Shiva Malek, Ph.D. - Publications

Affiliations: 
2000 University of California, San Diego, La Jolla, CA 
Area:
transcription, signaling, pre-mRNA splicing, mRNA transport, protein-protein, protein-DNA and protein-RNA interactions

41 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2016 Purkey HE, Robarge K, Chen J, Chen Z, Corson LB, Ding CZ, DiPasquale AG, Dragovich PS, Eigenbrot C, Evangelista M, Fauber BP, Gao Z, Ge H, Hitz A, Ho Q, ... ... Malek S, et al. Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice. Acs Medicinal Chemistry Letters. 7: 896-901. PMID 27774125 DOI: 10.1021/acsmedchemlett.6b00190  1
2016 Chan BK, Hanan EJ, Bowman K, Bryan MC, Burdick DJ, Chan EW, Chen Y, Clausen S, Dela Vega T, Dotson J, Eigenbrot C, Elliott RL, Heald RA, Jackson PS, Knight JD, ... ... Malek S, et al. Discovery of a Non-Covalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor. Journal of Medicinal Chemistry. PMID 27564586 DOI: 10.1021/acs.jmedchem.6b00995  1
2016 Boudreau A, Purkey HE, Hitz A, Robarge K, Peterson D, Labadie S, Kwong M, Hong R, Gao M, Del Nagro C, Pusapati R, Ma S, Salphati L, Pang J, Zhou A, ... ... Malek S, et al. Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition. Nature Chemical Biology. PMID 27479743 DOI: 10.1038/nchembio.2143  1
2016 Foster SA, Whalen DM, Özen A, Wongchenko MJ, Yin J, Yen I, Schaefer G, Mayfield JD, Chmielecki J, Stephens PJ, Albacker LA, Yan Y, Song K, Hatzivassiliou G, Eigenbrot C, ... ... Malek S, et al. Activation Mechanism of Oncogenic Deletion Mutations in BRAF, EGFR, and HER2. Cancer Cell. PMID 26996308 DOI: 10.1016/j.ccell.2016.02.010  1
2016 Heald R, Bowman KK, Bryan MC, Burdick D, Chan B, Chan E, Chen Y, Clausen S, Dominguez-Fernandez B, Eigenbrot C, Elliott R, Hanan EJ, Jackson P, Knight J, La H, ... ... Malek S, et al. Correction to Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study. Journal of Medicinal Chemistry. PMID 26967667 DOI: 10.1021/acs.jmedchem.6b00301  0.6
2016 Bryan MC, Burdick DJ, Chan BK, Chen Y, Clausen S, Dotson J, Eigenbrot C, Elliott R, Hanan EJ, Heald R, Jackson P, La H, Lainchbury M, Malek S, Mann SE, et al. Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR. Acs Medicinal Chemistry Letters. 7: 100-4. PMID 26819674 DOI: 10.1021/acsmedchemlett.5b00428  1
2015 Hanan EJ, Baumgardner M, Bryan MC, Chen Y, Eigenbrot C, Fan P, Gu XH, La H, Malek S, Purkey HE, Schaefer G, Schmidt S, Sideris S, Yen I, Yu C, et al. 4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase. Bioorganic & Medicinal Chemistry Letters. PMID 26639762 DOI: 10.1016/j.bmcl.2015.11.078  1
2015 Heald RA, Chan BK, Bryan 2C, Eigenbrot C, Yu C, Burdick D, Hanan EJ, Chan E, Schaefer G, La H, Purkey H, Knight J, Yen I, Jackson P, Bowman K, ... ... Malek S, et al. Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case History. Journal of Medicinal Chemistry. PMID 26455919 DOI: 10.1021/acs.jmedchem.5b01412  1
2015 Gazzard L, Williams K, Chen H, Axford L, Blackwood E, Burton B, Chapman K, Crackett P, Drobnick J, Ellwood C, Epler J, Flagella M, Gancia E, Gill M, Goodacre S, ... ... Malek S, et al. Mitigation of Acetylcholine Esterase Activity in the 1,7-Diazacarbazole Series of Inhibitors of Checkpoint Kinase 1. Journal of Medicinal Chemistry. 58: 5053-74. PMID 25988399 DOI: 10.1021/acs.jmedchem.5b00464  1
