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Items: 18


Structural Basis and Kinetic Pathway of RBM39 Recruitment to DCAF15 by a Sulfonamide Molecular Glue E7820.

Du X, Volkov OA, Czerwinski RM, Tan H, Huerta C, Morton ER, Rizzi JP, Wehn PM, Xu R, Nijhawan D, Wallace EM.

Structure. 2019 Nov 5;27(11):1625-1633.e3. doi: 10.1016/j.str.2019.10.005.


3-[(1S,2S,3R)-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma.

Xu R, Wang K, Rizzi JP, Huang H, Grina JA, Schlachter ST, Wang B, Wehn PM, Yang H, Dixon DD, Czerwinski RM, Du X, Ged EL, Han G, Tan H, Wong T, Xie S, Josey JA, Wallace EM.

J Med Chem. 2019 Aug 8;62(15):6876-6893. doi: 10.1021/acs.jmedchem.9b00719. Epub 2019 Jul 8.


Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate ( S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385).

Wehn PM, Rizzi JP, Dixon DD, Grina JA, Schlachter ST, Wang B, Xu R, Yang H, Du X, Han G, Wang K, Cao Z, Cheng T, Czerwinski RM, Goggin BS, Huang H, Halfmann MM, Maddie MA, Morton EL, Olive SR, Tan H, Xie S, Wong T, Josey JA, Wallace EM.

J Med Chem. 2018 Nov 8;61(21):9691-9721. doi: 10.1021/acs.jmedchem.8b01196. Epub 2018 Oct 18.


Targeting renal cell carcinoma with a HIF-2 antagonist.

Chen W, Hill H, Christie A, Kim MS, Holloman E, Pavia-Jimenez A, Homayoun F, Ma Y, Patel N, Yell P, Hao G, Yousuf Q, Joyce A, Pedrosa I, Geiger H, Zhang H, Chang J, Gardner KH, Bruick RK, Reeves C, Hwang TH, Courtney K, Frenkel E, Sun X, Zojwalla N, Wong T, Rizzi JP, Wallace EM, Josey JA, Xie Y, Xie XJ, Kapur P, McKay RM, Brugarolas J.

Nature. 2016 Nov 3;539(7627):112-117. doi: 10.1038/nature19796. Epub 2016 Sep 5.


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.


A Small-Molecule Antagonist of HIF2α Is Efficacious in Preclinical Models of Renal Cell Carcinoma.

Wallace EM, Rizzi JP, Han G, Wehn PM, Cao Z, Du X, Cheng T, Czerwinski RM, Dixon DD, Goggin BS, Grina JA, Halfmann MM, Maddie MA, Olive SR, Schlachter ST, Tan H, Wang B, Wang K, Xie S, Xu R, Yang H, Josey JA.

Cancer Res. 2016 Sep 15;76(18):5491-500. doi: 10.1158/0008-5472.CAN-16-0473. Epub 2016 Sep 6.


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.


Spirocyclic β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: from hit to lowering of cerebrospinal fluid (CSF) amyloid β in a higher species.

Hunt KW, Cook AW, Watts RJ, Clark CT, Vigers G, Smith D, Metcalf AT, Gunawardana IW, Burkard M, Cox AA, Geck Do MK, Dutcher D, Thomas AA, Rana S, Kallan NC, DeLisle RK, Rizzi JP, Regal K, Sammond D, Groneberg R, Siu M, Purkey H, Lyssikatos JP, Marlow A, Liu X, Tang TP.

J Med Chem. 2013 Apr 25;56(8):3379-403. doi: 10.1021/jm4002154. Epub 2013 Apr 16.


Multiple active site corrections for docking and virtual screening.

Vigers GP, Rizzi JP.

J Med Chem. 2004 Jan 1;47(1):80-9.


UK-78,282, a novel piperidine compound that potently blocks the Kv1.3 voltage-gated potassium channel and inhibits human T cell activation.

Hanson DC, Nguyen A, Mather RJ, Rauer H, Koch K, Burgess LE, Rizzi JP, Donovan CB, Bruns MJ, Canniff PC, Cunningham AC, Verdries KA, Mena E, Kath JC, Gutman GA, Cahalan MD, Grissmer S, Chandy KG.

Br J Pharmacol. 1999 Apr;126(8):1707-16.


Inhibition of MMP-1 and MMP-13 with phosphinic acids that exploit binding in the S2 pocket.

Reiter LA, Rizzi JP, Pandit J, Lasut MJ, McGahee SM, Parikh VD, Blake JF, Danley DE, Laird ER, Lopez-Anaya A, Lopresti-Morrow LL, Mansour MN, Martinelli GJ, Mitchell PG, Owens BS, Pauly TA, Reeves LM, Schulte GK, Yocum SA.

Bioorg Med Chem Lett. 1999 Jan 18;9(2):127-32.


The signature sequence of voltage-gated potassium channels projects into the external vestibule.

Aiyar J, Rizzi JP, Gutman GA, Chandy KG.

J Biol Chem. 1996 Dec 6;271(49):31013-6.


Topology of the pore-region of a K+ channel revealed by the NMR-derived structures of scorpion toxins.

Aiyar J, Withka JM, Rizzi JP, Singleton DH, Andrews GC, Lin W, Boyd J, Hanson DC, Simon M, Dethlefs B, et al.

Neuron. 1995 Nov;15(5):1169-81.


Importance of parallel vectors and "hydrophobic collapse" of the aligned aromatic rings: discovery of a potent substance P antagonist.

Desai MC, Vincent LA, Rizzi JP.

J Med Chem. 1994 Dec 9;37(25):4263-6. No abstract available.


Novel thiazolidine-2,4-diones as potent euglycemic agents.

Hulin B, Clark DA, Goldstein SW, McDermott RE, Dambek PJ, Kappeler WH, Lamphere CH, Lewis DM, Rizzi JP.

J Med Chem. 1992 May 15;35(10):1853-64.


Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists.

Rosen T, Nagel AA, Rizzi JP, Ives JL, Daffeh JB, Ganong AH, Guarino K, Heym J, McLean S, Nowakowski JT, et al.

J Med Chem. 1990 Oct;33(10):2715-20.


An initial three-component pharmacophore for specific serotonin-3 receptor ligands.

Rizzi JP, Nagel AA, Rosen T, McLean S, Seeger T.

J Med Chem. 1990 Oct;33(10):2721-5.


Rotationally restricted mimics of rigid molecules: nonspirocyclic hydantoin aldose reductase inhibitors.

Rizzi JP, Schnur RC, Hutson NJ, Kraus KG, Kelbaugh PR.

J Med Chem. 1989 Jun;32(6):1208-13.


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