, Pop D, Williams DL, Connelly MA (2006). Scavenger receptor class B Type I (SR-BI) assembles into detergent-sensitive dimers and tetramers. Biochim Biophys Acta. 2006 Mar 31; (Epub ahead of print) [PubMed]

Sun B, Eckhardt ER, Shetty S, van der Westhuyzen DR, Webb NR (2006). Quantitative analysis of SR-BI-dependent HDL retroendocytosis in hepatocytes and fibroblasts. J Lipid Res 47(8):1700-13. [PubMed]

Zimetti F, Weibel GK, Duong M, Rothblat GH (2006). Measurement of cholesterol bidirectional flux between cells and lipoproteins. J Lipid Res 47(3):605-13. [PubMed]

Nieland TJ, Ehrlich M, Krieger M, Kirchhausen T (2005). Endocytosis is not required for the selective lipid uptake mediated by murine SR-BI. Biochim Biophys Acta 1734(1):44-51. [PubMed]

Reboul E, Abou L, Mikail C, Ghiringhelli O, Andre M, Portugal H, Jourdheuil-Rahmani D, Amiot MJ, Lairon D, Borel P (2005). Lutein transport by Caco-2 TC-7 cells occurs partly by a facilitated process involving the scavenger receptor class B type I (SR-BI). Biochem J 387(Pt 2):455-61. [PubMed]

van der Westhuyzen DR, Cai L, de Beer MC, de Beer FC (2005). Serum amyloid A promotes cholesterol efflux mediated by scavenger receptor B-I. J Biol Chem 280(43):35890-5. [PubMed]

Nieland TJ, Chroni A, Fitzgerald ML, Maliga Z, Zannis VI, Kirchhausen T, Krieger M. (2004). Cross-inhibition of SR-BI- and ABCA1-mediated cholesterol transport by the small molecules BLT-4 and glyburide. J Lipid Res 45(7):1256-65. [PubMed]

O'Connell BJ, Denis M, Genest J (2004). Cellular physiology of cholesterol efflux in vascular endothelial cells. Circulation 110(18):2881-8. [PubMed]

Nieland, T., Penman, M., Dori, L., Krieger, M., Kirchhausen, T. (2002). Discovery of chemical inhibitors of the selective transfer of lipids mediated by the HDL receptor SR-BI. Proc. Natl. Acad. Sci. USA. 99, 15422-15427. [PubMed]

BLT-4

Bartosch B, Verney G, Dreux M, Donot P, Morice Y, Penin F, Pawlotsky JM, Lavillette D, Cosset FL (2005). An interplay between hypervariable region 1 of the hepatitis C virus E2 glycoprotein, the scavenger receptor BI, and high-density lipoprotein promotes both enhancement of infection and protection against neutralizing antibodies. J Virol 79(13):8217-29. [PubMed]

Dreux M, Pietschmann T, Granier C, Voisset C, Ricard-Blum S, Mangeot PE, Keck Z, Foung S, Vu-Dac N, Dubuisson J, Bartenschlager R, Lavillette D, Cosset FL (2006). High density lipoprotein inhibits hepatitis C virus-neutralizing antibodies by stimulating cell entry via activation of the scavenger receptor BI. J Biol Chem 281(27):18285-95. [PubMed]

Pagler TA, Rhode S, Neuhofer A, Laggner H, Strobl W, Hinterndorfer C, Volf I, Pavelka M, Eckhardt ER, van der Westhuyzen DR, Schutz GJ, Stangl H (2006). SR-BI-mediated high density lipoprotein (HDL) endocytosis leads to HDL resecretion facilitating cholesterol efflux. J Biol Chem 281(16):11193-204. [PubMed]

Voisset C, Op de Beeck A, Horellou P, Dreux M, Gustot T, Duverlie G, Cosset FL, Vu-Dac N, Dubuisson J (2006). High-density lipoproteins reduce the neutralizing effect of hepatitis C virus (HCV)-infected patient antibodies by promoting HCV entry. J Gen Virol 87(Pt 9):2577-81. [PubMed]

Voisset C, Callens N, Blanchard E, Op De Beeck A, Dubuisson J, Vu-Dac N (2005). High density lipoproteins facilitate hepatitis C virus entry through the scavenger receptor class B type I. J Biol Chem 280(9):7793-9. [PubMed]

