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Items: 46

1.

Data-Driven Construction of Antitumor Agents with Controlled Polypharmacology.

Da C, Zhang D, Stashko M, Vasileiadi E, Parker RE, Minson KA, Huey MG, Huelse JM, Hunter D, Gilbert TSK, Norris-Drouin J, Miley M, Herring LE, Graves LM, DeRyckere D, Earp HS, Graham DK, Frye SV, Wang X, Kireev D.

J Am Chem Soc. 2019 Oct 2;141(39):15700-15709. doi: 10.1021/jacs.9b08660. Epub 2019 Sep 20.

PMID:
31497954
2.

Inhibition of Inositol Polyphosphate Kinases by Quercetin and Related Flavonoids: A Structure-Activity Analysis.

Gu C, Stashko MA, Puhl-Rubio AC, Chakraborty M, Chakraborty A, Frye SV, Pearce KH, Wang X, Shears SB, Wang H.

J Med Chem. 2019 Feb 14;62(3):1443-1454. doi: 10.1021/acs.jmedchem.8b01593. Epub 2019 Jan 25.

3.

Highly Selective MERTK Inhibitors Achieved by a Single Methyl Group.

Zhao J, Zhang D, Zhang W, Stashko MA, DeRyckere D, Vasileiadi E, Parker RE, Hunter D, Liu Q, Zhang Y, Norris-Drouin J, Li B, Drewry DH, Kireev D, Graham DK, Earp HS, Frye SV, Wang X.

J Med Chem. 2018 Nov 21;61(22):10242-10254. doi: 10.1021/acs.jmedchem.8b01229. Epub 2018 Nov 5.

PMID:
30347155
4.

Use of Protein Kinase-Focused Compound Libraries for the Discovery of New Inositol Phosphate Kinase Inhibitors.

Puhl-Rubio AC, Stashko MA, Wang H, Hardy PB, Tyagi V, Li B, Wang X, Kireev D, Jessen HJ, Frye SV, Shears SB, Pearce KH.

SLAS Discov. 2018 Oct;23(9):982-988. doi: 10.1177/2472555218775323. Epub 2018 May 29.

5.

Retraction: A High-Throughput Screening-Compatible Strategy for the Identification of Inositol Pyrophosphate Kinase Inhibitors.

Baughman BM, Wang H, An Y, Kireev D, Stashko MA, Jessen HJ, Pearce KH, Frye SV, Shears SB.

PLoS One. 2017 Jun 21;12(6):e0180272. doi: 10.1371/journal.pone.0180272. eCollection 2017. No abstract available.

6.

Discovery of Macrocyclic Pyrimidines as MerTK-Specific Inhibitors.

McIver AL, Zhang W, Liu Q, Jiang X, Stashko MA, Nichols J, Miley MJ, Norris-Drouin J, Machius M, DeRyckere D, Wood E, Graham DK, Earp HS, Kireev D, Frye SV, Wang X.

ChemMedChem. 2017 Feb 3;12(3):207-213. doi: 10.1002/cmdc.201600589. Epub 2017 Jan 9.

7.

Design and Synthesis of Novel Macrocyclic Mer Tyrosine Kinase Inhibitors.

Wang X, Liu J, Zhang W, Stashko MA, Nichols J, Miley MJ, Norris-Drouin J, Chen Z, Machius M, DeRyckere D, Wood E, Graham DK, Earp HS, Kireev D, Frye SV.

ACS Med Chem Lett. 2016 Sep 13;7(12):1044-1049. eCollection 2016 Dec 8.

8.

A High-Throughput Screening-Compatible Strategy for the Identification of Inositol Pyrophosphate Kinase Inhibitors.

Baughman BM, Wang H, An Y, Kireev D, Stashko MA, Jessen HJ, Pearce KH, Frye SV, Shears SB.

PLoS One. 2016 Oct 13;11(10):e0164378. doi: 10.1371/journal.pone.0164378. eCollection 2016. Retraction in: PLoS One. 2017 Jun 21;12 (6):e0180272.

9.

Identification of small molecule inhibitors that block the Toxoplasma gondii rhoptry kinase ROP18.

