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Items: 42

1.

The Novel Bromodomain and Extraterminal Domain Inhibitor INCB054329 Induces Vulnerabilities in Myeloma Cells That Inform Rational Combination Strategies.

Stubbs MC, Burn TC, Sparks RB, Maduskuie T, Diamond S, Rupar M, Wen X, Volgina A, Zolotarjova N, Waeltz P, Favata M, Jalluri R, Liu H, Liu XM, Li J, Collins R, Falahatpisheh N, Polam P, DiMatteo D, Feldman P, Dostalik V, Thekkat P, Gardiner C, He X, Li Y, Covington M, Wynn R, Ruggeri B, Yeleswaram S, Xue C, Yao W, Combs AP, Huber R, Hollis G, Scherle P, Liu P.

Clin Cancer Res. 2018 Sep 11. pii: clincanres.0098.2018. doi: 10.1158/1078-0432.CCR-18-0098. [Epub ahead of print]

PMID:
30206163
2.

INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology.

Yue EW, Sparks R, Polam P, Modi D, Douty B, Wayland B, Glass B, Takvorian A, Glenn J, Zhu W, Bower M, Liu X, Leffet L, Wang Q, Bowman KJ, Hansbury MJ, Wei M, Li Y, Wynn R, Burn TC, Koblish HK, Fridman JS, Emm T, Scherle PA, Metcalf B, Combs AP.

ACS Med Chem Lett. 2017 Mar 6;8(5):486-491. doi: 10.1021/acsmedchemlett.6b00391. eCollection 2017 May 11.

3.

Roles of UGT, P450, and Gut Microbiota in the Metabolism of Epacadostat in Humans.

Boer J, Young-Sciame R, Lee F, Bowman KJ, Yang X, Shi JG, Nedza FM, Frietze W, Galya L, Combs AP, Yeleswaram S, Diamond S.

Drug Metab Dispos. 2016 Oct;44(10):1668-74. doi: 10.1124/dmd.116.070680. Epub 2016 Jul 25.

4.

Synthesis and structure-activity relationships of pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones as corticotropin-releasing factor-1 receptor antagonists.

Dzierba CD, Sielecki TM, Arvanitis AG, Galka A, Johnson TL, Takvorian AG, Rafalski M, Kasireddy-Polam P, Vig S, Dasgupta B, Zhang G, Molski TF, Wong H, Zaczek RC, Lodge NJ, Combs AP, Gilligan PJ, Trainor GL, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2012 Aug 1;22(15):4986-9. doi: 10.1016/j.bmcl.2012.06.034. Epub 2012 Jun 16.

PMID:
22749422
5.

Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors.

Thompson LA, Shi J, Decicco CP, Tebben AJ, Olson RE, Boy KM, Guernon JM, Good AC, Liauw A, Zheng C, Copeland RA, Combs AP, Trainor GL, Camac DM, Muckelbauer JK, Lentz KA, Grace JE, Burton CR, Toyn JH, Barten DM, Marcinkeviciene J, Meredith JE, Albright CF, Macor JE.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6909-15. doi: 10.1016/j.bmcl.2011.06.116. Epub 2011 Jul 2.

PMID:
21974952
6.

Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity.

Liu X, Shin N, Koblish HK, Yang G, Wang Q, Wang K, Leffet L, Hansbury MJ, Thomas B, Rupar M, Waeltz P, Bowman KJ, Polam P, Sparks RB, Yue EW, Li Y, Wynn R, Fridman JS, Burn TC, Combs AP, Newton RC, Scherle PA.

Blood. 2010 Apr 29;115(17):3520-30. doi: 10.1182/blood-2009-09-246124. Epub 2010 Mar 2.

7.

Efficacy of the JAK2 inhibitor INCB16562 in a murine model of MPLW515L-induced thrombocytosis and myelofibrosis.

Koppikar P, Abdel-Wahab O, Hedvat C, Marubayashi S, Patel J, Goel A, Kucine N, Gardner JR, Combs AP, Vaddi K, Haley PJ, Burn TC, Rupar M, Bromberg JF, Heaney ML, de Stanchina E, Fridman JS, Levine RL.

Blood. 2010 Apr 8;115(14):2919-27. doi: 10.1182/blood-2009-04-218842. Epub 2010 Feb 12.

8.

Hydroxyamidine inhibitors of indoleamine-2,3-dioxygenase potently suppress systemic tryptophan catabolism and the growth of IDO-expressing tumors.

