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The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity.

Canon J, Rex K, Saiki AY, Mohr C, Cooke K, Bagal D, Gaida K, Holt T, Knutson CG, Koppada N, Lanman BA, Werner J, Rapaport AS, San Miguel T, Ortiz R, Osgood T, Sun JR, Zhu X, McCarter JD, Volak LP, Houk BE, Fakih MG, O'Neil BH, Price TJ, Falchook GS, Desai J, Kuo J, Govindan R, Hong DS, Ouyang W, Henary H, Arvedson T, Cee VJ, Lipford JR.

Nature. 2019 Nov;575(7781):217-223. doi: 10.1038/s41586-019-1694-1. Epub 2019 Oct 30.


Dual inhibition of angiopoietin-TIE2 and MET alters the tumor microenvironment and prolongs survival in a metastatic model of renal cell carcinoma.

Elbanna M, Orillion AR, Damayanti NP, Adelaiye-Ogala R, Shen L, Miles KM, Chintala S, Ciamporcero E, Ramakrishnan S, Ku SY, Rex K, Caenepeel S, Coxon A, Pili R.

Mol Cancer Ther. 2019 Oct 3. pii: molcanther.1202.2018. doi: 10.1158/1535-7163.MCT-18-1202. [Epub ahead of print]


Iodine in Edible Seaweed, Its Absorption, Dietary Use, and Relation to Iodine Nutrition in Arctic People.

Andersen S, Noahsen P, Rex KF, Florian-Sørensen HC, Mulvad G.

J Med Food. 2019 Apr;22(4):421-426. doi: 10.1089/jmf.2018.0187.


Discovery of ( R)-8-(6-Methyl-4-oxo-1,4,5,6-tetrahydropyrrolo[3,4- b]pyrrol-2-yl)-3-(1-methylcyclopropyl)-2-((1-methylcyclopropyl)amino)quinazolin-4(3 H)-one, a Potent and Selective Pim-1/2 Kinase Inhibitor for Hematological Malignancies.

Wang HL, Andrews KL, Booker SK, Canon J, Cee VJ, Chavez F Jr, Chen Y, Eastwood H, Guerrero N, Herberich B, Hickman D, Lanman BA, Laszlo J 3rd, Lee MR, Lipford JR, Mattson B, Mohr C, Nguyen Y, Norman MH, Pettus LH, Powers D, Reed AB, Rex K, Sastri C, Tamayo N, Wang P, Winston JT, Wu B, Wu Q, Wu T, Wurz RP, Xu Y, Zhou Y, Tasker AS.

J Med Chem. 2019 Feb 14;62(3):1523-1540. doi: 10.1021/acs.jmedchem.8b01733. Epub 2019 Jan 17.


Serum 25-hydroxyvitamin D, calcium and parathyroid hormone levels in Native and European populations in Greenland.

Andersen S, Noahsen P, Rex KF, Fleischer I, Albertsen N, Jørgensen ME, Schæbel LK, Laursen MB.

Br J Nutr. 2018 Feb;119(4):391-397. doi: 10.1017/S0007114517003944.


Selective MET Kinase Inhibition in MET-Dependent Glioma Models Alters Gene Expression and Induces Tumor Plasticity.

van den Heuvel CNAM, Navis AC, de Bitter T, Amiri H, Verrijp K, Heerschap A, Rex K, Dussault I, Caenepeel S, Coxon A, Span PN, Wesseling P, Hendriks W, Leenders WPJ.

Mol Cancer Res. 2017 Nov;15(11):1587-1597. doi: 10.1158/1541-7786.MCR-17-0177. Epub 2017 Jul 27.


The IDL of E. coli SSB links ssDNA and protein binding by mediating protein-protein interactions.

Bianco PR, Pottinger S, Tan HY, Nguyenduc T, Rex K, Varshney U.

Protein Sci. 2017 Feb;26(2):227-241. doi: 10.1002/pro.3072. Epub 2017 Jan 26.