2015 Labadie S, Dragovich PS, Chen J, Fauber BP, Boggs J, Corson LB, Ding CZ, Eigenbrot C, Ge H, Ho Q, Lai KW, Ma S, Malek S, Peterson D, Purkey HE, et al. Optimization of 5-(2,6-dichlorophenyl)-3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase. Bioorganic & Medicinal Chemistry Letters. 25: 75-82. PMID 25466195 DOI: 10.1016/j.bmcl.2014.11.008  1
2014 Fauber BP, Dragovich PS, Chen J, Corson LB, Ding CZ, Eigenbrot C, Labadie S, Malek S, Peterson D, Purkey HE, Robarge K, Sideris S, Ultsch M, Wei B, Yen I, et al. Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase. Bioorganic & Medicinal Chemistry Letters. 24: 5683-7. PMID 25467161 DOI: 10.1016/j.bmcl.2014.10.067  1
2014 Gazzard L, Appleton B, Chapman K, Chen H, Clark K, Drobnick J, Goodacre S, Halladay J, Lyssikatos J, Schmidt S, Sideris S, Wiesmann C, Williams K, Wu P, Yen I, ... Malek S, et al. Discovery of the 1,7-diazacarbazole class of inhibitors of checkpoint kinase 1. Bioorganic & Medicinal Chemistry Letters. 24: 5704-9. PMID 25453805 DOI: 10.1016/j.bmcl.2014.10.063  1
2014 Hanan EJ, Eigenbrot C, Bryan MC, Burdick DJ, Chan BK, Chen Y, Dotson J, Heald RA, Jackson PS, La H, Lainchbury MD, Malek S, Purkey HE, Schaefer G, Schmidt S, et al. Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation. Journal of Medicinal Chemistry. 57: 10176-91. PMID 25383627 DOI: 10.1021/jm501578n  1
2014 Haling JR, Sudhamsu J, Yen I, Sideris S, Sandoval W, Phung W, Bravo BJ, Giannetti AM, Peck A, Masselot A, Morales T, Smith D, Brandhuber BJ, Hymowitz SG, Malek S. Structure of the BRAF-MEK complex reveals a kinase activity independent role for BRAF in MAPK signaling. Cancer Cell. 26: 402-13. PMID 25155755 DOI: 10.1016/j.ccr.2014.07.007  1
2014 Dragovich PS, Fauber BP, Boggs J, Chen J, Corson LB, Ding CZ, Eigenbrot C, Ge H, Giannetti AM, Hunsaker T, Labadie S, Li C, Liu Y, Liu Y, Ma S, ... Malek S, et al. Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase. Bioorganic & Medicinal Chemistry Letters. 24: 3764-71. PMID 25037916 DOI: 10.1016/j.bmcl.2014.06.076  1
2014 Cao F, Townsend EC, Karatas H, Xu J, Li L, Lee S, Liu L, Chen Y, Ouillette P, Zhu J, Hess JL, Atadja P, Lei M, Qin ZS, Malek S, et al. Targeting MLL1 H3K4 methyltransferase activity in mixed-lineage leukemia. Molecular Cell. 53: 247-61. PMID 24389101 DOI: 10.1016/j.molcel.2013.12.001  0.6
2013 Pei Z, Blackwood E, Liu L, Malek S, Belvin M, Koehler MF, Ortwine DF, Chen H, Cohen F, Kenny JR, Bergeron P, Lau K, Ly C, Zhao X, Estrada AA, et al. Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349. Acs Medicinal Chemistry Letters. 4: 103-7. PMID 24900569 DOI: 10.1021/ml3003132  1
2013 Xiao Y, Ramiscal J, Kowanetz K, Del Nagro C, Malek S, Evangelista M, Blackwood E, Jackson PK, O'Brien T. Identification of preferred chemotherapeutics for combining with a CHK1 inhibitor. Molecular Cancer Therapeutics. 12: 2285-95. PMID 24038068 DOI: 10.1158/1535-7163.MCT-13-0404  1
