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Items: 1 to 50 of 227

1.

Mutant p53 induces a hypoxia transcriptional program in gastric and esophageal adenocarcinoma.

Sethi N, Kikuchi O, McFarland J, Zhang Y, Chung M, Kafker N, Islam M, Lampson B, Chakraborty A, Kaelin WG Jr, Bass AJ.

JCI Insight. 2019 Aug 8;4(15). pii: 128439. doi: 10.1172/jci.insight.128439. eCollection 2019 Aug 8.

2.

EglN3 hydroxylase stabilizes BIM-EL linking VHL type 2C mutations to pheochromocytoma pathogenesis and chemotherapy resistance.

Li S, Rodriguez J, Li W, Bullova P, Fell SM, Surova O, Westerlund I, Topcic D, Bergsland M, Stenman A, Muhr J, Nistér M, Holmberg J, Juhlin CC, Larsson C, von Kriegsheim A, Kaelin WG Jr, Schlisio S.

Proc Natl Acad Sci U S A. 2019 Aug 20;116(34):16997-17006. doi: 10.1073/pnas.1900748116. Epub 2019 Aug 2.

PMID:
31375625
3.

Histone demethylase KDM6A directly senses oxygen to control chromatin and cell fate.

Chakraborty AA, Laukka T, Myllykoski M, Ringel AE, Booker MA, Tolstorukov MY, Meng YJ, Meier SR, Jennings RB, Creech AL, Herbert ZT, McBrayer SK, Olenchock BA, Jaffe JD, Haigis MC, Beroukhim R, Signoretti S, Koivunen P, Kaelin WG Jr.

Science. 2019 Mar 15;363(6432):1217-1222. doi: 10.1126/science.aaw1026. Epub 2019 Mar 14.

PMID:
30872525
4.

Deubiquitinases Maintain Protein Homeostasis and Survival of Cancer Cells upon Glutathione Depletion.

Harris IS, Endress JE, Coloff JL, Selfors LM, McBrayer SK, Rosenbluth JM, Takahashi N, Dhakal S, Koduri V, Oser MG, Schauer NJ, Doherty LM, Hong AL, Kang YP, Younger ST, Doench JG, Hahn WC, Buhrlage SJ, DeNicola GM, Kaelin WG Jr, Brugge JS.

Cell Metab. 2019 May 7;29(5):1166-1181.e6. doi: 10.1016/j.cmet.2019.01.020. Epub 2019 Feb 21.

PMID:
30799286
5.

Peptidic degron for IMiD-induced degradation of heterologous proteins.

Koduri V, McBrayer SK, Liberzon E, Wang AC, Briggs KJ, Cho H, Kaelin WG Jr.

Proc Natl Acad Sci U S A. 2019 Feb 12;116(7):2539-2544. doi: 10.1073/pnas.1818109116. Epub 2019 Jan 25.

6.

Cells Lacking the RB1 Tumor Suppressor Gene Are Hyperdependent on Aurora B Kinase for Survival.

Oser MG, Fonseca R, Chakraborty AA, Brough R, Spektor A, Jennings RB, Flaifel A, Novak JS, Gulati A, Buss E, Younger ST, McBrayer SK, Cowley GS, Bonal DM, Nguyen QD, Brulle-Soumare L, Taylor P, Cairo S, Ryan CJ, Pease EJ, Maratea K, Travers J, Root DE, Signoretti S, Pellman D, Ashton S, Lord CJ, Barry ST, Kaelin WG Jr.

Cancer Discov. 2019 Feb;9(2):230-247. doi: 10.1158/2159-8290.CD-18-0389. Epub 2018 Oct 29.

7.

BRCA1-IRIS promotes human tumor progression through PTEN blockade and HIF-1α activation.

Li AG, Murphy EC, Culhane AC, Powell E, Wang H, Bronson RT, Von T, Giobbie-Hurder A, Gelman RS, Briggs KJ, Piwnica-Worms H, Zhao JJ, Kung AL, Kaelin WG Jr, Livingston DM.