Discovery and Optimization of Quinazolinone-pyrrolopyrrolones as Potent and Orally Bioavailable Pan-Pim Kinase Inhibitors.

Pettus LH, Andrews KL, Booker SK, Chen J, Cee VJ, Chavez F Jr, Chen Y, Eastwood H, Guerrero N, Herberich B, Hickman D, Lanman BA, Laszlo J 3rd, Lee MR, Lipford JR, Mattson B, Mohr C, Nguyen Y, Norman MH, Powers D, Reed AB, Rex K, Sastri C, Tamayo N, Wang P, Winston JT, Wu B, Wu T, Wurz RP, Xu Y, Zhou Y, Tasker AS, Wang HL.

J Med Chem. 2016 Jul 14;59(13):6407-30. doi: 10.1021/acs.jmedchem.6b00610. Epub 2016 Jun 22.


In Vitro and In Vivo Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models.

Hughes PE, Rex K, Caenepeel S, Yang Y, Zhang Y, Broome MA, Kha HT, Burgess TL, Amore B, Kaplan-Lefko PJ, Moriguchi J, Werner J, Damore MA, Baker D, Choquette DM, Harmange JC, Radinsky R, Kendall R, Dussault I, Coxon A.

Mol Cancer Ther. 2016 Jul;15(7):1568-79. doi: 10.1158/1535-7163.MCT-15-0871. Epub 2016 Apr 19.


Preclinical Evaluation of AMG 337, a Highly Selective Small Molecule MET Inhibitor, in Hepatocellular Carcinoma.

Du Z, Caenepeel S, Shen Y, Rex K, Zhang Y, He Y, Tang ET, Wang O, Zhong W, Zhou H, Huang J, Huang E, Hu L, Coxon A, Zhang M.

Mol Cancer Ther. 2016 Jun;15(6):1227-37. doi: 10.1158/1535-7163.MCT-15-0745. Epub 2016 Mar 29.


Discovery and Optimization of Macrocyclic Quinoxaline-pyrrolo-dihydropiperidinones as Potent Pim-1/2 Kinase Inhibitors.

Cee VJ, Chavez F Jr, Herberich B, Lanman BA, Pettus LH, Reed AB, Wu B, Wurz RP, Andrews KL, Chen J, Hickman D, Laszlo J 3rd, Lee MR, Guerrero N, Mattson BK, Nguyen Y, Mohr C, Rex K, Sastri CE, Wang P, Wu Q, Wu T, Xu Y, Zhou Y, Winston JT, Lipford JR, Tasker AS, Wang HL.

ACS Med Chem Lett. 2016 Feb 12;7(4):408-12. doi: 10.1021/acsmedchemlett.5b00403. eCollection 2016 Apr 14.


Liver biochemistry and associations with alcohol intake, hepatitis B virus infection and Inuit ethnicity: a population-based comparative epidemiological survey in Greenland and Denmark.

Rex KF, Krarup HB, Laurberg P, Andersen S.

Int J Circumpolar Health. 2016 Feb 26;75:29528. doi: 10.3402/ijch.v75.29528. eCollection 2016.


Discovery of (R)-6-(1-(8-Fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity.

Boezio AA, Copeland KW, Rex K, K Albrecht B, Bauer D, Bellon SF, Boezio C, Broome MA, Choquette D, Coxon A, Dussault I, Hirai S, Lewis R, Lin MH, Lohman J, Liu J, Peterson EA, Potashman M, Shimanovich R, Teffera Y, Whittington DA, Vaida KR, Harmange JC.

J Med Chem. 2016 Mar 24;59(6):2328-42. doi: 10.1021/acs.jmedchem.5b01716. Epub 2016 Feb 11.


Simultaneous presence of fhs and purT genes is disadvantageous for the fitness of Escherichia coli growth.

Aluri S, Rex K, Varshney U.