Koblish HK, Hansbury MJ, Bowman KJ, Yang G, Neilan CL, Haley PJ, Burn TC, Waeltz P, Sparks RB, Yue EW, Combs AP, Scherle PA, Vaddi K, Fridman JS.

Mol Cancer Ther. 2010 Feb;9(2):489-98. doi: 10.1158/1535-7163.MCT-09-0628. Epub 2010 Feb 2.

9.

INCB16562, a JAK1/2 selective inhibitor, is efficacious against multiple myeloma cells and reverses the protective effects of cytokine and stromal cell support.

Li J, Favata M, Kelley JA, Caulder E, Thomas B, Wen X, Sparks RB, Arvanitis A, Rogers JD, Combs AP, Vaddi K, Solomon KA, Scherle PA, Newton R, Fridman JS.

Neoplasia. 2010 Jan;12(1):28-38.

10.

Recent advances in the discovery of competitive protein tyrosine phosphatase 1B inhibitors for the treatment of diabetes, obesity, and cancer.

Combs AP.

J Med Chem. 2010 Mar 25;53(6):2333-44. doi: 10.1021/jm901090b. No abstract available.

PMID:
20000419
11.

Combined inhibition of Janus kinase 1/2 for the treatment of JAK2V617F-driven neoplasms: selective effects on mutant cells and improvements in measures of disease severity.

Liu PC, Caulder E, Li J, Waeltz P, Margulis A, Wynn R, Becker-Pasha M, Li Y, Crowgey E, Hollis G, Haley P, Sparks RB, Combs AP, Rodgers JD, Burn TC, Vaddi K, Fridman JS.

Clin Cancer Res. 2009 Nov 15;15(22):6891-900. doi: 10.1158/1078-0432.CCR-09-1298. Epub 2009 Nov 3.

12.

Synthesis, structure-activity relationships, and in vivo evaluation of N3-phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists.

Hartz RA, Ahuja VT, Arvanitis AG, Rafalski M, Yue EW, Denhart DJ, Schmitz WD, Ditta JL, Deskus JA, Brenner AB, Hobbs FW, Payne J, Lelas S, Li YW, Molski TF, Mattson GK, Peng Y, Wong H, Grace JE, Lentz KA, Qian-Cutrone J, Zhuo X, Shu YZ, Lodge NJ, Zaczek R, Combs AP, Olson RE, Bronson JJ, Mattson RJ, Macor JE.

J Med Chem. 2009 Jul 23;52(14):4173-91. doi: 10.1021/jm900301y.

PMID:
19552437
13.

In vitro intrinsic clearance-based optimization of N3-phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists.

Hartz RA, Ahuja VT, Rafalski M, Schmitz WD, Brenner AB, Denhart DJ, Ditta JL, Deskus JA, Yue EW, Arvanitis AG, Lelas S, Li YW, Molski TF, Wong H, Grace JE, Lentz KA, Li J, Lodge NJ, Zaczek R, Combs AP, Olson RE, Mattson RJ, Bronson JJ, Macor JE.

J Med Chem. 2009 Jul 23;52(14):4161-72. doi: 10.1021/jm900302q. Erratum in: J Med Chem. 2009 Sep 24;52(18):5770.

PMID:
19552436
14.

Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model.

Yue EW, Douty B, Wayland B, Bower M, Liu X, Leffet L, Wang Q, Bowman KJ, Hansbury MJ, Liu C, Wei M, Li Y, Wynn R, Burn TC, Koblish HK, Fridman JS, Metcalf B, Scherle PA, Combs AP.

J Med Chem. 2009 Dec 10;52(23):7364-7. doi: 10.1021/jm900518f.

PMID:
19507862
15.

Isothiazolidinone inhibitors of PTP1B containing imidazoles and imidazolines.

Douty B, Wayland B, Ala PJ, Bower MJ, Pruitt J, Bostrom L, Wei M, Klabe R, Gonneville L, Wynn R, Burn TC, Liu PC, Combs AP, Yue EW.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):66-71. Epub 2007 Nov 9.

PMID:
18037290
16.

Dihydropyridopyrazinones and dihydropteridinones as corticotropin-releasing factor-1 receptor antagonists: structure-activity relationships and computational modeling.

Dzierba CD, Tebben AJ, Wilde RG, Takvorian AG, Rafalski M, Kasireddy-Polam P, Klaczkiewicz JD, Pechulis AD, Davis AL, Sweet MP, Woo AM, Yang Z, Ebeltoft SM, Molski TF, Zhang G, Zaczek RC, Trainor GL, Combs AP, Gilligan PJ.

J Med Chem. 2007 May 3;50(9):2269-72. Epub 2007 Apr 3.