Nieland TJ, Chroni A, Fitzgerald ML, Maliga Z, Zannis VI, Kirchhausen T, Krieger M (2004). Cross-inhibition of SR-BI- and ABCA1-mediated cholesterol transport by the small molecules BLT-4 and glyburide. J Lipid Res 45(7):1256-65. [PubMed]

CDI-x

Perlman, Z.E., Mitchison, T.J., Mayer, T.U. (2005). High-content screening and profiling of drug activity in an automated centrosome-duplication assay. Chembiochem 6(1), 145-151. [PubMed]

Cincreasin

Dorer RK, Zhong S, Tallarico JA, Wong WH, Mitchison TJ, Murray AW (2005). A small-molecule inhibitor of Mps1 blocks the spindle-checkpoint response to a lack of tension on mitotic chromosomes. Curr Biol 15(11):1070-6. [PubMed]

Eeyarestatin

Fiebiger E, Hirsch C, Vyas JM, Gordon E, Ploegh HL, Tortorella D (2004). Dissection of the dislocation pathway for type I membrane proteins with a new small molecule inhibitor, eeyarestatin. Mol Biol Cell 15(4):1635-46. [PubMed]

Emunin

Zaarur N, Gabai VL, Porco JA Jr, Calderwood S, Sherman MY (2006). Targeting heat shock response to sensitize cancer cells to proteasome and Hsp90 inhibitors. Cancer Res 66(3):1783-91. [PubMed]

Exo1

Feng Y, Yu S, Lasell TK, Jadhav AP, Macia E, Chardin P, Melancon P, Roth M, Mitchison T, Kirchhausen T (2003). Exo1: a new chemical inhibitor of the exocytic pathway. Proc Natl Acad Sci USA 100(11):6469-74. [PubMed]

Exo2

Feng Y, Jadhav AP, Rodighiero C, Fujinaga Y, Kirchhausen T, Lencer WI (2004). Retrograde transport of cholera toxin from the plasma membrane to the endoplasmic reticulum requires the trans-Golgi network but not the Golgi apparatus in Exo2-treated cells. EMBO Rep 5(6):596-601. [PubMed]

GS4012

Peterson RT, Shaw SY, Peterson TA, Milan DJ, Zhong TP, Schreiber SL, MacRae CA, Fishman MC (2004). Chemical suppression of a genetic mutation in a zebrafish model of aortic coarctation. Nat Biotechnol 22(5):595-9. [PubMed]

Haptamide

Koehler AN, Shamji AF, Schreiber SL (2003). Discovery of an inhibitor of a transcription factor using small molecule microarrays and diversity-oriented synthesis. J Am Chem Soc 125(28):8420-1. [PubMed]

Histacin

Haggarty SJ, Koeller KM, Wong JC, Butcher RA, Schreiber SL (2003). Multidimensional chemical genetic analysis of diversity-oriented synthesis-derived deacetylase inhibitors using cell-based assays. Chem Biol 10(5):383-96. [PubMed]

INCAs

Kang S, Li H, Rao A, Hogan PG (2005). Inhibition of the calcineurin-NFAT interaction by small organic molecules reflects binding at an allosteric site. J Biol Chem 280(45):37698-706. [PubMed]

Roehrl, M.H.A., Kang, S., Aramburu, J., Wagner, G., Rao, A, Hogan, P.G. (2004). Selective inhibition of calcineurin-NFAT signaling by blocking protein-protein interaction with small organic molecules. Proc. Natl. Acad. Sci. U.S.A. 101(20), 7554-9. [PubMed]

ITSA1

Koeller KM, Haggarty SJ, Perkins BD, Leykin I, Wong JC, Kao MC, Schreiber SL (2003). Chemical genetic modifier screens: small molecule trichostatin suppressors as probes of intracellular histone and tubulin acetylation. Chem Biol 10(5):397-410. [PubMed]

JF959602

Sim DS, Merrill-Skoloff G, Furie BC, Furie B, Flaumenhaft R (2004). Initial accumulation of platelets during arterial thrombus formation in vivo is inhibited by elevation of basal cAMP levels. Blood 103(6):2127-34. [PubMed]

Necrostatin

Bao L, Li Y, Deng SX, Landry D, Tabas I (2006). Sitosterol-containing lipoproteins trigger free sterol-induced caspase-independent death in ACAT-competent macrophages: Implications for sterol structure-dependent mechanisms of cell death and for atherosclerotic vascular disease in sitosterolemia. J Biol Chem 281(44):33635-49. [PubMed]

