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Items: 44


Ligand-mediated protein degradation reveals functional conservation among sequence variants of the CUL4-type E3 ligase substrate receptor cereblon.

Akuffo AA, Alontaga AY, Metcalf R, Beatty MS, Becker A, McDaniel JM, Hesterberg RS, Goodheart WE, Gunawan S, Ayaz M, Yang Y, Karim MR, Orobello ME, Daniel K, Guida W, Yoder JA, Rajadhyaksha AM, Schonbrunn E, Lawrence HR, Lawrence NJ, Epling-Burnette PK.

J Biol Chem. 2018 Feb 15. pii: jbc.M117.816868. doi: 10.1074/jbc.M117.816868. [Epub ahead of print]


Blockade of ACK1/TNK2 To Squelch the Survival of Prostate Cancer Stem-like Cells.

Mahajan NP, Coppola D, Kim J, Lawrence HR, Lawrence NJ, Mahajan K.

Sci Rep. 2018 Jan 31;8(1):1954. doi: 10.1038/s41598-018-20172-z.


Dabrafenib inhibits the growth of BRAF-WT cancers through CDK16 and NEK9 inhibition.

Phadke M, Remsing Rix LL, Smalley I, Bryant AT, Luo Y, Lawrence HR, Schaible BJ, Chen YA, Rix U, Smalley KSM.

Mol Oncol. 2018 Jan;12(1):74-88. doi: 10.1002/1878-0261.12152. Epub 2017 Nov 23.


ACK1/TNK2 Regulates Histone H4 Tyr88-phosphorylation and AR Gene Expression in Castration-Resistant Prostate Cancer.

Mahajan K, Malla P, Lawrence HR, Chen Z, Kumar-Sinha C, Malik R, Shukla S, Kim J, Coppola D, Lawrence NJ, Mahajan NP.

Cancer Cell. 2017 Jun 12;31(6):790-803.e8. doi: 10.1016/j.ccell.2017.05.003.


Dual Targeting of WEE1 and PLK1 by AZD1775 Elicits Single Agent Cellular Anticancer Activity.

Wright G, Golubeva V, Remsing Rix LL, Berndt N, Luo Y, Ward GA, Gray JE, Schonbrunn E, Lawrence HR, Monteiro ANA, Rix U.

ACS Chem Biol. 2017 Jul 21;12(7):1883-1892. doi: 10.1021/acschembio.7b00147. Epub 2017 Jun 7.


Potent Dual BET Bromodomain-Kinase Inhibitors as Value-Added Multitargeted Chemical Probes and Cancer Therapeutics.

Ember SW, Lambert QT, Berndt N, Gunawan S, Ayaz M, Tauro M, Zhu JY, Cranfill PJ, Greninger P, Lynch CC, Benes CH, Lawrence HR, Reuther GW, Lawrence NJ, Schönbrunn E.

Mol Cancer Ther. 2017 Jun;16(6):1054-1067. doi: 10.1158/1535-7163.MCT-16-0568-T. Epub 2017 Mar 23.


Targeting Aurora kinase A and JAK2 prevents GVHD while maintaining Treg and antitumor CTL function.

Betts BC, Veerapathran A, Pidala J, Yang H, Horna P, Walton K, Cubitt CL, Gunawan S, Lawrence HR, Lawrence NJ, Sebti SM, Anasetti C.

Sci Transl Med. 2017 Jan 11;9(372). pii: eaai8269. doi: 10.1126/scitranslmed.aai8269.


Proteome-wide Profiling of Clinical PARP Inhibitors Reveals Compound-Specific Secondary Targets.

Knezevic CE, Wright G, Rix LLR, Kim W, Kuenzi BM, Luo Y, Watters JM, Koomen JM, Haura EB, Monteiro AN, Radu C, Lawrence HR, Rix U.

Cell Chem Biol. 2016 Dec 22;23(12):1490-1503. doi: 10.1016/j.chembiol.2016.10.011. Epub 2016 Nov 17.


Behavioral Couples Treatment for Substance Use Disorder: Secondary Effects on the Reduction of Risk for Child Abuse.

Kelley ML, Bravo AJ, Braitman AL, Lawless AK, Lawrence HR.

J Subst Abuse Treat. 2016 Mar;62:10-9. doi: 10.1016/j.jsat.2015.11.008. Epub 2015 Dec 2.


Inhibition of Shp2 suppresses mutant EGFR-induced lung tumors in transgenic mouse model of lung adenocarcinoma.