Proc Natl Acad Sci U S A. 2018 Oct 9;115(41):E9600-E9609. doi: 10.1073/pnas.1807112115. Epub 2018 Sep 25.

8.

Transaminase Inhibition by 2-Hydroxyglutarate Impairs Glutamate Biosynthesis and Redox Homeostasis in Glioma.

McBrayer SK, Mayers JR, DiNatale GJ, Shi DD, Khanal J, Chakraborty AA, Sarosiek KA, Briggs KJ, Robbins AK, Sewastianik T, Shareef SJ, Olenchock BA, Parker SJ, Tateishi K, Spinelli JB, Islam M, Haigis MC, Looper RE, Ligon KL, Bernstein BE, Carrasco RD, Cahill DP, Asara JM, Metallo CM, Yennawar NH, Vander Heiden MG, Kaelin WG Jr.

Cell. 2018 Sep 20;175(1):101-116.e25. doi: 10.1016/j.cell.2018.08.038. Epub 2018 Sep 13.

PMID:
30220459
9.

VHL substrate transcription factor ZHX2 as an oncogenic driver in clear cell renal cell carcinoma.

Zhang J, Wu T, Simon J, Takada M, Saito R, Fan C, Liu XD, Jonasch E, Xie L, Chen X, Yao X, Teh BT, Tan P, Zheng X, Li M, Lawrence C, Fan J, Geng J, Liu X, Hu L, Wang J, Liao C, Hong K, Zurlo G, Parker JS, Auman JT, Perou CM, Rathmell WK, Kim WY, Kirschner MW, Kaelin WG Jr, Baldwin AS, Zhang Q.

Science. 2018 Jul 20;361(6399):290-295. doi: 10.1126/science.aap8411.

10.

Autochthonous tumors driven by Rb1 loss have an ongoing requirement for the RBP2 histone demethylase.

McBrayer SK, Olenchock BA, DiNatale GJ, Shi DD, Khanal J, Jennings RB, Novak JS, Oser MG, Robbins AK, Modiste R, Bonal D, Moslehi J, Bronson RT, Neuberg D, Nguyen QD, Signoretti S, Losman JA, Kaelin WG Jr.

Proc Natl Acad Sci U S A. 2018 Apr 17;115(16):E3741-E3748. doi: 10.1073/pnas.1716029115. Epub 2018 Apr 2.

11.

HIF2 Inhibitor Joins the Kidney Cancer Armamentarium.

Kaelin WG Jr.

J Clin Oncol. 2018 Mar 20;36(9):908-910. doi: 10.1200/JCO.2017.77.5254. Epub 2018 Jan 31. No abstract available.

PMID:
29384723
12.

Genomic correlates of response to immune checkpoint therapies in clear cell renal cell carcinoma.

Miao D, Margolis CA, Gao W, Voss MH, Li W, Martini DJ, Norton C, Bossé D, Wankowicz SM, Cullen D, Horak C, Wind-Rotolo M, Tracy A, Giannakis M, Hodi FS, Drake CG, Ball MW, Allaf ME, Snyder A, Hellmann MD, Ho T, Motzer RJ, Signoretti S, Kaelin WG Jr, Choueiri TK, Van Allen EM.

Science. 2018 Feb 16;359(6377):801-806. doi: 10.1126/science.aan5951. Epub 2018 Jan 4.

13.

Senator McCain and Our Shared Humanity.

Kaelin WG Jr.

Am J Med. 2018 Mar;131(3):216-217. doi: 10.1016/j.amjmed.2017.11.028. Epub 2017 Dec 8. No abstract available.

PMID:
29229468
14.

Climate Change: What Would Lincoln Do?

Kaelin WG Jr.

JAMA. 2017 Aug 15;318(7):611. doi: 10.1001/jama.2017.6999. No abstract available.