FEMS Microbiol Lett. 2015 Jul;362(14). pii: fnv101. doi: 10.1093/femsle/fnv101. Epub 2015 Jun 22.


Hepatitis B among Inuit: A review with focus on Greenland Inuit.

Rex KF, Andersen S, Krarup HB.

World J Hepatol. 2015 May 28;7(9):1265-71. doi: 10.4254/wjh.v7.i9.1265. Review.


Correction to Discovery of Potent and Selective 8-Fluorotriazolopyridine c-Met Inhibitors.

Peterson EA, Teffera Y, Albrecht BK, Bauer D, Bellon SF, Boezio A, Boezio C, Broome MA, Choquette D, Copeland KW, Dussault I, Lewis R, Lin MH, Lohman J, Liu J, Potashman M, Rex K, Shimanovich R, Whittington DA, Vaida KR, Harmange JC.

J Med Chem. 2015 May 14;58(9):4087. doi: 10.1021/acs.jmedchem.5b00591. Epub 2015 Apr 22. No abstract available.


Recurrence rates after EMR of large sessile serrated polyps.

Rex KD, Vemulapalli KC, Rex DK.

Gastrointest Endosc. 2015 Sep;82(3):538-41. doi: 10.1016/j.gie.2015.01.025. Epub 2015 Apr 4.


Discovery of potent and selective 8-fluorotriazolopyridine c-Met inhibitors.

Peterson EA, Teffera Y, Albrecht BK, Bauer D, Bellon SF, Boezio A, Boezio C, Broome MA, Choquette D, Copeland KW, Dussault I, Lewis R, Lin MH, Lohman J, Liu J, Potashman M, Rex K, Shimanovich R, Whittington DA, Vaida KR, Harmange JC.

J Med Chem. 2015 Mar 12;58(5):2417-30. doi: 10.1021/jm501913a. Epub 2015 Mar 3. Erratum in: J Med Chem. 2015 May 14;58(9):4087.


One-carbon metabolic pathway rewiring in Escherichia coli reveals an evolutionary advantage of 10-formyltetrahydrofolate synthetase (Fhs) in survival under hypoxia.

Sah S, Aluri S, Rex K, Varshney U.

J Bacteriol. 2015 Feb 15;197(4):717-26. doi: 10.1128/JB.02365-14. Epub 2014 Dec 1.


A national study on weight classes among children in Greenland at school entry.

Rex KF, Larsen NH, Rex H, Niclasen B, Pedersen ML.

Int J Circumpolar Health. 2014 Oct 20;73. doi: 10.3402/ijch.v73.25537. eCollection 2014.


Circadian polymorphisms in night owls, in bipolars, and in non-24-hour sleep cycles.

Kripke DF, Klimecki WT, Nievergelt CM, Rex KM, Murray SS, Shekhtman T, Tranah GJ, Loving RT, Lee HJ, Rhee MK, Shadan FF, Poceta JS, Jamil SM, Kline LE, Kelsoe JR.

Psychiatry Investig. 2014 Oct;11(4):345-62. doi: 10.4306/pi.2014.11.4.345. Epub 2014 Oct 20.


Species undersampling in tropical bat surveys: effects on emerging biodiversity patterns.

Meyer CF, Aguiar LM, Aguirre LF, Baumgarten J, Clarke FM, Cosson JF, Estrada Villegas S, Fahr J, Faria D, Furey N, Henry M, Jenkins RK, Kunz TH, Cristina MacSwiney González M, Moya I, Pons JM, Racey PA, Rex K, Sampaio EM, Stoner KE, Voigt CC, von Staden D, Weise CD, Kalko EK.

J Anim Ecol. 2015 Jan;84(1):113-23. doi: 10.1111/1365-2656.12261. Epub 2014 Jul 22.


Forty-five year trends in overweight and obesity in an indigenous arctic Inuit Society in transition and spatiotemporal trends.