PMID:
17402721
17.
18.

Structure-based drug design of new leads for phosphatase research.

Combs AP.

IDrugs. 2007 Feb;10(2):112-5. Review.

PMID:
17285463
19.

Benzothiazole benzimidazole (S)-isothiazolidinone derivatives as protein tyrosine phosphatase-1B inhibitors.

Sparks RB, Polam P, Zhu W, Crawley ML, Takvorian A, McLaughlin E, Wei M, Ala PJ, Gonneville L, Taylor N, Li Y, Wynn R, Burn TC, Liu PC, Combs AP.

Bioorg Med Chem Lett. 2007 Feb 1;17(3):736-40. Epub 2006 Oct 28.

PMID:
17097290
20.

Structural insights into the design of nonpeptidic isothiazolidinone-containing inhibitors of protein-tyrosine phosphatase 1B.

Ala PJ, Gonneville L, Hillman M, Becker-Pasha M, Yue EW, Douty B, Wayland B, Polam P, Crawley ML, McLaughlin E, Sparks RB, Glass B, Takvorian A, Combs AP, Burn TC, Hollis GF, Wynn R.

J Biol Chem. 2006 Dec 8;281(49):38013-21. Epub 2006 Oct 6.

21.

Structural basis for inhibition of protein-tyrosine phosphatase 1B by isothiazolidinone heterocyclic phosphonate mimetics.

Ala PJ, Gonneville L, Hillman MC, Becker-Pasha M, Wei M, Reid BG, Klabe R, Yue EW, Wayland B, Douty B, Polam P, Wasserman Z, Bower M, Combs AP, Burn TC, Hollis GF, Wynn R.

J Biol Chem. 2006 Oct 27;281(43):32784-95. Epub 2006 Aug 17.

22.

Potent benzimidazole sulfonamide protein tyrosine phosphatase 1B inhibitors containing the heterocyclic (S)-isothiazolidinone phosphotyrosine mimetic.

Combs AP, Zhu W, Crawley ML, Glass B, Polam P, Sparks RB, Modi D, Takvorian A, McLaughlin E, Yue EW, Wasserman Z, Bower M, Wei M, Rupar M, Ala PJ, Reid BM, Ellis D, Gonneville L, Emm T, Taylor N, Yeleswaram S, Li Y, Wynn R, Burn TC, Hollis G, Liu PC, Metcalf B.

J Med Chem. 2006 Jun 29;49(13):3774-89.

PMID:
16789735
23.

Isothiazolidinone heterocycles as inhibitors of protein tyrosine phosphatases: synthesis and structure-activity relationships of a peptide scaffold.

Yue EW, Wayland B, Douty B, Crawley ML, McLaughlin E, Takvorian A, Wasserman Z, Bower MJ, Wei M, Li Y, Ala PJ, Gonneville L, Wynn R, Burn TC, Liu PC, Combs AP.

Bioorg Med Chem. 2006 Sep 1;14(17):5833-49.

PMID:
16769216
24.

Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors.

Thompson LA, Liauw AY, Ramanjulu MM, Kasireddy-Polam P, Mercer SE, Maduskuie TP, Glicksman M, Roach AH, Meredith JE, Liu RQ, Combs AP, Higaki JN, Cordell B, Seiffert D, Zaczek RC, Robertson DW, Olson RE.

Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63. Epub 2006 Feb 10.

PMID:
16473009
25.
26.

Structure-based design and discovery of protein tyrosine phosphatase inhibitors incorporating novel isothiazolidinone heterocyclic phosphotyrosine mimetics.

Combs AP, Yue EW, Bower M, Ala PJ, Wayland B, Douty B, Takvorian A, Polam P, Wasserman Z, Zhu W, Crawley ML, Pruitt J, Sparks R, Glass B, Modi D, McLaughlin E, Bostrom L, Li M, Galya L, Blom K, Hillman M, Gonneville L, Reid BG, Wei M, Becker-Pasha M, Klabe R, Huber R, Li Y, Hollis G, Burn TC, Wynn R, Liu P, Metcalf B.

J Med Chem. 2005 Oct 20;48(21):6544-8.

PMID:
16220970
27.

Preparative LC-MS purification: improved compound-specific method optimization.

Blom KF, Glass B, Sparks R, Combs AP.

J Comb Chem. 2004 Nov-Dec;6(6):874-83.

PMID:
15530113
28.

Synthesis, structure-activity relationships, and in vivo properties of 3,4-dihydro-1H-pyrido[2,3-b]pyrazin-2-ones as corticotropin-releasing factor-1 receptor antagonists.