Degterev A, Huang Z, Boyce M, Li Y, Jagtap P, Mizushima N, Cuny GD, Mitchison TJ, Moskowitz MA, Yuan J (2005). Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury. Nat Chem Biol 1(2):112-9. [PubMed]

Teng X, Degterev A, Jagtap P, Xing X, Choi S, Denu R, Yuan J, Cuny GD (2005). Structure-activity relationship study of novel necroptosis inhibitors. Bioorg Med Chem Lett 15(22):5039-44. [PubMed]

Persynthamide

Stern HM, Murphey RD, Shepard JL, Amatruda JF, Straub CT, Pfaff KL, Weber G, Tallarico JA, King RW, Zon LI (2005). Small molecules that delay S phase suppress a zebrafish bmyb mutant. Nat Chem Biol 1(7):366-70. [PubMed]

Rockout

Yarrow JC, Totsukawa G, Charras GT, Mitchison TJ (2005). Screening for cell migration inhibitors via automated microscopy reveals a Rho-kinase inhibitor. Chem Biol 12(3):385-95. [PubMed]

Salubrinal

Cnop M, Ladriere L, Hekerman P, Ortis F, Cardozo AK, Dogusan Z, Flamez D, Boyce M, Yuan J, Eizirik DL (2006). Selective inhibition of EIF2alpha dephosphorylation potentiates fatty acid-induced er stress and causes pancreatic beta -cell dysfunction and apoptosis. J Biol Chem (Epub ahead of print) [PubMed]

Hao W, Takano T, Guillemette J, Papillon J, Ren G, Cybulsky AV (2006). Induction of apoptosis by the Ste20-like kinase SLK, a germinal center kinase that activates apoptosis signal-regulating kinase and p38. J Biol Chem 281(6):3075-84. [PubMed]

Kessel D (2006). Protection of Bcl-2 by salubrinal. Biochem Biophys Res Commun 346(4):1320-3. [PubMed]

Pae HO, Jeong SO, Jeong GS, Kim KM, Kim HS, Kim SA, Kim YC, Kang SD, Kim BN, Chung HT (2006). Curcumin induces pro-apoptotic endoplasmic reticulum stress in human leukemia HL-60 cells. Biochem Biophys Res Commun (Epub ahead of print) [PubMed]

Robert F, Kapp LD, Khan SN, Acker MG, Kolitz S, Kazemi S, Kaufman RJ, Merrick WC, Koromilas AE, Lorsch JR, Pelletier J (2006). Initiation of Protein Synthesis by Hepatitis C Virus Is Refractory to Reduced eIF2•GTP•Met-tRNA_i^Met Ternary Complex Availability. Mol Biol Cell 2006 Aug 23; (Epub ahead of print) [PubMed]

Mierde, D.V., Scheuner, D., Quintens, R., Patel, R., Song, B., Tsukamoto, K., Beullens, M., Kaufman, R.J., Bollen, M., Schuit, F.C. (2006). Glucose activates a PP1 mediated signaling pathway to enhance overall translation in pancreatic beta cells. Endocrinol Nov 2, 2006; [Epub ahead of print] [PubMed]

Boyce M, Bryant KF, Jousse C, Long K, Harding HP, Scheuner D, Kaufman RJ, Ma D, Coen DM, Ron D, Yuan J (2005). A selective inhibitor of eIF2α dephosphorylation protects cells from ER stress. Science 307(5711):935-9. [PubMed]

Long K, Boyce M, Lin H, Yuan J, Ma D (2005). Structure-activity relationship studies of salubrinal lead to its active biotinylated derivative. Bioorg Med Chem Lett 15(17):3849-52. [PubMed]

Smith WW, Jiang H, Pei Z, Tanaka Y, Morita H, Sawa A, Dawson VL, Dawson TM, Ross CA (2005). Endoplasmic reticulum stress and mitochondrial cell death pathways mediate A53T mutant alpha-synuclein-induced toxicity. Hum Mol Genet 14(24):3801-11. [PubMed]

Secramine

Pelish HE, Peterson JR, Salvarezza SB, Rodriguez-Boulan E, Chen JL, Stamnes M, Macia E, Feng Y, Shair MD, Kirchhausen T (2005). Secramine inhibits Cdc42-dependent functions in cells and Cdc42 activation in vitro. Nat Chem Biol 2(1):39-46. [PubMed]

