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Items: 18

1.

MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology.

Boga SB, Deng Y, Zhu L, Nan Y, Cooper AB, Shipps GW Jr, Doll R, Shih NY, Zhu H, Sun R, Wang T, Paliwal S, Tsui HC, Gao X, Yao X, Desai J, Wang J, Alhassan AB, Kelly J, Patel M, Muppalla K, Gudipati S, Zhang LK, Buevich A, Hesk D, Carr D, Dayananth P, Black S, Mei H, Cox K, Sherborne B, Hruza AW, Xiao L, Jin W, Long B, Liu G, Taylor SA, Kirschmeier P, Windsor WT, Bishop R, Samatar AA.

ACS Med Chem Lett. 2018 Jun 14;9(7):761-767. doi: 10.1021/acsmedchemlett.8b00220. eCollection 2018 Jul 12.

PMID:
30034615
2.

Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology.

Boga SB, Alhassan AB, Cooper AB, Doll R, Shih NY, Shipps G, Deng Y, Zhu H, Nan Y, Sun R, Zhu L, Desai J, Patel M, Muppalla K, Gao X, Wang J, Yao X, Kelly J, Gudipati S, Paliwal S, Tsui HC, Wang T, Sherborne B, Xiao L, Hruza A, Buevich A, Zhang LK, Hesk D, Samatar AA, Carr D, Long B, Black S, Dayananth P, Windsor W, Kirschmeier P, Bishop R.

Bioorg Med Chem Lett. 2018 Jun 15;28(11):2029-2034. doi: 10.1016/j.bmcl.2018.04.063. Epub 2018 Apr 26.

PMID:
29748051
3.

Development of MK-8353, an orally administered ERK1/2 inhibitor, in patients with advanced solid tumors.

Moschos SJ, Sullivan RJ, Hwu WJ, Ramanathan RK, Adjei AA, Fong PC, Shapira-Frommer R, Tawbi HA, Rubino J, Rush TS 3rd, Zhang D, Miselis NR, Samatar AA, Chun P, Rubin EH, Schiller J, Long BJ, Dayananth P, Carr D, Kirschmeier P, Bishop WR, Deng Y, Cooper A, Shipps GW, Moreno BH, Robert L, Ribas A, Flaherty KT.

JCI Insight. 2018 Feb 22;3(4). pii: 92352. doi: 10.1172/jci.insight.92352. [Epub ahead of print]

4.

Targeting Notch enhances the efficacy of ERK inhibitors in BRAF-V600E melanoma.

Krepler C, Xiao M, Samanta M, Vultur A, Chen HY, Brafford P, Reyes-Uribe PI, Halloran M, Chen T, He X, Hristova D, Liu Q, Samatar AA, Davies MA, Nathanson KL, Fukunaga-Kalabis M, Herlyn M, Villanueva J.

Oncotarget. 2016 Nov 1;7(44):71211-71222. doi: 10.18632/oncotarget.12078.

5.

Dissecting Therapeutic Resistance to ERK Inhibition.

Jha S, Morris EJ, Hruza A, Mansueto MS, Schroeder GK, Arbanas J, McMasters D, Restaino CR, Dayananth P, Black S, Elsen NL, Mannarino A, Cooper A, Fawell S, Zawel L, Jayaraman L, Samatar AA.

Mol Cancer Ther. 2016 Apr;15(4):548-59. doi: 10.1158/1535-7163.MCT-15-0172. Epub 2016 Feb 1.

6.

Long-Term ERK Inhibition in KRAS-Mutant Pancreatic Cancer Is Associated with MYC Degradation and Senescence-like Growth Suppression.

Hayes TK, Neel NF, Hu C, Gautam P, Chenard M, Long B, Aziz M, Kassner M, Bryant KL, Pierobon M, Marayati R, Kher S, George SD, Xu M, Wang-Gillam A, Samatar AA, Maitra A, Wennerberg K, Petricoin EF 3rd, Yin HH, Nelkin B, Cox AD, Yeh JJ, Der CJ.

Cancer Cell. 2016 Jan 11;29(1):75-89. doi: 10.1016/j.ccell.2015.11.011. Epub 2015 Dec 24.

7.

Network-level effects of kinase inhibitors modulate TNF-α-induced apoptosis in the intestinal epithelium.

Gierut JJ, Wood LB, Lau KS, Lin YJ, Genetti C, Samatar AA, Lauffenburger DA, Haigis KM.

Sci Signal. 2015 Dec 15;8(407):ra129. doi: 10.1126/scisignal.aac7235.

8.

Cooperative induction of apoptosis in NRAS mutant melanoma by inhibition of MEK and ROCK.