Simpson C, Jones NG, Hull-Ryde EA, Kireev D, Stashko M, Tang K, Janetka J, Wildman SA, Zuercher WJ, Schapira M, Hui R, Janzen W, Sibley LD.

ACS Infect Dis. 2016 Mar 11;2(3):194-206. Epub 2015 Dec 28.

10.

The MERTK/FLT3 inhibitor MRX-2843 overcomes resistance-conferring FLT3 mutations in acute myeloid leukemia.

Minson KA, Smith CC, DeRyckere D, Libbrecht C, Lee-Sherick AB, Huey MG, Lasater EA, Kirkpatrick GD, Stashko MA, Zhang W, Jordan CT, Kireev D, Wang X, Frye SV, Earp HS, Shah NP, Graham DK.

JCI Insight. 2016 Mar;1(3):e85630. doi: 10.1172/jci.insight.85630.

11.

Efficacy of a Mer and Flt3 tyrosine kinase small molecule inhibitor, UNC1666, in acute myeloid leukemia.

Lee-Sherick AB, Zhang W, Menachof KK, Hill AA, Rinella S, Kirkpatrick G, Page LS, Stashko MA, Jordan CT, Wei Q, Liu J, Zhang D, DeRyckere D, Wang X, Frye S, Earp HS, Graham DK.

Oncotarget. 2015 Mar 30;6(9):6722-36.

12.

Discovery of Mer kinase inhibitors by virtual screening using Structural Protein-Ligand Interaction Fingerprints.

Da C, Stashko M, Jayakody C, Wang X, Janzen W, Frye S, Kireev D.

Bioorg Med Chem. 2015 Mar 1;23(5):1096-101. doi: 10.1016/j.bmc.2015.01.001. Epub 2015 Jan 13.

13.

Development of a High-Throughput Screening Assay to Identify Inhibitors of the Lipid Kinase PIP5K1C.

Wright BD, Simpson C, Stashko M, Kireev D, Hull-Ryde EA, Zylka MJ, Janzen WP.

J Biomol Screen. 2015 Jun;20(5):655-62. doi: 10.1177/1087057114564057. Epub 2014 Dec 22.

14.

UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor.

Zhang W, DeRyckere D, Hunter D, Liu J, Stashko MA, Minson KA, Cummings CT, Lee M, Glaros TG, Newton DL, Sather S, Zhang D, Kireev D, Janzen WP, Earp HS, Graham DK, Frye SV, Wang X.

J Med Chem. 2014 Aug 28;57(16):7031-41. doi: 10.1021/jm500749d. Epub 2014 Aug 6.

15.

The lipid kinase PIP5K1C regulates pain signaling and sensitization.

Wright BD, Loo L, Street SE, Ma A, Taylor-Blake B, Stashko MA, Jin J, Janzen WP, Frye SV, Zylka MJ.

Neuron. 2014 May 21;82(4):836-47. doi: 10.1016/j.neuron.2014.04.006.

16.

Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis.

Zhang W, McIver AL, Stashko MA, DeRyckere D, Branchford BR, Hunter D, Kireev D, Miley MJ, Norris-Drouin J, Stewart WM, Lee M, Sather S, Zhou Y, Di Paola JA, Machius M, Janzen WP, Earp HS, Graham DK, Frye SV, Wang X.

J Med Chem. 2013 Dec 12;56(23):9693-700. doi: 10.1021/jm4013888. Epub 2013 Nov 20.

17.

Pseudo-cyclization through intramolecular hydrogen bond enables discovery of pyridine substituted pyrimidines as new Mer kinase inhibitors.

Zhang W, Zhang D, Stashko MA, DeRyckere D, Hunter D, Kireev D, Miley MJ, Cummings C, Lee M, Norris-Drouin J, Stewart WM, Sather S, Zhou Y, Kirkpatrick G, Machius M, Janzen WP, Earp HS, Graham DK, Frye SV, Wang X.

J Med Chem. 2013 Dec 12;56(23):9683-92. doi: 10.1021/jm401387j. Epub 2013 Nov 20. Erratum in: J Med Chem. 2014 Aug 28;57(16):7141.

