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Items: 30

1.

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.

PMID:
31693911
2.

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.

PMID:
31282155
3.

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.

PMID:
30289716
4.

Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans.

Thorarensen A, Dowty ME, Banker ME, Juba B, Jussif J, Lin T, Vincent F, Czerwinski RM, Casimiro-Garcia A, Unwalla R, Trujillo JI, Liang S, Balbo P, Che Y, Gilbert AM, Brown MF, Hayward M, Montgomery J, Leung L, Yang X, Soucy S, Hegen M, Coe J, Langille J, Vajdos F, Chrencik J, Telliez JB.

J Med Chem. 2017 Mar 9;60(5):1971-1993. doi: 10.1021/acs.jmedchem.6b01694. Epub 2017 Feb 16.

PMID:
28139931
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.

6.

ATP-mediated kinome selectivity: the missing link in understanding the contribution of individual JAK Kinase isoforms to cellular signaling.

Thorarensen A, Banker ME, Fensome A, Telliez JB, Juba B, Vincent F, Czerwinski RM, Casimiro-Garcia A.

ACS Chem Biol. 2014 Jul 18;9(7):1552-8. doi: 10.1021/cb5002125. Epub 2014 May 28.

PMID:
24814050
7.

Selectively targeting an inactive conformation of interleukin-2-inducible T-cell kinase by allosteric inhibitors.

Han S, Czerwinski RM, Caspers NL, Limburg DC, Ding W, Wang H, Ohren JF, Rajamohan F, McLellan TJ, Unwalla R, Choi C, Parikh MD, Seth N, Edmonds J, Phillips C, Shakya S, Li X, Spaulding V, Hughes S, Cook A, Robinson C, Mathias JP, Navratilova I, Medley QG, Anderson DR, Kurumbail RG, Aulabaugh A.

Biochem J. 2014 Jun 1;460(2):211-22. doi: 10.1042/BJ20131139.

PMID:
24593284
8.

Covalent inhibitors of interleukin-2 inducible T cell kinase (itk) with nanomolar potency in a whole-blood assay.

Zapf CW, Gerstenberger BS, Xing L, Limburg DC, Anderson DR, Caspers N, Han S, Aulabaugh A, Kurumbail R, Shakya S, Li X, Spaulding V, Czerwinski RM, Seth N, Medley QG.

J Med Chem. 2012 Nov 26;55(22):10047-63. doi: 10.1021/jm301190s. Epub 2012 Nov 12.

PMID:
23098091
9.

Kinetic and structural characterization of DmpI from Helicobacter pylori and Archaeoglobus fulgidus, two 4-oxalocrotonate tautomerase family members.

Almrud JJ, Dasgupta R, Czerwinski RM, Kern AD, Hackert ML, Whitman CP.

Bioorg Chem. 2010 Dec;38(6):252-9. doi: 10.1016/j.bioorg.2010.07.002. Epub 2010 Jul 18.

10.
11.

Inactivation of the phenylpyruvate tautomerase activity of macrophage migration inhibitory factor by 2-oxo-4-phenyl-3-butynoate.

Golubkov PA, Johnson WH Jr, Czerwinski RM, Person MD, Wang SC, Whitman CP, Hackert ML.

Bioorg Chem. 2006 Aug;34(4):183-99. Epub 2006 Jun 14.

PMID:
16780921
12.

4-Oxalocrotonate tautomerase, its homologue YwhB, and active vinylpyruvate hydratase: synthesis and evaluation of 2-fluoro substrate analogues.

Johnson WH Jr, Wang SC, Stanley TM, Czerwinski RM, Almrud JJ, Poelarends GJ, Murzin AG, Whitman CP.

Biochemistry. 2004 Aug 17;43(32):10490-501.

PMID:
15301547
13.

Reactions of 4-oxalocrotonate tautomerase and YwhB with 3-halopropiolates: analysis and implications.

Wang SC, Johnson WH Jr, Czerwinski RM, Whitman CP.

Biochemistry. 2004 Jan 27;43(3):748-58.

PMID:
14730980
14.

Catalytically active MAP KAP kinase 2 structures in complex with staurosporine and ADP reveal differences with the autoinhibited enzyme.

Underwood KW, Parris KD, Federico E, Mosyak L, Czerwinski RM, Shane T, Taylor M, Svenson K, Liu Y, Hsiao CL, Wolfrom S, Maguire M, Malakian K, Telliez JB, Lin LL, Kriz RW, Seehra J, Somers WS, Stahl ML.

