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Items: 24

1.

Correction to "Discovery of Irreversible Inhibitors Targeting Histone Methyltransferase, SMYD3".

Huang C, Liew SS, Lin GR, Poulsen A, Ang MJY, Chia BCS, Chew SY, Kwek ZP, Wee JLK, Ong EH, Retna P, Baburajendran N, Li R, Yu W, Koh-Stenta X, Ngo A, Manesh S, Fulwood J, Ke Z, Chung HH, Sepramaniam S, Chew XH, Dinie N, Lee MA, Chew YS, Low CB, Pendharkar V, Manoharan V, Vuddagiri S, Sangthongpitag K, Joy J, Matter A, Hill J, Keller TH, Foo K.

ACS Med Chem Lett. 2019 Jul 9;10(8):1240. doi: 10.1021/acsmedchemlett.9b00278. eCollection 2019 Aug 8.

2.

Discovery of Irreversible Inhibitors Targeting Histone Methyltransferase, SMYD3.

Huang C, Liew SS, Lin GR, Poulsen A, Ang MJY, Chia BCS, Chew SY, Kwek ZP, Wee JLK, Ong EH, Retna P, Baburajendran N, Li R, Yu W, Koh-Stenta X, Ngo A, Manesh S, Fulwood J, Ke Z, Chung HH, Sepramaniam S, Chew XH, Dinie N, Lee MA, Chew YS, Low CB, Pendharkar V, Manoharan V, Vuddagiri S, Sangthongpitag K, Joy J, Matter A, Hill J, Keller TH, Foo K.

ACS Med Chem Lett. 2019 May 23;10(6):978-984. doi: 10.1021/acsmedchemlett.9b00170. eCollection 2019 Jun 13. Erratum in: ACS Med Chem Lett. 2019 Jul 09;10(8):1240.

PMID:
31223458
3.

Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria.

Ho SY, Wang W, Ng FM, Wong YX, Poh ZY, Tan SWE, Ang SH, Liew SS, Joyner Wong YS, Tan Y, Poulsen A, Pendharkar V, Sangthongpitag K, Manchester J, Basarab G, Hill J, Keller TH, Cherian J.

Eur J Med Chem. 2018 Sep 5;157:610-621. doi: 10.1016/j.ejmech.2018.08.025. Epub 2018 Aug 11.

PMID:
30125722
4.

Fragment-Based Drug Discovery of Potent Protein Kinase C Iota Inhibitors.

Kwiatkowski J, Liu B, Tee DHY, Chen G, Ahmad NHB, Wong YX, Poh ZY, Ang SH, Tan ESW, Ong EH, Nurul Dinie, Poulsen A, Pendharkar V, Sangthongpitag K, Lee MA, Sepramaniam S, Ho SY, Cherian J, Hill J, Keller TH, Hung AW.

J Med Chem. 2018 May 24;61(10):4386-4396. doi: 10.1021/acs.jmedchem.8b00060. Epub 2018 May 4.

PMID:
29688013
5.

Optimization of Selective Mitogen-Activated Protein Kinase Interacting Kinases 1 and 2 Inhibitors for the Treatment of Blast Crisis Leukemia.

Yang H, Chennamaneni LR, Ho MWT, Ang SH, Tan ESW, Jeyaraj DA, Yeap YS, Liu B, Ong EH, Joy JK, Wee JLK, Kwek P, Retna P, Dinie N, Nguyen TTH, Tai SJ, Manoharan V, Pendharkar V, Low CB, Chew YS, Vuddagiri S, Sangthongpitag K, Choong ML, Lee MA, Kannan S, Verma CS, Poulsen A, Lim S, Chuah C, Ong TS, Hill J, Matter A, Nacro K.

J Med Chem. 2018 May 24;61(10):4348-4369. doi: 10.1021/acs.jmedchem.7b01714. Epub 2018 May 7.

PMID:
29683667
6.

Scaffold Hopping and Optimization of Maleimide Based Porcupine Inhibitors.

Ho SY, Alam J, Jeyaraj DA, Wang W, Lin GR, Ang SH, Tan ESW, Lee MA, Ke Z, Madan B, Virshup DM, Ding LJ, Manoharan V, Chew YS, Low CB, Pendharkar V, Sangthongpitag K, Hill J, Keller TH, Poulsen A.

J Med Chem. 2017 Aug 10;60(15):6678-6692. doi: 10.1021/acs.jmedchem.7b00662. Epub 2017 Jul 20.

PMID:
28671458
7.