Andersen S, Rex KF, Noahsen P, Sørensen HC, Larsen NH, Mulvad G, Laurberg P.

Am J Hum Biol. 2014 Jul-Aug;26(4):511-7. doi: 10.1002/ajhb.22556. Epub 2014 May 2.


A genetic analysis of the functional interactions within Mycobacterium tuberculosis single-stranded DNA binding protein.

Rex K, Bharti SK, Sah S, Varshney U.

PLoS One. 2014 Apr 10;9(4):e94669. doi: 10.1371/journal.pone.0094669. eCollection 2014.


Hypersensitivity of hypoxia grown Mycobacterium smegmatis to DNA damaging agents: implications of the DNA repair deficiencies in attenuation of mycobacteria.

Rex K, Kurthkoti K, Varshney U.

Mech Ageing Dev. 2013 Oct;134(10):516-22. doi: 10.1016/j.mad.2013.08.006. Epub 2013 Sep 4.


Sphingosine kinase activity is not required for tumor cell viability.

Rex K, Jeffries S, Brown ML, Carlson T, Coxon A, Fajardo F, Frank B, Gustin D, Kamb A, Kassner PD, Li S, Li Y, Morgenstern K, Plant M, Quon K, Ruefli-Brasse A, Schmidt J, Swearingen E, Walker N, Wang Z, Watson JE, Wickramasinghe D, Wong M, Xu G, Wesche H.

PLoS One. 2013 Jul 5;8(7):e68328. doi: 10.1371/journal.pone.0068328. Print 2013.


Structure guided design of a series of sphingosine kinase (SphK) inhibitors.

Gustin DJ, Li Y, Brown ML, Min X, Schmitt MJ, Wanska M, Wang X, Connors R, Johnstone S, Cardozo M, Cheng AC, Jeffries S, Franks B, Li S, Shen S, Wong M, Wesche H, Xu G, Carlson TJ, Plant M, Morgenstern K, Rex K, Schmitt J, Coxon A, Walker N, Kayser F, Wang Z.

Bioorg Med Chem Lett. 2013 Aug 15;23(16):4608-16. doi: 10.1016/j.bmcl.2013.06.030. Epub 2013 Jun 20.


FMR1, circadian genes and depression: suggestive associations or false discovery?

Kripke DF, Nievergelt CM, Tranah GJ, Murray SS, Rex KM, Grizas AP, Hahn EK, Lee HJ, Kelsoe JR, Kline LE.

J Circadian Rhythms. 2013 Mar 23;11(1):3. doi: 10.1186/1740-3391-11-3.


Evaluation of the antitumor effects of rilotumumab by PET imaging in a U-87 MG mouse xenograft model.

Rex K, Lewis XZ, Gobalakrishnan S, Glaus C, Silva MD, Radinsky R, Burgess TL, Gambhir SS, Coxon A.

Nucl Med Biol. 2013 May;40(4):458-63. doi: 10.1016/j.nucmedbio.2013.01.004. Epub 2013 Feb 28.


Evaluation of two circadian rhythm questionnaires for screening for the delayed sleep phase disorder.

Rhee MK, Lee HJ, Rex KM, Kripke DF.

Psychiatry Investig. 2012 Sep;9(3):236-44. Epub 2012 Sep 6.


Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors.

Bode CM, Boezio AA, Albrecht BK, Bellon SF, Berry L, Broome MA, Choquette D, Dussault I, Lewis RT, Lin MH, Rex K, Whittington DA, Yang Y, Harmange JC.

Bioorg Med Chem Lett. 2012 Jun 15;22(12):4089-93. doi: 10.1016/j.bmcl.2012.04.072. Epub 2012 Apr 25.


Structure-based design of novel class II c-Met inhibitors: 1. Identification of pyrazolone-based derivatives.

Norman MH, Liu L, Lee M, Xi N, Fellows I, D'Angelo ND, Dominguez C, Rex K, Bellon SF, Kim TS, Dussault I.