De Regge N, Nauwynck HJ, Geenen K, Krummenacher C, Cohen GH, Eisenberg RJ, Mettenleiter TC, Favoreel HW (2006). α-Herpesvirus glycoprotein D interaction with sensory neurons triggers formation of varicosities that serve as virus exit sites. J Cell Biol 174(2):267-75. [PubMed]

Pelish HE, Ciesla W, Tanaka N, Reddy K, Shair MD, Kirchhausen T, Lencer WI (2006). The Cdc42 inhibitor secramine B prevents cAMP-induced K+ conductance in intestinal epithelial cells. Biochem Pharmacol 71(12):1720-6. [PubMed]

Pula G, Schuh K, Nakayama K, Nakayama KI, Walter U, Poole AW (2006). PKCδ regulates collagen-induced platelet aggregation through inhibition of VASP-mediated filopodia formation. Blood (Epub ahead of print)[PubMed]

SFK1

Butcher RA, Schreiber SL (2003). A small molecule suppressor of FK506 that targets the mitochondria and modulates ionic balance in Saccharomyces cerevisiae. Chem Biol 10(6):521-31. [PubMed]

SFK2

Butcher RA, Schreiber SL (2004). Identification of Ald6p as the target of a class of small-molecule suppressors of FK506 and their use in network dissection. Proc Natl Acad Sci USA 101(21):7868-73. [PubMed]

SMIRs

Huang J, Zhu H, Haggarty SJ, Spring DR, Hwang H, Jin F, Snyder M, Schreiber SL (2004). Finding new components of the target of rapamycin (TOR) signaling network through chemical genetics and proteome chips. Proc Natl Acad Sci USA 101(47):16594-9. [PubMed]

Suptopin-1

Haggarty SJ, Koeller KM, Kau TR, Silver PA, Roberge M, Schreiber SL (2003). Small molecule modulation of the human chromatid decatenation checkpoint. Chem Biol 10(12):1267-79. [PubMed]

Tubacin

Cabrero JR, Serrador JM, Barreiro O, Mittelbrunn M, Naranjo-Suarez S, Martin-Cofreces N, Vicente-Manzanares M, Mazitschek R, Bradner JE, Avila J, Valenzuela-Fernandez A, Sanchez-Madrid F (2006). Lymphocyte chemotaxis is regulated by histone deacetylase 6, independently of its deacetylase activity. Mol Biol Cell 17(8):3435-45. [PubMed]

Carta S, Tassi S, Semino C, Fossati G, Mascagni P, Dinarello CA, Rubartelli A (2006). Histone deacetylase inhibitors prevent exocytosis of interleukin-1beta-containing secretory lysosomes: role of microtubules. Blood 108(5):1618-26. [PubMed]

Santander VS, Bisig CG, Purro SA, Casale CH, Arce CA, Barra HS (2006). Tubulin must be acetylated in order to form a complex with membrane Na(+),K (+)-ATPase and to inhibit its enzyme activity. Mol Cell Biochem 291(1-2):167-74. [PubMed]

Bali P, Pranpat M, Bradner J, Balasis M, Fiskus W, Guo F, Rocha K, Kumaraswamy S, Boyapalle S, Atadja P, Seto E, Bhalla K (2005). Inhibition of histone deacetylase 6 acetylates and disrupts the chaperone function of heat shock protein 90: a novel basis for antileukemia activity of histone deacetylase inhibitors. J Biol Chem 280(29):26729-34. [PubMed]

Hideshima T, Bradner JE, Wong J, Chauhan D, Richardson P, Schreiber SL, Anderson KC (2005). Small-molecule inhibition of proteasome and aggresome function induces synergistic antitumor activity in multiple myeloma. Proc Natl Acad Sci USA 102(24):8567-72. [PubMed]

Iwata A, Riley BE, Johnston JA, Kopito RR (2005). HDAC6 and microtubules are required for autophagic degradation of aggregated huntingtin. J Biol Chem 280(48):40282-92. [PubMed]

Marcus AI, Zhou J, O'Brate A, Hamel E, Wong J, Nivens M, El-Naggar A, Yao TP, Khuri FR, Giannakakou P (2005). The synergistic combination of the farnesyl transferase inhibitor lonafarnib and paclitaxel enhances tubulin acetylation and requires a functional tubulin deacetylase. Cancer Res 65(9):3883-93. [PubMed]