Towards Selective Mycobacterial ClpP1P2 Inhibitors with Reduced Activity against the Human Proteasome.

Moreira W, Santhanakrishnan S, Ngan GJY, Low CB, Sangthongpitag K, Poulsen A, Dymock BW, Dick T.

Antimicrob Agents Chemother. 2017 Apr 24;61(5). pii: e02307-16. doi: 10.1128/AAC.02307-16. Print 2017 May.

8.

p53 Maintains Genomic Stability by Preventing Interference between Transcription and Replication.

Yeo CQX, Alexander I, Lin Z, Lim S, Aning OA, Kumar R, Sangthongpitag K, Pendharkar V, Ho VHB, Cheok CF.

Cell Rep. 2016 Apr 5;15(1):132-146. doi: 10.1016/j.celrep.2016.03.011. Epub 2016 Mar 24.

9.

Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells.

Cherian J, Nacro K, Poh ZY, Guo S, Jeyaraj DA, Wong YX, Ho M, Yang HY, Joy JK, Kwek ZP, Liu B, Wee JL, Ong EH, Choong ML, Poulsen A, Lee MA, Pendharkar V, Ding LJ, Manoharan V, Chew YS, Sangthongpitag K, Lim S, Ong ST, Hill J, Keller TH.

J Med Chem. 2016 Apr 14;59(7):3063-78. doi: 10.1021/acs.jmedchem.5b01712. Epub 2016 Apr 5.

PMID:
27011159
10.

Wnt addiction of genetically defined cancers reversed by PORCN inhibition.

Madan B, Ke Z, Harmston N, Ho SY, Frois AO, Alam J, Jeyaraj DA, Pendharkar V, Ghosh K, Virshup IH, Manoharan V, Ong EH, Sangthongpitag K, Hill J, Petretto E, Keller TH, Lee MA, Matter A, Virshup DM.

Oncogene. 2016 Apr 28;35(17):2197-207. doi: 10.1038/onc.2015.280. Epub 2015 Aug 10.

11.

Discovery and Optimization of a Porcupine Inhibitor.

Duraiswamy AJ, Lee MA, Madan B, Ang SH, Tan ES, Cheong WW, Ke Z, Pendharkar V, Ding LJ, Chew YS, Manoharan V, Sangthongpitag K, Alam J, Poulsen A, Ho SY, Virshup DM, Keller TH.

J Med Chem. 2015 Aug 13;58(15):5889-99. doi: 10.1021/acs.jmedchem.5b00507. Epub 2015 Jul 16.

PMID:
26110200
12.

Feedback regulation on PTEN/AKT pathway by the ER stress kinase PERK mediated by interaction with the Vault complex.

Zhang W, Neo SP, Gunaratne J, Poulsen A, Boping L, Ong EH, Sangthongpitag K, Pendharkar V, Hill J, Cohen SM.

Cell Signal. 2015 Mar;27(3):436-42. doi: 10.1016/j.cellsig.2014.12.010. Epub 2014 Dec 19.

13.

Combination treatment for myeloproliferative neoplasms using JAK and pan-class I PI3K inhibitors.

Choong ML, Pecquet C, Pendharkar V, Diaconu CC, Yong JW, Tai SJ, Wang SF, Defour JP, Sangthongpitag K, Villeval JL, Vainchenker W, Constantinescu SN, Lee MA.

J Cell Mol Med. 2013 Nov;17(11):1397-409. doi: 10.1111/jcmm.12156. Epub 2013 Nov 19.

14.

Fragment-based ligand design of novel potent inhibitors of tankyrases.

Larsson EA, Jansson A, Ng FM, Then SW, Panicker R, Liu B, Sangthongpitag K, Pendharkar V, Tai SJ, Hill J, Dan C, Ho SY, Cheong WW, Poulsen A, Blanchard S, Lin GR, Alam J, Keller TH, Nordlund P.

J Med Chem. 2013 Jun 13;56(11):4497-508. doi: 10.1021/jm400211f. Epub 2013 Jun 4.

PMID:
23672613
15.

Identification and characterization of a small-molecule inhibitor of Wnt signaling in glioblastoma cells.

De Robertis A, Valensin S, Rossi M, Tunici P, Verani M, De Rosa A, Giordano C, Varrone M, Nencini A, Pratelli C, Benicchi T, Bakker A, Hill J, Sangthongpitag K, Pendharkar V, Liu B, Ng FM, Then SW, Jing Tai S, Cheong SM, He X, Caricasole A, Salerno M.