J Med Chem. 2012 Mar 8;55(5):1858-67. doi: 10.1021/jm201330u. Epub 2012 Feb 24.


Population-based comparative epidemiological survey of hepatitis B, D, and C among Inuit migrated to Denmark and in high endemic Greenland.

Rex KF, Krarup HB, Laurberg P, Andersen S.

Scand J Gastroenterol. 2012 Jun;47(6):692-701. doi: 10.3109/00365521.2011.634026. Epub 2012 Jan 10.


Chimeras of Escherichia coli and Mycobacterium tuberculosis single-stranded DNA binding proteins: characterization and function in Escherichia coli.

Bharti SK, Rex K, Sreedhar P, Krishnan N, Varshney U.

PLoS One. 2011;6(12):e27216. doi: 10.1371/journal.pone.0027216. Epub 2011 Dec 12.


Morphological innovation, diversification and invasion of a new adaptive zone.

Dumont ER, Dávalos LM, Goldberg A, Santana SE, Rex K, Voigt CC.

Proc Biol Sci. 2012 May 7;279(1734):1797-805. doi: 10.1098/rspb.2011.2005. Epub 2011 Nov 23.


Polymorphisms in melatonin synthesis pathways: possible influences on depression.

Kripke DF, Nievergelt CM, Tranah GJ, Murray SS, McCarthy MJ, Rex KM, Parimi N, Kelsoe JR.

J Circadian Rhythms. 2011 Aug 9;9:8. doi: 10.1186/1740-3391-9-8.


Delayed sleep phase syndrome is related to seasonal affective disorder.

Lee HJ, Rex KM, Nievergelt CM, Kelsoe JR, Kripke DF.

J Affect Disord. 2011 Oct;133(3):573-9. doi: 10.1016/j.jad.2011.04.046. Epub 2011 May 20.


Context-dependent role of angiopoietin-1 inhibition in the suppression of angiogenesis and tumor growth: implications for AMG 386, an angiopoietin-1/2-neutralizing peptibody.

Coxon A, Bready J, Min H, Kaufman S, Leal J, Yu D, Lee TA, Sun JR, Estrada J, Bolon B, McCabe J, Wang L, Rex K, Caenepeel S, Hughes P, Cordover D, Kim H, Han SJ, Michaels ML, Hsu E, Shimamoto G, Cattley R, Hurh E, Nguyen L, Wang SX, Ndifor A, Hayward IJ, Falcón BL, McDonald DM, Li L, Boone T, Kendall R, Radinsky R, Oliner JD.

Mol Cancer Ther. 2010 Oct;9(10):2641-51. doi: 10.1158/1535-7163.MCT-10-0213.


Mortality related to actigraphic long and short sleep.

Kripke DF, Langer RD, Elliott JA, Klauber MR, Rex KM.

Sleep Med. 2011 Jan;12(1):28-33. doi: 10.1016/j.sleep.2010.04.016. Epub 2010 Sep 25.


Weak evidence of bright light effects on human LH and FSH.

Kripke DF, Elliott JA, Youngstedt SD, Parry BL, Hauger RL, Rex KM.

J Circadian Rhythms. 2010 May 11;8:5. doi: 10.1186/1740-3391-8-5.


Therapeutic potential of hepatocyte growth factor/scatter factor neutralizing antibodies: inhibition of tumor growth in both autocrine and paracrine hepatocyte growth factor/scatter factor:c-Met-driven models of leiomyosarcoma.

Gao CF, Xie Q, Zhang YW, Su Y, Zhao P, Cao B, Furge K, Sun J, Rex K, Osgood T, Coxon A, Burgess TL, Vande Woude GF.

Mol Cancer Ther. 2009 Oct;8(10):2803-10. doi: 10.1158/1535-7163.MCT-09-0125.


Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors.

