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Items: 17


A phase 1 dose-escalation and expansion study of binimetinib (MEK162), a potent and selective oral MEK1/2 inhibitor.

Bendell JC, Javle M, Bekaii-Saab TS, Finn RS, Wainberg ZA, Laheru DA, Weekes CD, Tan BR, Khan GN, Zalupski MM, Infante JR, Jones S, Papadopoulos KP, Tolcher AW, Chavira RE, Christy-Bittel JL, Barrett E, Patnaik A.

Br J Cancer. 2017 Feb 28;116(5):575-583. doi: 10.1038/bjc.2017.10. Epub 2017 Feb 2.


Cytotoxic efficacy of filanesib and melphalan combination is governed by sequence of treatment in human myeloma cells.

Norris EJ, DeStephanis D, Tunquist B, Usmani S, Ganapathi R, Ganapathi M.

Blood Cancer J. 2016 Oct 7;6(10):e480. doi: 10.1038/bcj.2016.92. No abstract available.


A phase I dose-escalation study of TAK-733, an investigational oral MEK inhibitor, in patients with advanced solid tumors.

Adjei AA, LoRusso P, Ribas A, Sosman JA, Pavlick A, Dy GK, Zhou X, Gangolli E, Kneissl M, Faucette S, Neuwirth R, Bózon V.

Invest New Drugs. 2017 Feb;35(1):47-58. doi: 10.1007/s10637-016-0391-2. Epub 2016 Sep 21.


Selective inhibition of tropomyosin-receptor-kinase A (TrkA) reduces pain and joint damage in two rat models of inflammatory arthritis.

Ashraf S, Bouhana KS, Pheneger J, Andrews SW, Walsh DA.

Arthritis Res Ther. 2016 May 4;18(1):97. doi: 10.1186/s13075-016-0996-z.


Immobilized Cytochrome P450 for Monitoring of P450-P450 Interactions and Metabolism.

Bostick CD, Hickey KM, Wollenberg LA, Flora DR, Tracy TS, Gannett PM.

Drug Metab Dispos. 2016 May;44(5):741-9. doi: 10.1124/dmd.115.067637. Epub 2016 Mar 9.


Impact of race and tumor subtype on second malignancy risk in women with breast cancer.

Diab N, Clark G, Langer L, Wang Y, Hamlington B, Brzeskiewicz L, O'Shaughnessy J, Diab S, Jabbour SK.

Springerplus. 2016 Jan 6;5:14. doi: 10.1186/s40064-015-1657-4. eCollection 2016.


An exploratory, randomized, parallel-group, open-label, relative bioavailability study with an additional two-period crossover food-effect study exploring the pharmacokinetics of two novel formulations of pexmetinib (ARRY-614).

Wollenberg LA, Corson DT, Nugent CA, Peterson FL, Ptaszynski AM, Arrigo A, Mannila CG, Litwiler KS, Bell SJ.

Clin Pharmacol. 2015 Sep 30;7:87-95. doi: 10.2147/CPAA.S83871. eCollection 2015.


Characterization of degenerative human facet joints and facet joint capsular tissues.

Kim JS, Ali MH, Wydra F, Li X, Hamilton JL, An HS, Cs-Szabo G, Andrews S, Moric M, Xiao G, Wang JH, Chen D, Cavanaugh JM, Im HJ.

Osteoarthritis Cartilage. 2015 Dec;23(12):2242-51. doi: 10.1016/j.joca.2015.06.009. Epub 2015 Jun 25.


Protein Kinase A Opposes the Phosphorylation-dependent Recruitment of Glycogen Synthase Kinase 3β to A-kinase Anchoring Protein 220.

Whiting JL, Nygren PJ, Tunquist BJ, Langeberg LK, Seternes OM, Scott JD.

J Biol Chem. 2015 Aug 7;290(32):19445-57. doi: 10.1074/jbc.M115.654822. Epub 2015 Jun 18.


C5-Alkyl-2-methylurea-Substituted Pyridines as a New Class of Glucokinase Activators.