18.

UNC1062, a new and potent Mer inhibitor.

Liu J, Zhang W, Stashko MA, Deryckere D, Cummings CT, Hunter D, Yang C, Jayakody CN, Cheng N, Simpson C, Norris-Drouin J, Sather S, Kireev D, Janzen WP, Earp HS, Graham DK, Frye SV, Wang X.

Eur J Med Chem. 2013 Jul;65:83-93. doi: 10.1016/j.ejmech.2013.03.035. Epub 2013 Apr 2.

19.

Efficient solution-phase synthesis of 4,5,7-trisubstituted pyrrolo[3,2-d]pyrimidines.

Zhang W, Liu J, Stashko MA, Wang X.

ACS Comb Sci. 2013 Jan 14;15(1):10-9. doi: 10.1021/co300106f. Epub 2012 Dec 5.

20.

Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit.

Backes BJ, Longenecker K, Hamilton GL, Stewart K, Lai C, Kopecka H, von Geldern TW, Madar DJ, Pei Z, Lubben TH, Zinker BA, Tian Z, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Kempf-Grote AJ, Black-Schaefer C, Sham HL, Trevillyan JM.

Bioorg Med Chem Lett. 2007 Apr 1;17(7):2005-12. Epub 2007 Jan 19.

PMID:
17276063
21.

Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Pei Z, Li X, von Geldern TW, Madar DJ, Longenecker K, Yong H, Lubben TH, Stewart KD, Zinker BA, Backes BJ, Judd AS, Mulhern M, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Reinhart GA, Fryer RM, Preusser LC, Kempf-Grote AJ, Sham HL, Trevillyan JM.

J Med Chem. 2006 Nov 2;49(22):6439-42.

PMID:
17064063
22.

Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes.

Madar DJ, Kopecka H, Pireh D, Yong H, Pei Z, Li X, Wiedeman PE, Djuric SW, Von Geldern TW, Fickes MG, Bhagavatula L, McDermott T, Wittenberger S, Richards SJ, Longenecker KL, Stewart KD, Lubben TH, Ballaron SJ, Stashko MA, Long MA, Wells H, Zinker BA, Mika AK, Beno DW, Kempf-Grote AJ, Polakowski J, Segreti J, Reinhart GA, Fryer RM, Sham HL, Trevillyan JM.

J Med Chem. 2006 Oct 19;49(21):6416-20.

PMID:
17034148
23.

Crystal structures of DPP-IV (CD26) from rat kidney exhibit flexible accommodation of peptidase-selective inhibitors.

Longenecker KL, Stewart KD, Madar DJ, Jakob CG, Fry EH, Wilk S, Lin CW, Ballaron SJ, Stashko MA, Lubben TH, Yong H, Pireh D, Pei Z, Basha F, Wiedeman PE, von Geldern TW, Trevillyan JM, Stoll VS.

Biochemistry. 2006 Jun 20;45(24):7474-82.

PMID:
16768443
24.

Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity.

Szczepankiewicz BG, Kosogof C, Nelson LT, Liu G, Liu B, Zhao H, Serby MD, Xin Z, Liu M, Gum RJ, Haasch DL, Wang S, Clampit JE, Johnson EF, Lubben TH, Stashko MA, Olejniczak ET, Sun C, Dorwin SA, Haskins K, Abad-Zapatero C, Fry EH, Hutchins CW, Sham HL, Rondinone CM, Trevillyan JM.

J Med Chem. 2006 Jun 15;49(12):3563-80.

PMID:
16759099
25.

Discovery, structure-activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors.

Pei Z, Li X, Longenecker K, von Geldern TW, Wiedeman PE, Lubben TH, Zinker BA, Stewart K, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Long M, Wells H, Kempf-Grote AJ, Madar DJ, McDermott TS, Bhagavatula L, Fickes MG, Pireh D, Solomon LR, Lake MR, Edalji R, Fry EH, Sham HL, Trevillyan JM.

J Med Chem. 2006 Jun 15;49(12):3520-35. Erratum in: J Med Chem. 2006 Aug 24;49(17):5387.