Dzierba CD, Takvorian AG, Rafalski M, Kasireddy-Polam P, Wong H, Molski TF, Zhang G, Li YW, Lelas S, Peng Y, McElroy JF, Zaczek RC, Taub RA, Combs AP, Gilligan PJ, Trainor GL.

J Med Chem. 2004 Nov 4;47(23):5783-90.

PMID:
15509177
29.
30.
31.

Microwave-assisted solid-phase organic synthesis (MA-SPOS) of oxazolidinone antimicrobials.

Combs AP, Glass BM, Jackson SA.

Methods Enzymol. 2003;369:223-31. No abstract available.

PMID:
14722956
32.

Comparative studies of active site-ligand interactions among various recombinant constructs of human beta-amyloid precursor protein cleaving enzyme.

Kopcho LM, Ma J, Marcinkeviciene J, Lai Z, Witmer MR, Cheng J, Yanchunas J, Tredup J, Corbett M, Calambur D, Wittekind M, Paruchuri M, Kothari D, Lee G, Ganguly S, Ramamurthy V, Morin PE, Camac DM, King RW, Lasut AL, Ross OH, Hillman MC, Fish B, Shen K, Dowling RL, Kim YB, Graciani NR, Collins D, Combs AP, George H, Thompson LA, Copeland RA.

Arch Biochem Biophys. 2003 Feb 15;410(2):307-16.

PMID:
12573291
33.

Parallel synthesis of potent, pyrazole-based inhibitors of Helicobacter pylori dihydroorotate dehydrogenase.

Haque TS, Tadesse S, Marcinkeviciene J, Rogers MJ, Sizemore C, Kopcho LM, Amsler K, Ecret LD, Zhan DL, Hobbs F, Slee A, Trainor GL, Stern AM, Copeland RA, Combs AP.

J Med Chem. 2002 Oct 10;45(21):4669-78.

PMID:
12361393
34.

A concise synthesis of silanediol-based transition-state isostere inhibitors of proteases.

Organ MG, Buon C, Decicco CP, Combs AP.

Org Lett. 2002 Aug 8;4(16):2683-5.

PMID:
12153209
35.

Novel inhibition of porcine pepsin by a substituted piperidine. Preference for one of the enzyme conformers.

Marcinkeviciene J, Kopcho LM, Yang T, Copeland RA, Glass BM, Combs AP, Falahatpisheh N, Thompson L.

J Biol Chem. 2002 Aug 9;277(32):28677-82. Epub 2002 May 23.

36.

N-arylation of primary and secondary aliphatic amines on solid supports.

Combs AP, Tadesse S, Rafalski M, Haque TS, Lam PY.

J Comb Chem. 2002 Mar-Apr;4(2):179-82.

PMID:
11886294
37.
38.

Mechanism of Inhibition of beta-site amyloid precursor protein-cleaving enzyme (BACE) by a statine-based peptide.

Marcinkeviciene J, Luo Y, Graciani NR, Combs AP, Copeland RA.

J Biol Chem. 2001 Jun 29;276(26):23790-4. Epub 2001 Apr 16.

39.

Helicobacter pylori-selective antibacterials based on inhibition of pyrimidine biosynthesis.

Copeland RA, Marcinkeviciene J, Haque TS, Kopcho LM, Jiang W, Wang K, Ecret LD, Sizemore C, Amsler KA, Foster L, Tadesse S, Combs AP, Stern AM, Trainor GL, Slee A, Rogers MJ, Hobbs F.

J Biol Chem. 2000 Oct 27;275(43):33373-8.

40.

Presenilin-1 and -2 are molecular targets for gamma-secretase inhibitors.

Seiffert D, Bradley JD, Rominger CM, Rominger DH, Yang F, Meredith JE Jr, Wang Q, Roach AH, Thompson LA, Spitz SM, Higaki JN, Prakash SR, Combs AP, Copeland RA, Arneric SP, Hartig PR, Robertson DW, Cordell B, Stern AM, Olson RE, Zaczek R.

J Biol Chem. 2000 Nov 3;275(44):34086-91.

41.

N-Arylation of Sulfonamides on Solid Supports.

Combs AP, Rafalski M.

J Comb Chem. 2000 Jan 11;2(1):29-32.

PMID:
10813881
42.

Molecular basis for the binding of SH3 ligands with non-peptide elements identified by combinatorial synthesis.

Feng S, Kapoor TM, Shirai F, Combs AP, Schreiber SL.

Chem Biol. 1996 Aug;3(8):661-70.

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