2013 Fauber BP, Dragovich PS, Chen J, Corson LB, Ding CZ, Eigenbrot C, Giannetti AM, Hunsaker T, Labadie S, Liu Y, Liu Y, Malek S, Peterson D, Pitts K, Sideris S, et al. Identification of 2-amino-5-aryl-pyrazines as inhibitors of human lactate dehydrogenase. Bioorganic & Medicinal Chemistry Letters. 23: 5533-9. PMID 24012183 DOI: 10.1016/j.bmcl.2013.08.060  1
2013 Hatzivassiliou G, Haling JR, Chen H, Song K, Price S, Heald R, Hewitt JF, Zak M, Peck A, Orr C, Merchant M, Hoeflich KP, Chan J, Luoh SM, Anderson DJ, ... ... Malek S, et al. Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers. Nature. 501: 232-6. PMID 23934108 DOI: 10.1038/nature12441  1
2013 Lee W, Ortwine DF, Bergeron P, Lau K, Lin L, Malek S, Nonomiya J, Pei Z, Robarge KD, Schmidt S, Sideris S, Lyssikatos JP. A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors. Bioorganic & Medicinal Chemistry Letters. 23: 5097-104. PMID 23932790 DOI: 10.1016/j.bmcl.2013.07.027  1
2013 Blackwood E, Epler J, Yen I, Flagella M, O'Brien T, Evangelista M, Schmidt S, Xiao Y, Choi J, Kowanetz K, Ramiscal J, Wong K, Jakubiak D, Yee S, Cain G, ... ... Malek S, et al. Combination drug scheduling defines a "window of opportunity" for chemopotentiation of gemcitabine by an orally bioavailable, selective ChK1 inhibitor, GNE-900. Molecular Cancer Therapeutics. 12: 1968-80. PMID 23873850 DOI: 10.1158/1535-7163.MCT-12-1218  1
2013 Dragovich PS, Fauber BP, Corson LB, Ding CZ, Eigenbrot C, Ge H, Giannetti AM, Hunsaker T, Labadie S, Liu Y, Malek S, Pan B, Peterson D, Pitts K, Purkey HE, et al. Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase. Bioorganic & Medicinal Chemistry Letters. 23: 3186-94. PMID 23628333 DOI: 10.1016/j.bmcl.2013.04.001  1
2013 Estrada AA, Shore DG, Blackwood E, Chen YH, Deshmukh G, Ding X, Dipasquale AG, Epler JA, Friedman LS, Koehler MF, Liu L, Malek S, Nonomiya J, Ortwine DF, Pei Z, et al. Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR). Journal of Medicinal Chemistry. 56: 3090-101. PMID 23473235 DOI: 10.1021/jm400194n  1
2013 Lee HJ, Schaefer G, Heffron TP, Shao L, Ye X, Sideris S, Malek S, Chan E, Merchant M, La H, Ubhayakar S, Yauch RL, Pirazzoli V, Politi K, Settleman J. Noncovalent wild-type-sparing inhibitors of EGFR T790M. Cancer Discovery. 3: 168-81. PMID 23229345 DOI: 10.1158/2159-8290.CD-12-0357  1
2012 Koehler MF, Bergeron P, Blackwood E, Bowman KK, Chen YH, Deshmukh G, Ding X, Epler J, Lau K, Lee L, Liu L, Ly C, Malek S, Nonomiya J, Oeh J, et al. Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity. Journal of Medicinal Chemistry. 55: 10958-71. PMID 23199076 DOI: 10.1021/jm301389h  1
2012 Bussenius J, Blazey CM, Aay N, Anand NK, Arcalas A, Baik T, Bowles OJ, Buhr CA, Costanzo S, Curtis JK, DeFina SC, Dubenko L, Heuer TS, Huang P, Jaeger C, ... ... Malek S, et al. Discovery of XL888: a novel tropane-derived small molecule inhibitor of HSP90. Bioorganic & Medicinal Chemistry Letters. 22: 5396-404. PMID 22877636 DOI: 10.1016/j.bmcl.2012.07.052  1
2012 Maurer T, Garrenton LS, Oh A, Pitts K, Anderson DJ, Skelton NJ, Fauber BP, Pan B, Malek S, Stokoe D, Ludlam MJ, Bowman KK, Wu J, Giannetti AM, Starovasnik MA, et al. Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity. Proceedings of the National Academy of Sciences of the United States of America. 109: 5299-304. PMID 22431598 DOI: 10.1073/pnas.1116510109  1