Boezio AA, Berry L, Albrecht BK, Bauer D, Bellon SF, Bode C, Chen A, Choquette D, Dussault I, Fang M, Hirai S, Kaplan-Lefko P, Larrow JF, Lin MH, Lohman J, Potashman MH, Qu Y, Rex K, Santostefano M, Shah K, Shimanovich R, Springer SK, Teffera Y, Yang Y, Zhang Y, Harmange JC.

Bioorg Med Chem Lett. 2009 Nov 15;19(22):6307-12. doi: 10.1016/j.bmcl.2009.09.096. Epub 2009 Sep 27. Erratum in: Bioorg Med Chem Lett. 2010 Jan 15;20(2):773. Fang, Mei [added]; Qu, Yusheng [added].


Soluble c-Met receptors inhibit phosphorylation of c-Met and growth of hepatocyte growth factor: c-Met-dependent tumors in animal models.

Coxon A, Rex K, Meyer S, Sun J, Sun J, Chen Q, Radinsky R, Kendall R, Burgess TL.

Mol Cancer Ther. 2009 May;8(5):1119-25. doi: 10.1158/1535-7163.MCT-08-1032. Epub 2009 May 12.


Broad antitumor activity in breast cancer xenografts by motesanib, a highly selective, oral inhibitor of vascular endothelial growth factor, platelet-derived growth factor, and Kit receptors.

Coxon A, Bush T, Saffran D, Kaufman S, Belmontes B, Rex K, Hughes P, Caenepeel S, Rottman JB, Tasker A, Patel V, Kendall R, Radinsky R, Polverino A.

Clin Cancer Res. 2009 Jan 1;15(1):110-8. doi: 10.1158/1078-0432.CCR-08-1155.


Design, synthesis, and biological evaluation of potent c-Met inhibitors.

D'Angelo ND, Bellon SF, Booker SK, Cheng Y, Coxon A, Dominguez C, Fellows I, Hoffman D, Hungate R, Kaplan-Lefko P, Lee MR, Li C, Liu L, Rainbeau E, Reider PJ, Rex K, Siegmund A, Sun Y, Tasker AS, Xi N, Xu S, Yang Y, Zhang Y, Burgess TL, Dussault I, Kim TS.

J Med Chem. 2008 Sep 25;51(18):5766-79. doi: 10.1021/jm8006189.


Identification of a novel recepteur d'origine nantais/c-met small-molecule kinase inhibitor with antitumor activity in vivo.

Zhang Y, Kaplan-Lefko PJ, Rex K, Yang Y, Moriguchi J, Osgood T, Mattson B, Coxon A, Reese M, Kim TS, Lin J, Chen A, Burgess TL, Dussault I.

Cancer Res. 2008 Aug 15;68(16):6680-7. doi: 10.1158/0008-5472.CAN-07-6782.


Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458).

Liu L, Siegmund A, Xi N, Kaplan-Lefko P, Rex K, Chen A, Lin J, Moriguchi J, Berry L, Huang L, Teffera Y, Yang Y, Zhang Y, Bellon SF, Lee M, Shimanovich R, Bak A, Dominguez C, Norman MH, Harmange JC, Dussault I, Kim TS.

J Med Chem. 2008 Jul 10;51(13):3688-91. doi: 10.1021/jm800401t. Epub 2008 Jun 14.


Nutrient routing in omnivorous animals tracked by stable carbon isotopes in tissue and exhaled breath.

Voigt CC, Rex K, Michener RH, Speakman JR.

Oecologia. 2008 Aug;157(1):31-40. doi: 10.1007/s00442-008-1057-3. Epub 2008 May 22.


Delayed sleep phase cases and controls.

Kripke DF, Rex KM, Ancoli-Israel S, Nievergelt CM, Klimecki W, Kelsoe JR.

J Circadian Rhythms. 2008 Apr 29;6:6. doi: 10.1186/1740-3391-6-6.

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