PMID:
28810027
15.

The VHL Tumor Suppressor Gene: Insights into Oxygen Sensing and Cancer.

Kaelin WG Jr.

Trans Am Clin Climatol Assoc. 2017;128:298-307. Review.

16.

HIF activation causes synthetic lethality between the VHL tumor suppressor and the EZH1 histone methyltransferase.

Chakraborty AA, Nakamura E, Qi J, Creech A, Jaffe JD, Paulk J, Novak JS, Nagulapalli K, McBrayer SK, Cowley GS, Pineda J, Song J, Wang YE, Carr SA, Root DE, Signoretti S, Bradner JE, Kaelin WG Jr.

Sci Transl Med. 2017 Jul 12;9(398). pii: eaal5272. doi: 10.1126/scitranslmed.aal5272.

17.

The EGLN-HIF O2-Sensing System: Multiple Inputs and Feedbacks.

Ivan M, Kaelin WG Jr.

Mol Cell. 2017 Jun 15;66(6):772-779. doi: 10.1016/j.molcel.2017.06.002. Review.

18.

Publish houses of brick, not mansions of straw.

Kaelin WG Jr.

Nature. 2017 May 23;545(7655):387. doi: 10.1038/545387a. No abstract available.

PMID:
28541345
19.

Common pitfalls in preclinical cancer target validation.

Kaelin WG Jr.

Nat Rev Cancer. 2017 Jul;17(7):425-440. doi: 10.1038/nrc.2017.32. Epub 2017 May 19.

PMID:
28524181
20.

Inactivation of the PBRM1 tumor suppressor gene amplifies the HIF-response in VHL-/- clear cell renal carcinoma.

Gao W, Li W, Xiao T, Liu XS, Kaelin WG Jr.

Proc Natl Acad Sci U S A. 2017 Jan 31;114(5):1027-1032. doi: 10.1073/pnas.1619726114. Epub 2017 Jan 12.

21.

Targeting HIF2 in Clear Cell Renal Cell Carcinoma.

Cho H, Kaelin WG.

Cold Spring Harb Symp Quant Biol. 2016;81:113-121. doi: 10.1101/sqb.2016.81.030833. Epub 2016 Dec 8. Review.

PMID:
27932568
22.

On-target efficacy of a HIF-2α antagonist in preclinical kidney cancer models.

Cho H, Du X, Rizzi JP, Liberzon E, Chakraborty AA, Gao W, Carvo I, Signoretti S, Bruick RK, Josey JA, Wallace EM, Kaelin WG.

Nature. 2016 Nov 3;539(7627):107-111. doi: 10.1038/nature19795. Epub 2016 Sep 5.

23.

PHD3 Loss in Cancer Enables Metabolic Reliance on Fatty Acid Oxidation via Deactivation of ACC2.

German NJ, Yoon H, Yusuf RZ, Murphy JP, Finley LW, Laurent G, Haas W, Satterstrom FK, Guarnerio J, Zaganjor E, Santos D, Pandolfi PP, Beck AH, Gygi SP, Scadden DT, Kaelin WG Jr, Haigis MC.

Mol Cell. 2016 Sep 15;63(6):1006-20. doi: 10.1016/j.molcel.2016.08.014.

24.

Pathways for Oxygen Regulation and Homeostasis: The 2016 Albert Lasker Basic Medical Research Award.

Kaelin WG Jr, Ratcliffe PJ, Semenza GL.

JAMA. 2016 Sep 27;316(12):1252-3. doi: 10.1001/jama.2016.12386. No abstract available.

PMID:
27622845
25.

pVHL suppresses kinase activity of Akt in a proline-hydroxylation-dependent manner.

Guo J, Chakraborty AA, Liu P, Gan W, Zheng X, Inuzuka H, Wang B, Zhang J, Zhang L, Yuan M, Novak J, Cheng JQ, Toker A, Signoretti S, Zhang Q, Asara JM, Kaelin WG Jr, Wei W.