Schneeberger VE, Ren Y, Luetteke N, Huang Q, Chen L, Lawrence HR, Lawrence NJ, Haura EB, Koomen JM, Coppola D, Wu J.

Oncotarget. 2015 Mar 20;6(8):6191-202.


Modeling risk for child abuse and harsh parenting in families with depressed and substance-abusing parents.

Kelley ML, Lawrence HR, Milletich RJ, Hollis BF, Henson JM.

Child Abuse Negl. 2015 May;43:42-52. doi: 10.1016/j.chiabu.2015.01.017. Epub 2015 Feb 25.


Development of novel ACK1/TNK2 inhibitors using a fragment-based approach.

Lawrence HR, Mahajan K, Luo Y, Zhang D, Tindall N, Huseyin M, Gevariya H, Kazi S, Ozcan S, Mahajan NP, Lawrence NJ.

J Med Chem. 2015 Mar 26;58(6):2746-63. doi: 10.1021/jm501929n. Epub 2015 Mar 17.


CD4+ T cell STAT3 phosphorylation precedes acute GVHD, and subsequent Th17 tissue invasion correlates with GVHD severity and therapeutic response.

Betts BC, Sagatys EM, Veerapathran A, Lloyd MC, Beato F, Lawrence HR, Yue B, Kim J, Sebti SM, Anasetti C, Pidala J.

J Leukoc Biol. 2015 Apr;97(4):807-19. doi: 10.1189/jlb.5A1114-532RR. Epub 2015 Feb 6.


ACK1 tyrosine kinase interacts with histone demethylase KDM3A to regulate the mammary tumor oncogene HOXA1.

Mahajan K, Lawrence HR, Lawrence NJ, Mahajan NP.

J Biol Chem. 2014 Oct 10;289(41):28179-91. doi: 10.1074/jbc.M114.584425. Epub 2014 Aug 22.


Dual Aurora A and JAK2 kinase blockade effectively suppresses malignant transformation.

Yang H, Lawrence HR, Kazi A, Gevariya H, Patel R, Luo Y, Rix U, Schonbrunn E, Lawrence NJ, Sebti SM.

Oncotarget. 2014 May 30;5(10):2947-61.


Discovery of PI-1840, a novel noncovalent and rapidly reversible proteasome inhibitor with anti-tumor activity.

Kazi A, Ozcan S, Tecleab A, Sun Y, Lawrence HR, Sebti SM.

J Biol Chem. 2014 Apr 25;289(17):11906-15. doi: 10.1074/jbc.M113.533950. Epub 2014 Feb 25.


GSK3 alpha and beta are new functionally relevant targets of tivantinib in lung cancer cells.

Remsing Rix LL, Kuenzi BM, Luo Y, Remily-Wood E, Kinose F, Wright G, Li J, Koomen JM, Haura EB, Lawrence HR, Rix U.

ACS Chem Biol. 2014 Feb 21;9(2):353-8. doi: 10.1021/cb400660a. Epub 2013 Nov 20.


Lysophosphatidic acid acyltransferase beta regulates mTOR signaling.

Blaskovich MA, Yendluri V, Lawrence HR, Lawrence NJ, Sebti SM, Springett GM.

PLoS One. 2013 Oct 31;8(10):e78632. doi: 10.1371/journal.pone.0078632. eCollection 2013.


Development of new N-Arylbenzamides as STAT3 Dimerization Inhibitors.

Urlam MK, Pireddu R, Ge Y, Zhang X, Sun Y, Lawrence HR, Guida WC, Sebti SM, Lawrence NJ.

Medchemcomm. 2013 Jun;4(6):932-941.


Oxadiazole-isopropylamides as potent and noncovalent proteasome inhibitors.

Ozcan S, Kazi A, Marsilio F, Fang B, Guida WC, Koomen J, Lawrence HR, Sebti SM.

J Med Chem. 2013 May 23;56(10):3783-805. doi: 10.1021/jm400221d. Epub 2013 May 13.


A novel inhibitor of STAT3 homodimerization selectively suppresses STAT3 activity and malignant transformation.

Zhang X, Sun Y, Pireddu R, Yang H, Urlam MK, Lawrence HR, Guida WC, Lawrence NJ, Sebti SM.

Cancer Res. 2013 Mar 15;73(6):1922-33. doi: 10.1158/0008-5472.CAN-12-3175. Epub 2013 Jan 15.


Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors.

Lawrence HR, Martin MP, Luo Y, Pireddu R, Yang H, Gevariya H, Ozcan S, Zhu JY, Kendig R, Rodriguez M, Elias R, Cheng JQ, Sebti SM, Schonbrunn E, Lawrence NJ.

J Med Chem. 2012 Sep 13;55(17):7392-7416. doi: 10.1021/jm300334d. Epub 2012 Aug 30.


Ack1-mediated androgen receptor phosphorylation modulates radiation resistance in castration-resistant prostate cancer.

Mahajan K, Coppola D, Rawal B, Chen YA, Lawrence HR, Engelman RW, Lawrence NJ, Mahajan NP.

J Biol Chem. 2012 Jun 22;287(26):22112-22. doi: 10.1074/jbc.M112.357384. Epub 2012 May 7.


Ack1 tyrosine kinase activation correlates with pancreatic cancer progression.

Mahajan K, Coppola D, Chen YA, Zhu W, Lawrence HR, Lawrence NJ, Mahajan NP.

Am J Pathol. 2012 Apr;180(4):1386-93. doi: 10.1016/j.ajpath.2011.12.028. Epub 2012 Feb 7.


Enhanced anti-melanoma efficacy of interferon alfa-2b via inhibition of Shp2.

Win-Piazza H, Schneeberger VE, Chen L, Pernazza D, Lawrence HR, Sebti SM, Lawrence NJ, Wu J.

Cancer Lett. 2012 Jul 1;320(1):81-5. doi: 10.1016/j.canlet.2012.01.034. Epub 2012 Feb 1.


A novel mechanism by which small molecule inhibitors induce the DFG flip in Aurora A.

Martin MP, Zhu JY, Lawrence HR, Pireddu R, Luo Y, Alam R, Ozcan S, Sebti SM, Lawrence NJ, Schönbrunn E.

ACS Chem Biol. 2012 Apr 20;7(4):698-706. doi: 10.1021/cb200508b. Epub 2012 Jan 27.


Discovery and synthesis of hydronaphthoquinones as novel proteasome inhibitors.

Ge Y, Kazi A, Marsilio F, Luo Y, Jain S, Brooks W, Daniel KG, Guida WC, Sebti SM, Lawrence HR.

J Med Chem. 2012 Mar 8;55(5):1978-98. doi: 10.1021/jm201118h. Epub 2012 Feb 14.


Critical role of IRF-8 in negative regulation of TLR3 expression by Src homology 2 domain-containing protein tyrosine phosphatase-2 activity in human myeloid dendritic cells.

Fragale A, Stellacci E, Ilari R, Remoli AL, Lanciotti A, Perrotti E, Shytaj I, Orsatti R, Lawrence HR, Lawrence NJ, Wu J, Rehli M, Ozato K, Battistini A.

J Immunol. 2011 Feb 15;186(4):1951-62. doi: 10.4049/jimmunol.1000918. Epub 2011 Jan 10.


Shp2 protein tyrosine phosphatase inhibitor activity of estramustine phosphate and its triterpenoid analogs.

Scott LM, Chen L, Daniel KG, Brooks WH, Guida WC, Lawrence HR, Sebti SM, Lawrence NJ, Wu J.

Bioorg Med Chem Lett. 2011 Jan 15;21(2):730-3. doi: 10.1016/j.bmcl.2010.11.117. Epub 2010 Dec 4.


Synthesis and biological evaluation of naphthoquinone analogs as a novel class of proteasome inhibitors.

Lawrence HR, Kazi A, Luo Y, Kendig R, Ge Y, Jain S, Daniel K, Santiago D, Guida WC, Sebti SM.

Bioorg Med Chem. 2010 Aug 1;18(15):5576-92. doi: 10.1016/j.bmc.2010.06.038. Epub 2010 Jun 18.


Inhibition of cellular Shp2 activity by a methyl ester analog of SPI-112.

Chen L, Pernazza D, Scott LM, Lawrence HR, Ren Y, Luo Y, Wu X, Sung SS, Guida WC, Sebti SM, Lawrence NJ, Wu J.

Biochem Pharmacol. 2010 Sep 15;80(6):801-10. doi: 10.1016/j.bcp.2010.05.019. Epub 2010 May 25.


Targeting protein tyrosine phosphatases for anticancer drug discovery.

Scott LM, Lawrence HR, Sebti SM, Lawrence NJ, Wu J.

