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Items: 19


Structure-based design of N-substituted 1-hydroxy-4-sulfamoyl-2-naphthoates as selective inhibitors of the Mcl-1 oncoprotein.

Lanning ME, Yu W, Yap JL, Chauhan J, Chen L, Whiting E, Pidugu LS, Atkinson T, Bailey H, Li W, Roth BM, Hynicka L, Chesko K, Toth EA, Shapiro P, MacKerell AD Jr, Wilder PT, Fletcher S.

Eur J Med Chem. 2016 May 4;113:273-92. doi: 10.1016/j.ejmech.2016.02.006. Epub 2016 Feb 4.


Structural Re-engineering of the α-Helix Mimetic JY-1-106 into Small Molecules: Disruption of the Mcl-1-Bak-BH3 Protein-Protein Interaction with 2,6-Di-Substituted Nicotinates.

Drennen B, Scheenstra JA, Yap JL, Chen L, Lanning ME, Roth BM, Wilder PT, Fletcher S.

ChemMedChem. 2016 Apr 19;11(8):827-33. doi: 10.1002/cmdc.201500461. Epub 2016 Feb 4.


Towards more drug-like proteomimetics: two-faced, synthetic α-helix mimetics based on a purine scaffold.

Lanning ME, Wilder PT, Bailey H, Drennen B, Cavalier M, Chen L, Yap JL, Raje M, Fletcher S.

Org Biomol Chem. 2015 Aug 28;13(32):8642-6. doi: 10.1039/c5ob00478k. Epub 2015 Jul 24.


BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536.

Chen L, Yap JL, Yoshioka M, Lanning ME, Fountain RN, Raje M, Scheenstra JA, Strovel JW, Fletcher S.

ACS Med Chem Lett. 2015 May 18;6(7):764-9. doi: 10.1021/acsmedchemlett.5b00084. eCollection 2015 Jul 9.


Perturbation of the c-Myc-Max protein-protein interaction via synthetic α-helix mimetics.

Jung KY, Wang H, Teriete P, Yap JL, Chen L, Lanning ME, Hu A, Lambert LJ, Holien T, Sundan A, Cosford ND, Prochownik EV, Fletcher S.

J Med Chem. 2015 Apr 9;58(7):3002-24. doi: 10.1021/jm501440q. Epub 2015 Mar 30.


BCL-xL/MCL-1 inhibition and RARγ antagonism work cooperatively in human HL60 leukemia cells.

Perri M, Yap JL, Yu J, Cione E, Fletcher S, Kane MA.

Exp Cell Res. 2014 Oct 1;327(2):183-91. doi: 10.1016/j.yexcr.2014.07.024. Epub 2014 Aug 1.


Discovery of methyl 4'-methyl-5-(7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)-[1,1'-biphenyl]-3-carboxylate, an improved small-molecule inhibitor of c-Myc-max dimerization.

Chauhan J, Wang H, Yap JL, Sabato PE, Hu A, Prochownik EV, Fletcher S.

ChemMedChem. 2014 Oct;9(10):2274-85. doi: 10.1002/cmdc.201402189. Epub 2014 Jun 27.


Disruption of Myc-Max heterodimerization with improved cell-penetrating analogs of the small molecule 10074-G5.

Wang H, Chauhan J, Hu A, Pendleton K, Yap JL, Sabato PE, Jones JW, Perri M, Yu J, Cione E, Kane MA, Fletcher S, Prochownik EV.

Oncotarget. 2013 Jun;4(6):936-47.


Amphipathic α-helix mimetics based on a 1,2-diphenylacetylene scaffold.

Jung KY, Vanommeslaeghe K, Lanning ME, Yap JL, Gordon C, Wilder PT, MacKerell AD Jr, Fletcher S.

Org Lett. 2013 Jul 5;15(13):3234-7. doi: 10.1021/ol401197n. Epub 2013 Jun 13.


The novel BH3 α-helix mimetic JY-1-106 induces apoptosis in a subset of cancer cells (lung cancer, colon cancer and mesothelioma) by disrupting Bcl-xL and Mcl-1 protein-protein interactions with Bak.

Cao X, Yap JL, Newell-Rogers MK, Peddaboina C, Jiang W, Papaconstantinou HT, Jupitor D, Rai A, Jung KY, Tubin RP, Yu W, Vanommeslaeghe K, Wilder PT, MacKerell AD Jr, Fletcher S, Smythe RW.

Mol Cancer. 2013 May 16;12(1):42. doi: 10.1186/1476-4598-12-42.


Structural modifications of (Z)-3-(2-aminoethyl)-5-(4-ethoxybenzylidene)thiazolidine-2,4-dione that improve selectivity for inhibiting the proliferation of melanoma cells containing active ERK signaling.

Jung KY, Samadani R, Chauhan J, Nevels K, Yap JL, Zhang J, Worlikar S, Lanning ME, Chen L, Ensey M, Shukla S, Salmo R, Heinzl G, Gordon C, Dukes T, MacKerell AD Jr, Shapiro P, Fletcher S.

Org Biomol Chem. 2013 Jun 14;11(22):3706-32. doi: 10.1039/c3ob40199e.


Pharmacophore identification of c-Myc inhibitor 10074-G5.

Yap JL, Wang H, Hu A, Chauhan J, Jung KY, Gharavi RB, Prochownik EV, Fletcher S.

Bioorg Med Chem Lett. 2013 Jan 1;23(1):370-4. doi: 10.1016/j.bmcl.2012.10.013. Epub 2012 Oct 17.


The downregulation of Mcl-1 via USP9X inhibition sensitizes solid tumors to Bcl-xl inhibition.

Peddaboina C, Jupiter D, Fletcher S, Yap JL, Rai A, Tobin RP, Jiang W, Rascoe P, Rogers MK, Smythe WR, Cao X.

BMC Cancer. 2012 Nov 21;12:541. doi: 10.1186/1471-2407-12-541.


Treatment of cerebellar cognitive affective syndrome with aripiprazole.

Yap JL, Wachtel LE, Ahn ES, Sanz JH, Slomine BS, Pidcock FS.

J Pediatr Rehabil Med. 2012;5(3):233-8.


Relaxation of the rigid backbone of an oligoamide-foldamer-based α-helix mimetic: identification of potent Bcl-xL inhibitors.

Yap JL, Cao X, Vanommeslaeghe K, Jung KY, Peddaboina C, Wilder PT, Nan A, MacKerell AD Jr, Smythe WR, Fletcher S.

Org Biomol Chem. 2012 Apr 21;10(15):2928-33. doi: 10.1039/c2ob07125h. Epub 2012 Mar 7.


Small-molecule inhibitors of the ERK signaling pathway: Towards novel anticancer therapeutics.

Yap JL, Worlikar S, MacKerell AD Jr, Shapiro P, Fletcher S.

ChemMedChem. 2011 Jan 3;6(1):38-48. doi: 10.1002/cmdc.201000354. Review. No abstract available.


Serum concentrations and clinical effects of risperidone in schizophrenic patients in Singapore--a preliminary report.

Lee HS, Tan CH, Khoo YM, Chee KT, Wong KE, Chong SA, Mahendran R, Yap JL, Low BL, Choo CH, Chan A.

Br J Clin Pharmacol. 1999 Apr;47(4):460-1. No abstract available.


New muscle transplant method produces normal twitch tension in dystrophic muscle.

Law PK, Yap JL.

Muscle Nerve. 1979 Sep-Oct;2(5):356-63.

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