2011 Cohen F, Bergeron P, Blackwood E, Bowman KK, Chen H, Dipasquale AG, Epler JA, Koehler MF, Lau K, Lewis C, Liu L, Ly CQ, Malek S, Nonomiya J, Ortwine DF, et al. Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine. Journal of Medicinal Chemistry. 54: 3426-35. PMID 21495671 DOI: 10.1021/jm200215y  1
2010 Ramaswamy S, Yen I, Sideris S, Malek S, Heise CE. A plate-based assay to measure cellular ERK substrate phosphorylation: utility for drug discovery of the MAPK-signaling cascade. Assay and Drug Development Technologies. 8: 497-503. PMID 20482377 DOI: 10.1089/adt.2009.0259  1
2010 Hatzivassiliou G, Song K, Yen I, Brandhuber BJ, Anderson DJ, Alvarado R, Ludlam MJ, Stokoe D, Gloor SL, Vigers G, Morales T, Aliagas I, Liu B, Sideris S, Hoeflich KP, ... ... Malek S, et al. RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth. Nature. 464: 431-5. PMID 20130576 DOI: 10.1038/nature08833  1
2003 Malek S, Huang DB, Huxford T, Ghosh S, Ghosh G. X-ray crystal structure of an IkappaBbeta x NF-kappaB p65 homodimer complex. The Journal of Biological Chemistry. 278: 23094-100. PMID 12686541 DOI: 10.1074/jbc.M301022200  1
2001 Malek S, Chen Y, Huxford T, Ghosh G. IkappaBbeta, but not IkappaBalpha, functions as a classical cytoplasmic inhibitor of NF-kappaB dimers by masking both NF-kappaB nuclear localization sequences in resting cells. The Journal of Biological Chemistry. 276: 45225-35. PMID 11571291 DOI: 10.1074/jbc.M105865200  1
2000 Huxford T, Malek S, Ghosh G. Preparation and crystallization of dynamic NF-kappa B.Ikappa B complexes. The Journal of Biological Chemistry. 275: 32800-6. PMID 10906335 DOI: 10.1074/jbc.M006037200  1
2000 Phelps CB, Sengchanthalangsy LL, Malek S, Ghosh G. Mechanism of kappa B DNA binding by Rel/NF-kappa B dimers. The Journal of Biological Chemistry. 275: 24392-9. PMID 10825175 DOI: 10.1074/jbc.M003784200  1
1999 Huxford T, Malek S, Ghosh G. Structure and mechanism in NF-kappa B/I kappa B signaling. Cold Spring Harbor Symposia On Quantitative Biology. 64: 533-40. PMID 11232330  1
1998 Huxford T, Huang DB, Malek S, Ghosh G. The crystal structure of the IkappaBalpha/NF-kappaB complex reveals mechanisms of NF-kappaB inactivation. Cell. 95: 759-70. PMID 9865694 DOI: 10.1016/S0092-8674(00)81699-2  1
1998 Malek S, Huxford T, Ghosh G. Ikappa Balpha functions through direct contacts with the nuclear localization signals and the DNA binding sequences of NF-kappaB. The Journal of Biological Chemistry. 273: 25427-35. PMID 9738011 DOI: 10.1074/jbc.273.39.25427  1
1994 Ali S, Malek S, Hossain Z. Purification and characterization of a thermostable glucoamylase from a Myrothecium isolate Journal of Applied Bacteriology. 76: 210-215.  1
1992 Wang E, Malek S, Feigon J. Structure of a G.T.A triplet in an intramolecular DNA triplex. Biochemistry. 31: 4838-46. PMID 1591244  1
1991 Macaya RF, Gilbert DE, Malek S, Sinsheimer JS, Feigon J. Structure and stability of X.G.C mismatches in the third strand of intramolecular triplexes. Science (New York, N.Y.). 254: 270-4. PMID 1925581  1
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