Curr Pharm Des. 2010 Jun;16(16):1843-62. Review.


Identification of a disruptor of the MDM2-p53 protein-protein interaction facilitated by high-throughput in silico docking.

Lawrence HR, Li Z, Yip ML, Sung SS, Lawrence NJ, McLaughlin ML, McManus GJ, Zaworotko MJ, Sebti SM, Chen J, Guida WC.

Bioorg Med Chem Lett. 2009 Jul 15;19(14):3756-9. doi: 10.1016/j.bmcl.2009.04.124. Epub 2009 May 3.


Inhibitors of Src homology-2 domain containing protein tyrosine phosphatase-2 (Shp2) based on oxindole scaffolds.

Lawrence HR, Pireddu R, Chen L, Luo Y, Sung SS, Szymanski AM, Yip ML, Guida WC, Sebti SM, Wu J, Lawrence NJ.

J Med Chem. 2008 Aug 28;51(16):4948-56. doi: 10.1021/jm8002526. Epub 2008 Aug 5.


Novel inhibitors of 17beta-hydroxysteroid dehydrogenase type 1: templates for design.

Allan GM, Vicker N, Lawrence HR, Tutill HJ, Day JM, Huchet M, Ferrandis E, Reed MJ, Purohit A, Potter BV.

Bioorg Med Chem. 2008 Apr 15;16(8):4438-56. doi: 10.1016/j.bmc.2008.02.059. Epub 2008 Mar 7.


17beta-hydroxysteroid dehydrogenase Type 1, and not Type 12, is a target for endocrine therapy of hormone-dependent breast cancer.

Day JM, Foster PA, Tutill HJ, Parsons MF, Newman SP, Chander SK, Allan GM, Lawrence HR, Vicker N, Potter BV, Reed MJ, Purohit A.

Int J Cancer. 2008 May 1;122(9):1931-40. doi: 10.1002/ijc.23350.


Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity.

Siddiquee K, Zhang S, Guida WC, Blaskovich MA, Greedy B, Lawrence HR, Yip ML, Jove R, McLaughlin MM, Lawrence NJ, Sebti SM, Turkson J.

Proc Natl Acad Sci U S A. 2007 May 1;104(18):7391-6. Epub 2007 Apr 26.


Focused libraries of 16-substituted estrone derivatives and modified e-ring steroids: inhibitors of 17beta-hydroxysteroid dehydrogenase type 1.

Vicker N, Lawrence HR, Allan GM, Bubert C, Smith A, Tutill HJ, Purohit A, Day JM, Mahon MF, Reed MJ, Potter BV.

ChemMedChem. 2006 Apr;1(4):464-81.


Discovery of a novel shp2 protein tyrosine phosphatase inhibitor.

Chen L, Sung SS, Yip ML, Lawrence HR, Ren Y, Guida WC, Sebti SM, Lawrence NJ, Wu J.

Mol Pharmacol. 2006 Aug;70(2):562-70. Epub 2006 May 22.


17Beta-hydroxysteroid dehydrogenase Type 1 and Type 2: association between mRNA expression and activity in cell lines.

Day JM, Tutill HJ, Newman SP, Purohit A, Lawrence HR, Vicker N, Potter BV, Reed MJ.

Mol Cell Endocrinol. 2006 Mar 27;248(1-2):246-9. Epub 2006 Feb 21.


Modification of estrone at the 6, 16, and 17 positions: novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1.

Allan GM, Lawrence HR, Cornet J, Bubert C, Fischer DS, Vicker N, Smith A, Tutill HJ, Purohit A, Day JM, Mahon MF, Reed MJ, Potter BV.

J Med Chem. 2006 Feb 23;49(4):1325-45.


The regulation and inhibition of 17beta-hydroxysteroid dehydrogenase in breast cancer.

Purohit A, Tutill HJ, Day JM, Chander SK, Lawrence HR, Allan GM, Fischer DS, Vicker N, Newman SP, Potter BV, Reed MJ.

Mol Cell Endocrinol. 2006 Mar 27;248(1-2):199-203. Epub 2006 Jan 18.


Novel and potent 17beta-hydroxysteroid dehydrogenase type 1 inhibitors.

Lawrence HR, Vicker N, Allan GM, Smith A, Mahon MF, Tutill HJ, Purohit A, Reed MJ, Potter BV.

J Med Chem. 2005 Apr 21;48(8):2759-62.


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