Vogel CJ, Smit MA, Maddalo G, Possik PA, Sparidans RW, van der Burg SH, Verdegaal EM, Heck AJ, Samatar AA, Beijnen JH, Altelaar AF, Peeper DS.

Pigment Cell Melanoma Res. 2015 May;28(3):307-17. doi: 10.1111/pcmr.12364. Epub 2015 Apr 6.

PMID:
25728708
9.

Tunable-combinatorial mechanisms of acquired resistance limit the efficacy of BRAF/MEK cotargeting but result in melanoma drug addiction.

Moriceau G, Hugo W, Hong A, Shi H, Kong X, Yu CC, Koya RC, Samatar AA, Khanlou N, Braun J, Ruchalski K, Seifert H, Larkin J, Dahlman KB, Johnson DB, Algazi A, Sosman JA, Ribas A, Lo RS.

Cancer Cell. 2015 Feb 9;27(2):240-56. doi: 10.1016/j.ccell.2014.11.018. Epub 2015 Jan 15.

10.

Targeting RAS-ERK signalling in cancer: promises and challenges.

Samatar AA, Poulikakos PI.

Nat Rev Drug Discov. 2014 Dec;13(12):928-42. doi: 10.1038/nrd4281. Review.

PMID:
25435214
11.

Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.

Deng Y, Shipps GW Jr, Cooper A, English JM, Annis DA, Carr D, Nan Y, Wang T, Zhu HY, Chuang CC, Dayananth P, Hruza AW, Xiao L, Jin W, Kirschmeier P, Windsor WT, Samatar AA.

J Med Chem. 2014 Nov 13;57(21):8817-26. doi: 10.1021/jm500847m. Epub 2014 Oct 22.

PMID:
25313996
12.

Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors.

Morris EJ, Jha S, Restaino CR, Dayananth P, Zhu H, Cooper A, Carr D, Deng Y, Jin W, Black S, Long B, Liu J, Dinunzio E, Windsor W, Zhang R, Zhao S, Angagaw MH, Pinheiro EM, Desai J, Xiao L, Shipps G, Hruza A, Wang J, Kelly J, Paliwal S, Gao X, Babu BS, Zhu L, Daublain P, Zhang L, Lutterbach BA, Pelletier MR, Philippar U, Siliphaivanh P, Witter D, Kirschmeier P, Bishop WR, Hicklin D, Gilliland DG, Jayaraman L, Zawel L, Fawell S, Samatar AA.

Cancer Discov. 2013 Jul;3(7):742-50. doi: 10.1158/2159-8290.CD-13-0070. Epub 2013 Apr 24.

13.

Inhibitors of the ERK mitogen-activated protein kinase cascade for targeting RAS mutant cancers.

Gentry L, Samatar AA, Der CJ.

Enzymes. 2013;34 Pt. B:67-106. doi: 10.1016/B978-0-12-420146-0.00004-4. Epub 2013 Nov 7. Review.

PMID:
25034101
14.

Identification of overexpression of orphan G protein-coupled receptor GPR49 in human colon and ovarian primary tumors.

McClanahan T, Koseoglu S, Smith K, Grein J, Gustafson E, Black S, Kirschmeier P, Samatar AA.

Cancer Biol Ther. 2006 Apr;5(4):419-26. Epub 2006 Apr 19.

PMID:
16575208
15.

Development of a fluorescence polarization bead-based coupled assay to target different activity/conformation states of a protein kinase.

Lu Z, Yin Z, James L, Syto R, Stafford JM, Koseoglu S, Mayhood T, Myers J, Windsor W, Kirschmeier P, Samatar AA, Malcolm B, Turek-Etienne TC, Kumar CC.

J Biomol Screen. 2004 Jun;9(4):309-21.

PMID:
15191648
16.

Transforming growth factor-beta 2 is a transcriptional target for Akt/protein kinase B via forkhead transcription factor.

Samatar AA, Wang L, Mirza A, Koseoglu S, Liu S, Kumar CC.

J Biol Chem. 2002 Aug 2;277(31):28118-26. Epub 2002 May 14.

17.

Expression, purification, characterization and homology modeling of active Akt/PKB, a key enzyme involved in cell survival signaling.

Kumar CC, Diao R, Yin Z, Liu Y, Samatar AA, Madison V, Xiao L.

Biochim Biophys Acta. 2001 Jun 15;1526(3):257-68.

PMID:
11410335
18.

Biochemical characterization of a human band 4.1-related protein-tyrosine phosphatase, PTPH1.

Zhang SH, Eckberg WR, Yang Q, Samatar AA, Tonks NK.

J Biol Chem. 1995 Aug 25;270(34):20067-72.

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