Science. 2016 Aug 26;353(6302):929-32. doi: 10.1126/science.aad5755.

26.

Paracrine Induction of HIF by Glutamate in Breast Cancer: EglN1 Senses Cysteine.

Briggs KJ, Koivunen P, Cao S, Backus KM, Olenchock BA, Patel H, Zhang Q, Signoretti S, Gerfen GJ, Richardson AL, Witkiewicz AK, Cravatt BF, Clardy J, Kaelin WG Jr.

Cell. 2016 Jun 30;166(1):126-39. doi: 10.1016/j.cell.2016.05.042.

27.

EGLN1 Inhibition and Rerouting of α-Ketoglutarate Suffice for Remote Ischemic Protection.

Olenchock BA, Moslehi J, Baik AH, Davidson SM, Williams J, Gibson WJ, Chakraborty AA, Pierce KA, Miller CM, Hanse EA, Kelekar A, Sullivan LB, Wagers AJ, Clish CB, Vander Heiden MG, Kaelin WG Jr.

Cell. 2016 Apr 7;165(2):497. doi: 10.1016/j.cell.2016.03.037. No abstract available.

28.

EGLN1 Inhibition and Rerouting of α-Ketoglutarate Suffice for Remote Ischemic Protection.

Olenchock BA, Moslehi J, Baik AH, Davidson SM, Williams J, Gibson WJ, Chakraborty AA, Pierce KA, Miller CM, Hanse EA, Kelekar A, Sullivan LB, Wagers AJ, Clish CB, Vander Heiden MG, Kaelin WG Jr.

Cell. 2016 Feb 25;164(5):884-95. doi: 10.1016/j.cell.2016.02.006. Erratum in: Cell. 2016 Apr 7;165(2):497.

29.

Fumarate and Succinate Regulate Expression of Hypoxia-inducible Genes via TET Enzymes.

Laukka T, Mariani CJ, Ihantola T, Cao JZ, Hokkanen J, Kaelin WG Jr, Godley LA, Koivunen P.

J Biol Chem. 2016 Feb 19;291(8):4256-65. doi: 10.1074/jbc.M115.688762. Epub 2015 Dec 23.

30.

Peptidic degron in EID1 is recognized by an SCF E3 ligase complex containing the orphan F-box protein FBXO21.

Zhang C, Li X, Adelmant G, Dobbins J, Geisen C, Oser MG, Wucherpfenning KW, Marto JA, Kaelin WG Jr.

Proc Natl Acad Sci U S A. 2015 Dec 15;112(50):15372-7. doi: 10.1073/pnas.1522006112. Epub 2015 Dec 2.

31.

Treatment Response Assessment in IDH-Mutant Glioma Patients by Noninvasive 3D Functional Spectroscopic Mapping of 2-Hydroxyglutarate.

Andronesi OC, Loebel F, Bogner W, Marjańska M, Vander Heiden MG, Iafrate AJ, Dietrich J, Batchelor TT, Gerstner ER, Kaelin WG, Chi AS, Rosen BR, Cahill DP.

Clin Cancer Res. 2016 Apr 1;22(7):1632-41. doi: 10.1158/1078-0432.CCR-15-0656. Epub 2015 Nov 3.

32.

EglN2 associates with the NRF1-PGC1α complex and controls mitochondrial function in breast cancer.

Zhang J, Wang C, Chen X, Takada M, Fan C, Zheng X, Wen H, Liu Y, Wang C, Pestell RG, Aird KM, Kaelin WG Jr, Liu XS, Zhang Q.

EMBO J. 2015 Dec 2;34(23):2953-70. doi: 10.15252/embj.201591437. Epub 2015 Oct 22.

33.

Inhibition of the oxygen sensor PHD2 in the liver improves survival in lactic acidosis by activating the Cori cycle.

