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Items: 15

1.

The new small molecule tyrosine-kinase inhibitor ARQ531 targets acute myeloid leukemia cells by disrupting multiple tumor-addicted programs.

Soncini D, Orecchioni S, Ruberti S, Minetto P, Martinuzzi C, Agnelli L, Todoerti K, Cagnetta A, Miglino M, Clavio M, Contini P, Varaldo R, Bergamaschi M, Guolo F, Passalacqua M, Nencioni A, Monacelli F, Gobbi M, Neri A, Abbadessa G, Eathiraj S, Schwartz B, Bertolini F, Lemoli RM, Cea M.

Haematologica. 2019 Oct 17. pii: haematol.2019.224956. doi: 10.3324/haematol.2019.224956. [Epub ahead of print]

2.

The BTK Inhibitor ARQ 531 Targets Ibrutinib-Resistant CLL and Richter Transformation.

Reiff SD, Mantel R, Smith LL, Greene JT, Muhowski EM, Fabian CA, Goettl VM, Tran M, Harrington BK, Rogers KA, Awan FT, Maddocks K, Andritsos L, Lehman AM, Sampath D, Lapalombella R, Eathiraj S, Abbadessa G, Schwartz B, Johnson AJ, Byrd JC, Woyach JA.

Cancer Discov. 2018 Oct;8(10):1300-1315. doi: 10.1158/2159-8290.CD-17-1409. Epub 2018 Aug 9.

3.

In-vitro and in-vivo combined effect of ARQ 092, an AKT inhibitor, with ARQ 087, a FGFR inhibitor.

Yu Y, Hall T, Eathiraj S, Wick MJ, Schwartz B, Abbadessa G.

Anticancer Drugs. 2017 Jun;28(5):503-513. doi: 10.1097/CAD.0000000000000486.

4.

Preclinical Activity of ARQ 087, a Novel Inhibitor Targeting FGFR Dysregulation.

Hall TG, Yu Y, Eathiraj S, Wang Y, Savage RE, Lapierre JM, Schwartz B, Abbadessa G.

PLoS One. 2016 Sep 14;11(9):e0162594. doi: 10.1371/journal.pone.0162594. eCollection 2016.

5.

Discovery of 3-(3-(4-(1-Aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine (ARQ 092): An Orally Bioavailable, Selective, and Potent Allosteric AKT Inhibitor.

Lapierre JM, Eathiraj S, Vensel D, Liu Y, Bull CO, Cornell-Kennon S, Iimura S, Kelleher EW, Kizer DE, Koerner S, Makhija S, Matsuda A, Moussa M, Namdev N, Savage RE, Szwaya J, Volckova E, Westlund N, Wu H, Schwartz B.

J Med Chem. 2016 Jul 14;59(13):6455-69. doi: 10.1021/acs.jmedchem.6b00619. Epub 2016 Jun 29.

PMID:
27305487
6.

Targeting AKT1-E17K and the PI3K/AKT Pathway with an Allosteric AKT Inhibitor, ARQ 092.

Yu Y, Savage RE, Eathiraj S, Meade J, Wick MJ, Hall T, Abbadessa G, Schwartz B.

PLoS One. 2015 Oct 15;10(10):e0140479. doi: 10.1371/journal.pone.0140479. eCollection 2015.

7.

Discovery and optimization of a series of 3-(3-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: orally bioavailable, selective, and potent ATP-independent Akt inhibitors.

Ashwell MA, Lapierre JM, Brassard C, Bresciano K, Bull C, Cornell-Kennon S, Eathiraj S, France DS, Hall T, Hill J, Kelleher E, Khanapurkar S, Kizer D, Koerner S, Link J, Liu Y, Makhija S, Moussa M, Namdev N, Nguyen K, Nicewonger R, Palma R, Szwaya J, Tandon M, Uppalapati U, Vensel D, Volak LP, Volckova E, Westlund N, Wu H, Yang RY, Chan TC.

J Med Chem. 2012 Jun 14;55(11):5291-310. doi: 10.1021/jm300276x. Epub 2012 May 31.

PMID:
22533986
8.

A novel mode of protein kinase inhibition exploiting hydrophobic motifs of autoinhibited kinases: discovery of ATP-independent inhibitors of fibroblast growth factor receptor.

Eathiraj S, Palma R, Hirschi M, Volckova E, Nakuci E, Castro J, Chen CR, Chan TC, France DS, Ashwell MA.

J Biol Chem. 2011 Jun 10;286(23):20677-87. doi: 10.1074/jbc.M110.213736. Epub 2011 Mar 24.

9.

Discovery of a novel mode of protein kinase inhibition characterized by the mechanism of inhibition of human mesenchymal-epithelial transition factor (c-Met) protein autophosphorylation by ARQ 197.

Eathiraj S, Palma R, Volckova E, Hirschi M, France DS, Ashwell MA, Chan TC.

J Biol Chem. 2011 Jun 10;286(23):20666-76. doi: 10.1074/jbc.M110.213801. Epub 2011 Mar 24.

10.

Structural basis for Rab GTPase recognition and endosome tethering by the C2H2 zinc finger of Early Endosomal Autoantigen 1 (EEA1).

Mishra A, Eathiraj S, Corvera S, Lambright DG.

Proc Natl Acad Sci U S A. 2010 Jun 15;107(24):10866-71. doi: 10.1073/pnas.1000843107. Epub 2010 Jun 1.

11.

Structural basis for Rab11-mediated recruitment of FIP3 to recycling endosomes.

Eathiraj S, Mishra A, Prekeris R, Lambright DG.

J Mol Biol. 2006 Nov 24;364(2):121-35. Epub 2006 Aug 26.

PMID:
17007872
12.

TBC-domain GAPs for Rab GTPases accelerate GTP hydrolysis by a dual-finger mechanism.

Pan X, Eathiraj S, Munson M, Lambright DG.

Nature. 2006 Jul 20;442(7100):303-6.

PMID:
16855591
13.

ESCRT complexes assembled and GLUEd.

Eathiraj S, Lambright DG.

Structure. 2006 Apr;14(4):631-2.

14.

Structural basis of family-wide Rab GTPase recognition by rabenosyn-5.

Eathiraj S, Pan X, Ritacco C, Lambright DG.

Nature. 2005 Jul 21;436(7049):415-9.

15.

Determinants of Rab5 interaction with the N terminus of early endosome antigen 1.

Merithew E, Stone C, Eathiraj S, Lambright DG.

J Biol Chem. 2003 Mar 7;278(10):8494-500. Epub 2002 Dec 19.

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