Saji S, Kawakami M, Hayashi S, Yoshida N, Hirose M, Horiguchi S, Itoh A, Funata N, Schreiber SL, Yoshida M, Toi M (2005). Significance of HDAC6 regulation via estrogen signaling for cell motility and prognosis in estrogen receptor-positive breast cancer. Oncogene 24(28):4531-9. [PubMed]

Haggarty SJ, Koeller KM, Wong JC, Butcher RA, Schreiber SL (2003). Multidimensional chemical genetic analysis of diversity-oriented synthesis-derived deacetylase inhibitors using cell-based assays. Chem Biol 10(5):383-96. [PubMed]

Haggarty SJ, Koeller KM, Wong JC, Grozinger CM, Schreiber SL (2003). Domain-selective small-molecule inhibitor of histone deacetylase 6 (HDAC6)-mediated tubulin deacetylation. Proc Natl Acad Sci USA 100(8):4389-94. [PubMed]

Wong JC, Hong R, Schreiber SL (2003). Structural biasing elements for in-cell histone deacetylase paralog selectivity. J Am Chem Soc 125(19):5586-7. [PubMed]

Ubistatin

Verma R, Peters NR, D'Onofrio M, Tochtrop GP, Sakamoto KM, Varadan R, Zhang M, Coffino P, Fushman D, Deshaies RJ, King RW (2004). Ubistatins inhibit proteasome-dependent degradation by binding the ubiquitin chain. Science 306(5693):117-20. [PubMed]

Wiskostatin

Haller C, Rauch S, Michel N, Hannemann S, Lehmann MJ, Keppler OT, Fackler OT (2006). The HIV-1 pathogenicity factor Nef interferes with maturation of stimulatory T-lymphocyte contacts by modulation of N-Wasp activity. J Biol Chem 281(28):19618-30. [PubMed]

Kovacs EM, Makar RS, Gertler FB (2006). Tuba stimulates intracellular N-WASP-dependent actin assembly. J Cell Sci 119(Pt 13):2715-26. [PubMed]

Leung DW, Morgan DM, Rosen MK (2006). Biochemical properties and inhibitors of (N-)WASP. Methods Enzymol 406:281-96. [PubMed]

Robert A, Smadja-Lamere N, Landry MC, Champagne C, Petrie R, Lamarche-Vane N, Hosoya H, Lavoie JN (2006). Adenovirus E4orf4 hijacks rho GTPase-dependent actin dynamics to kill cells: a role for endosome-associated actin assembly. Mol Biol Cell 17(7):3329-44. [PubMed]

Schroder A, Schroder B, Roppenser B, Linder S, Sinha B, Fassler R, Aepfelbacher M (2006). Staphylococcus aureus Fibronectin Binding Protein-A Induces Motile Attachment Sites and Complex Actin Remodeling in Living Endothelial Cells. Mol Biol Cell. (Epub ahead of print) [PubMed]

Ivanov AI, Hunt D, Utech M, Nusrat A, Parkos CA (2005). Differential roles for actin polymerization and a myosin II motor in assembly of the epithelial apical junctional complex. Mol Biol Cell 16(6):2636-50. [PubMed]

Peterson JR, Bickford LC, Morgan D, Kim AS, Ouerfelli O, Kirschner MW, Rosen MK (2004). Chemical inhibition of N-WASP by stabilization of a native autoinhibited conformation. Nat Struct Mol Biol 11(8):747-55. [PubMed]

Vacuolin-1

Huynh C, Andrews NW (2005). The small chemical vacuolin-1 alters the morphology of lysosomes without inhibiting Ca2+-regulated exocytosis. EMBO Rep 6(9):843-7. [PubMed]

Cerny J, Feng Y, Yu A, Miyake K, Borgonovo B, Klumperman J, Meldolesi J, McNeil PL, Kirchhausen T (2004). The small chemical vacuolin-1 inhibits Ca(2+)-dependent lysosomal exocytosis but not cell resealing. EMBO Rep 5(9):883-8. [PubMed]

Virstatin

Hung DT, Shakhnovich EA, Pierson E, Mekalanos JJ (2005). Small-molecule inhibitor of Vibrio cholerae virulence and intestinal colonization. Science 310(5748):670-4. [PubMed]

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