Suhara T, Hishiki T, Kasahara M, Hayakawa N, Oyaizu T, Nakanishi T, Kubo A, Morisaki H, Kaelin WG Jr, Suematsu M, Minamishima YA.

Proc Natl Acad Sci U S A. 2015 Sep 15;112(37):11642-7. doi: 10.1073/pnas.1515872112. Epub 2015 Aug 31.

34.

DisABLing kidney cancers caused by fumarate hydratase mutations.

Kaelin WG Jr.

Cancer Cell. 2014 Dec 8;26(6):779-780. doi: 10.1016/j.ccell.2014.11.022.

35.

A genetic mechanism for Tibetan high-altitude adaptation.

Lorenzo FR, Huff C, Myllymäki M, Olenchock B, Swierczek S, Tashi T, Gordeuk V, Wuren T, Ri-Li G, McClain DA, Khan TM, Koul PA, Guchhait P, Salama ME, Xing J, Semenza GL, Liberzon E, Wilson A, Simonson TS, Jorde LB, Kaelin WG Jr, Koivunen P, Prchal JT.

Nat Genet. 2014 Sep;46(9):951-6. doi: 10.1038/ng.3067. Epub 2014 Aug 17.

36.

Phosphorylation of ETS1 by Src family kinases prevents its recognition by the COP1 tumor suppressor.

Lu G, Zhang Q, Huang Y, Song J, Tomaino R, Ehrenberger T, Lim E, Liu W, Bronson RT, Bowden M, Brock J, Krop IE, Dillon DA, Gygi SP, Mills GB, Richardson AL, Signoretti S, Yaffe MB, Kaelin WG Jr.

Cancer Cell. 2014 Aug 11;26(2):222-34. doi: 10.1016/j.ccr.2014.06.026.

37.

Prolyl hydroxylation by EglN2 destabilizes FOXO3a by blocking its interaction with the USP9x deubiquitinase.

Zheng X, Zhai B, Koivunen P, Shin SJ, Lu G, Liu J, Geisen C, Chakraborty AA, Moslehi JJ, Smalley DM, Wei X, Chen X, Chen Z, Beres JM, Zhang J, Tsao JL, Brenner MC, Zhang Y, Fan C, DePinho RA, Paik J, Gygi SP, Kaelin WG Jr, Zhang Q.

Genes Dev. 2014 Jul 1;28(13):1429-44. doi: 10.1101/gad.242131.114.

38.

A phase I study of cabozantinib (XL184) in patients with renal cell cancer.

Choueiri TK, Pal SK, McDermott DF, Morrissey S, Ferguson KC, Holland J, Kaelin WG, Dutcher JP.

Ann Oncol. 2014 Aug;25(8):1603-8. doi: 10.1093/annonc/mdu184. Epub 2014 May 14.

39.

D-2-hydroxyglutarate produced by mutant IDH2 causes cardiomyopathy and neurodegeneration in mice.

Akbay EA, Moslehi J, Christensen CL, Saha S, Tchaicha JH, Ramkissoon SH, Stewart KM, Carretero J, Kikuchi E, Zhang H, Cohoon TJ, Murray S, Liu W, Uno K, Fisch S, Jones K, Gurumurthy S, Gliser C, Choe S, Keenan M, Son J, Stanley I, Losman JA, Padera R, Bronson RT, Asara JM, Abdel-Wahab O, Amrein PC, Fathi AT, Danial NN, Kimmelman AC, Kung AL, Ligon KL, Yen KE, Kaelin WG Jr, Bardeesy N, Wong KK.

Genes Dev. 2014 Mar 1;28(5):479-90. doi: 10.1101/gad.231233.113.

40.

SQSTM1 is a pathogenic target of 5q copy number gains in kidney cancer.