Structure. 2003 Jun;11(6):627-36.

15.

The crystal structure of YdcE, a 4-oxalocrotonate tautomerase homologue from Escherichia coli, confirms the structural basis for oligomer diversity.

Almrud JJ, Kern AD, Wang SC, Czerwinski RM, Johnson WH Jr, Murzin AG, Hackert ML, Whitman CP.

Biochemistry. 2002 Oct 8;41(40):12010-24.

PMID:
12356301
16.

Identification, characterization, and crystal structure of Bacillus subtilis nicotinic acid mononucleotide adenylyltransferase.

Olland AM, Underwood KW, Czerwinski RM, Lo MC, Aulabaugh A, Bard J, Stahl ML, Somers WS, Sullivan FX, Chopra R.

J Biol Chem. 2002 Feb 1;277(5):3698-707. Epub 2001 Nov 9.

17.

The structural basis for the perturbed pKa of the catalytic base in 4-oxalocrotonate tautomerase: kinetic and structural effects of mutations of Phe-50.

Czerwinski RM, Harris TK, Massiah MA, Mildvan AS, Whitman CP.

Biochemistry. 2001 Feb 20;40(7):1984-95.

PMID:
11329265
18.
19.

Enzymatically inactive macrophage migration inhibitory factor inhibits monocyte chemotaxis and random migration.

Hermanowski-Vosatka A, Mundt SS, Ayala JM, Goyal S, Hanlon WA, Czerwinski RM, Wright SD, Whitman CP.

Biochemistry. 1999 Sep 28;38(39):12841-9.

PMID:
10504254
20.

Effects of mutations of the active site arginine residues in 4-oxalocrotonate tautomerase on the pKa values of active site residues and on the pH dependence of catalysis.

Czerwinski RM, Harris TK, Johnson WH Jr, Legler PM, Stivers JT, Mildvan AS, Whitman CP.

Biochemistry. 1999 Sep 21;38(38):12358-66.

PMID:
10493803
21.

Kinetic, stereochemical, and structural effects of mutations of the active site arginine residues in 4-oxalocrotonate tautomerase.

Harris TK, Czerwinski RM, Johnson WH Jr, Legler PM, Abeygunawardana C, Massiah MA, Stivers JT, Whitman CP, Mildvan AS.

Biochemistry. 1999 Sep 21;38(38):12343-57.

PMID:
10493802
22.
23.
24.

Inactivation of 4-oxalocrotonate tautomerase by 2-oxo-3-pentynoate.

Johnson WH Jr, Czerwinski RM, Fitzgerald MC, Whitman CP.

Biochemistry. 1997 Dec 16;36(50):15724-32.

PMID:
9398301
25.

Kinetic and structural effects of mutations of the catalytic amino-terminal proline in 4-oxalocrotonate tautomerase.

Czerwinski RM, Johnson WH Jr, Whitman CP.

Biochemistry. 1997 Nov 25;36(47):14551-60.

PMID:
9398173
26.
27.

Topoisomerase I is differently phosphorylated in two sublines of L5178Y mouse lymphoma cells.

Staron K, Kowalska-Loth B, Zabek J, Czerwinski RM, Nieznanski K, Szumiel I.

Biochim Biophys Acta. 1995 Jan 2;1260(1):35-42.

PMID:
7999792
28.

PKA controls a level of topoisomerase I mRNA in mouse L5178Y lymphoma cells treated with db-cAMP.

Czerwinski RM, Nieznanski K, Sochanowicz B, Staron K.

Mol Biol Rep. 1994 Mar;19(2):93-7.

PMID:
8072495
29.

Effects of fluorodeoxyuridine and nalidixic acid on the activity of topoisomerase I in plasmodia of Physarum polycephalum.

Staron K, Kowalska-Loth B, Czerwiński RM.

Int J Biochem. 1992 Aug;24(8):1303-6.

PMID:
1379557
30.

Topoisomerase I in actively growing plasmodia and during differentiation of the slime mold Physarum polycephalum.

Staron K, Kowalska-Loth B, Czerwinski RM, Bandorowska J, Guberska J.

Biochim Biophys Acta. 1991 Jan 17;1088(1):36-40.

PMID:
1846567

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