Mol Cancer Ther. 2013 Jul;12(7):1180-9. doi: 10.1158/1535-7163.MCT-12-1176-T. Epub 2013 Apr 25.

16.

Preclinical metabolism and disposition of SB939 (Pracinostat), an orally active histone deacetylase inhibitor, and prediction of human pharmacokinetics.

Jayaraman R, Pilla Reddy V, Pasha MK, Wang H, Sangthongpitag K, Yeo P, Hu CY, Wu X, Xin L, Goh E, New LS, Ethirajulu K.

Drug Metab Dispos. 2011 Dec;39(12):2219-32. doi: 10.1124/dmd.111.041558. Epub 2011 Aug 26.

PMID:
21873472
17.

Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.

Wang H, Yu N, Chen D, Lee KC, Lye PL, Chang JW, Deng W, Ng MC, Lu T, Khoo ML, Poulsen A, Sangthongpitag K, Wu X, Hu C, Goh KC, Wang X, Fang L, Goh KL, Khng HH, Goh SK, Yeo P, Liu X, Bonday Z, Wood JM, Dymock BW, Kantharaj E, Sun ET.

J Med Chem. 2011 Jul 14;54(13):4694-720. doi: 10.1021/jm2003552. Epub 2011 Jun 16.

PMID:
21634430
18.

Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.

Wang H, Lim ZY, Zhou Y, Ng M, Lu T, Lee K, Sangthongpitag K, Goh KC, Wang X, Wu X, Khng HH, Goh SK, Ong WC, Bonday Z, Sun ET.

Bioorg Med Chem Lett. 2010 Jun 1;20(11):3314-21. doi: 10.1016/j.bmcl.2010.04.041. Epub 2010 Apr 14.

PMID:
20451378
19.

SB939, a novel potent and orally active histone deacetylase inhibitor with high tumor exposure and efficacy in mouse models of colorectal cancer.

Novotny-Diermayr V, Sangthongpitag K, Hu CY, Wu X, Sausgruber N, Yeo P, Greicius G, Pettersson S, Liang AL, Loh YK, Bonday Z, Goh KC, Hentze H, Hart S, Wang H, Ethirajulu K, Wood JM.

Mol Cancer Ther. 2010 Mar;9(3):642-52. doi: 10.1158/1535-7163.MCT-09-0689. Epub 2010 Mar 2.

20.

N-Hydroxy-1,2-disubstituted-1H-benzimidazol-5-yl acrylamides as novel histone deacetylase inhibitors: design, synthesis, SAR studies, and in vivo antitumor activity.

Wang H, Yu N, Song H, Chen D, Zou Y, Deng W, Lye PL, Chang J, Ng M, Sun ET, Sangthongpitag K, Wang X, Wu X, Khng HH, Fang L, Goh SK, Ong WC, Bonday Z, Stünkel W, Poulsen A, Entzeroth M.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1403-8. doi: 10.1016/j.bmcl.2009.01.041. Epub 2009 Jan 19.

PMID:
19181524
21.

In vitro phase I cytochrome P450 metabolism, permeability and pharmacokinetics of SB639, a novel histone deacetylase inhibitor in preclinical species.

Venkatesh PR, Goh E, Zeng P, New LS, Xin L, Pasha MK, Sangthongpitag K, Yeo P, Kantharaj E.

Biol Pharm Bull. 2007 May;30(5):1021-4.

22.

Complete molecular scanning of the human Fas gene: mutational analysis and linkage studies in families with type I diabetes mellitus. The Danish Study Group of Diabetes in Childhood and The Danish IDDM Epidemiology and Genetics Group.

Nolsøe RL, Kristiansen OP, Sangthongpitag K, Larsen ZM, Johannesen J, Karlsen AE, Pociot F, Nerup J, Verge CF, Mandrup-Poulsen T.

Diabetologia. 2000 Jun;43(6):800-8.

PMID:
10907126
23.

No evidence for linkage of a novel CA repeat polymorphism for apoptosis antigen 1 (APO-1 or fas) with type I diabetes in a Caucasian population.

Sangthongpitag K, Moore KR, Lapsys NM, Bao F, Babu SR, Fain PR, Verge CF.

Hum Hered. 1998 Nov-Dec;48(6):343-5.

PMID:
9813457
24.

Cloning and expression of the Bacillus sphaericus 2362 mosquitocidal genes in a non-toxic unicellular cyanobacterium, Synechococcus PCC6301.

Sangthongpitag K, Penfold RJ, Delaney SF, Rogers PL.

Appl Microbiol Biotechnol. 1997 Apr;47(4):379-84.

PMID:
9163952

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