Li L, Shen C, Nakamura E, Ando K, Signoretti S, Beroukhim R, Cowley GS, Lizotte P, Liberzon E, Bair S, Root DE, Tamayo P, Tsherniak A, Cheng SC, Tabak B, Jacobsen A, Hakimi AA, Schultz N, Ciriello G, Sander C, Hsieh JJ, Kaelin WG Jr.

Cancer Cell. 2013 Dec 9;24(6):738-50. doi: 10.1016/j.ccr.2013.10.025.

41.

The myeloma drug lenalidomide promotes the cereblon-dependent destruction of Ikaros proteins.

Lu G, Middleton RE, Sun H, Naniong M, Ott CJ, Mitsiades CS, Wong KK, Bradner JE, Kaelin WG Jr.

Science. 2014 Jan 17;343(6168):305-9. doi: 10.1126/science.1244917. Epub 2013 Nov 29.

42.

What a difference a hydroxyl makes: mutant IDH, (R)-2-hydroxyglutarate, and cancer.

Losman JA, Kaelin WG Jr.

Genes Dev. 2013 Apr 15;27(8):836-52. doi: 10.1101/gad.217406.113. Review.

43.

Influence of metabolism on epigenetics and disease.

Kaelin WG Jr, McKnight SL.

Cell. 2013 Mar 28;153(1):56-69. doi: 10.1016/j.cell.2013.03.004. Review.

44.

(R)-2-hydroxyglutarate is sufficient to promote leukemogenesis and its effects are reversible.

Losman JA, Looper RE, Koivunen P, Lee S, Schneider RK, McMahon C, Cowley GS, Root DE, Ebert BL, Kaelin WG Jr.

Science. 2013 Mar 29;339(6127):1621-5. doi: 10.1126/science.1231677. Epub 2013 Feb 7.

45.

Coordinated repression of cell cycle genes by KDM5A and E2F4 during differentiation.

Beshiri ML, Holmes KB, Richter WF, Hess S, Islam AB, Yan Q, Plante L, Litovchick L, Gévry N, Lopez-Bigas N, Kaelin WG Jr, Benevolenskaya EV.

Proc Natl Acad Sci U S A. 2012 Nov 6;109(45):18499-504. doi: 10.1073/pnas.1216724109. Epub 2012 Oct 23.

46.

Molecular biology. Use and abuse of RNAi to study mammalian gene function.

Kaelin WG Jr.

Science. 2012 Jul 27;337(6093):421-2. doi: 10.1126/science.1225787. No abstract available.

47.

The VHL/HIF axis in clear cell renal carcinoma.

Shen C, Kaelin WG Jr.

Semin Cancer Biol. 2013 Feb;23(1):18-25. doi: 10.1016/j.semcancer.2012.06.001. Epub 2012 Jun 13. Review.

48.

Treatment of erythropoietin deficiency in mice with systemically administered siRNA.

Querbes W, Bogorad RL, Moslehi J, Wong J, Chan AY, Bulgakova E, Kuchimanchi S, Akinc A, Fitzgerald K, Koteliansky V, Kaelin WG Jr.

Blood. 2012 Aug 30;120(9):1916-22. doi: 10.1182/blood-2012-04-423715. Epub 2012 May 18.

49.

Transformation by the (R)-enantiomer of 2-hydroxyglutarate linked to EGLN activation.

Koivunen P, Lee S, Duncan CG, Lopez G, Lu G, Ramkissoon S, Losman JA, Joensuu P, Bergmann U, Gross S, Travins J, Weiss S, Looper R, Ligon KL, Verhaak RG, Yan H, Kaelin WG Jr.

Nature. 2012 Feb 15;483(7390):484-8. doi: 10.1038/nature10898.

50.

Cancer and altered metabolism: potential importance of hypoxia-inducible factor and 2-oxoglutarate-dependent dioxygenases.

Kaelin WG Jr.

Cold Spring Harb Symp Quant Biol. 2011;76:335-45. doi: 10.1101/sqb.2011.76.010975. Epub 2011 Nov 16. Review.

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