Du X, Hinklin RJ, Xiong Y, Dransfield P, Park J, Kohn TJ, Pattaropong V, Lai S, Fu Z, Jiao X, Chow D, Jin L, Davda J, Veniant MM, Anderson DA, Baer BR, Bencsik JR, Boyd SA, Chicarelli MJ, Mohr PJ, Wang B, Condroski KR, DeWolf WE, Conn M, Tran T, Yang J, Aicher TD, Medina JC, Coward P, Houze JB.

ACS Med Chem Lett. 2014 Nov 22;5(12):1284-9. doi: 10.1021/ml500341w. eCollection 2014 Dec 11.


A phase I study of oral ARRY-614, a p38 MAPK/Tie2 dual inhibitor, in patients with low or intermediate-1 risk myelodysplastic syndromes.

Garcia-Manero G, Khoury HJ, Jabbour E, Lancet J, Winski SL, Cable L, Rush S, Maloney L, Hogeland G, Ptaszynski M, Calvo MC, Bohannan Z, List A, Kantarjian H, Komrokji R.

Clin Cancer Res. 2015 Mar 1;21(5):985-94. doi: 10.1158/1078-0432.CCR-14-1765. Epub 2014 Dec 5.


Discovery of a Novel Class of Imidazo[1,2-a]Pyridines with Potent PDGFR Activity and Oral Bioavailability.

Hicken EJ, Marmsater FP, Munson MC, Schlachter ST, Robinson JE, Allen S, Burgess LE, DeLisle RK, Rizzi JP, Topalov GT, Zhao Q, Hicks JM, Kallan NC, Tarlton E, Allen A, Callejo M, Cox A, Rana S, Klopfenstein N, Woessner R, Lyssikatos JP.

ACS Med Chem Lett. 2013 Nov 12;5(1):78-83. doi: 10.1021/ml4003953. eCollection 2014 Jan 9.


Characterization of a novel glucokinase activator in rat and mouse models.

Lu M, Li P, Bandyopadhyay G, Lagakos W, Dewolf WE Jr, Alford T, Chicarelli MJ, Williams L, Anderson DA, Baer BR, McVean M, Conn M, Véniant MM, Coward P.

PLoS One. 2014 Feb 12;9(2):e88431. doi: 10.1371/journal.pone.0088431. eCollection 2014.


Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.

Wang T, Lamb ML, Block MH, Davies AM, Han Y, Hoffmann E, Ioannidis S, Josey JA, Liu ZY, Lyne PD, MacIntyre T, Mohr PJ, Omer CA, Sjögren T, Thress K, Wang B, Wang H, Yu D, Zhang HJ.

ACS Med Chem Lett. 2012 Jul 26;3(9):705-9. doi: 10.1021/ml300074j. eCollection 2012 Sep 13.


Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors.

Wenglowsky S, Ren L, Ahrendt KA, Laird ER, Aliagas I, Alicke B, Buckmelter AJ, Choo EF, Dinkel V, Feng B, Gloor SL, Gould SE, Gross S, Gunzner-Toste J, Hansen JD, Hatzivassiliou G, Liu B, Malesky K, Mathieu S, Newhouse B, Raddatz NJ, Ran Y, Rana S, Randolph N, Risom T, Rudolph J, Savage S, Selby LT, Shrag M, Song K, Sturgis HL, Voegtli WC, Wen Z, Willis BS, Woessner RD, Wu WI, Young WB, Grina J.

ACS Med Chem Lett. 2011 Mar 8;2(5):342-7. doi: 10.1021/ml200025q. eCollection 2011 May 12.


Crystal structure of human AKT1 with an allosteric inhibitor reveals a new mode of kinase inhibition.

Wu WI, Voegtli WC, Sturgis HL, Dizon FP, Vigers GP, Brandhuber BJ.

PLoS One. 2010 Sep 23;5(9):e12913. doi: 10.1371/journal.pone.0012913.


Potent selective nonpeptidic inhibitors of human lung tryptase.

Burgess LE, Newhouse BJ, Ibrahim P, Rizzi J, Kashem MA, Hartman A, Brandhuber BJ, Wright CD, Thomson DS, Vigers GP, Koch K.

Proc Natl Acad Sci U S A. 1999 Jul 20;96(15):8348-52.

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