PMID:
16759095
26.

Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators.

Elmore SW, Pratt JK, Coghlan MJ, Mao Y, Green BE, Anderson DD, Stashko MA, Lin CW, Falls D, Nakane M, Miller L, Tyree CM, Miner JN, Lane B.

Bioorg Med Chem Lett. 2004 Apr 5;14(7):1721-7.

PMID:
15026058
27.

Identification of a monoacid-based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B.

Xin Z, Liu G, Abad-Zapatero C, Pei Z, Szczepankiewicz BG, Li X, Zhang T, Hutchins CW, Hajduk PJ, Ballaron SJ, Stashko MA, Lubben TH, Trevillyan JM, Jirousek MR.

Bioorg Med Chem Lett. 2003 Nov 17;13(22):3947-50.

PMID:
14592481
28.

Selective protein tyrosine phosphatase 1B inhibitors: targeting the second phosphotyrosine binding site with non-carboxylic acid-containing ligands.

Liu G, Xin Z, Liang H, Abad-Zapatero C, Hajduk PJ, Janowick DA, Szczepankiewicz BG, Pei Z, Hutchins CW, Ballaron SJ, Stashko MA, Lubben TH, Berg CE, Rondinone CM, Trevillyan JM, Jirousek MR.

J Med Chem. 2003 Jul 31;46(16):3437-40.

PMID:
12877578
29.

Potent, selective inhibitors of protein tyrosine phosphatase 1B.

Xin Z, Oost TK, Abad-Zapatero C, Hajduk PJ, Pei Z, Szczepankiewicz BG, Hutchins CW, Ballaron SJ, Stashko MA, Lubben T, Trevillyan JM, Jirousek MR, Liu G.

Bioorg Med Chem Lett. 2003 Jun 2;13(11):1887-90.

PMID:
12749891
30.

Discovery and structure-activity relationship of oxalylarylaminobenzoic acids as inhibitors of protein tyrosine phosphatase 1B.

Liu G, Szczepankiewicz BG, Pei Z, Janowick DA, Xin Z, Hajduk PJ, Abad-Zapatero C, Liang H, Hutchins CW, Fesik SW, Ballaron SJ, Stashko MA, Lubben T, Mika AK, Zinker BA, Trevillyan JM, Jirousek MR.

J Med Chem. 2003 May 22;46(11):2093-103.

PMID:
12747781
31.

Discovery of a potent, selective protein tyrosine phosphatase 1B inhibitor using a linked-fragment strategy.

Szczepankiewicz BG, Liu G, Hajduk PJ, Abad-Zapatero C, Pei Z, Xin Z, Lubben TH, Trevillyan JM, Stashko MA, Ballaron SJ, Liang H, Huang F, Hutchins CW, Fesik SW, Jirousek MR.

J Am Chem Soc. 2003 Apr 9;125(14):4087-96.

PMID:
12670229
32.

Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.

Kym PR, Kort ME, Coghlan MJ, Moore JL, Tang R, Ratajczyk JD, Larson DP, Elmore SW, Pratt JK, Stashko MA, Falls HD, Lin CW, Nakane M, Miller L, Tyree CM, Miner JN, Jacobson PB, Wilcox DM, Nguyen P, Lane BC.

J Med Chem. 2003 Mar 13;46(6):1016-30.

PMID:
12620078
33.

trans-Activation and repression properties of the novel nonsteroid glucocorticoid receptor ligand 2,5-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5-(1-methylcyclohexen-3-y1)-1H-[1]benzopyrano[3,4-f]quinoline (A276575) and its four stereoisomers.

Lin CW, Nakane M, Stashko M, Falls D, Kuk J, Miller L, Huang R, Tyree C, Miner JN, Rosen J, Kym PR, Coghlan MJ, Carter G, Lane BC.

Mol Pharmacol. 2002 Aug;62(2):297-303.

PMID:
12130681
34.

Nonsteroidal selective glucocorticoid modulators: the effect of C-5 alkyl substitution on the transcriptional activation/repression profile of 2,5-dihydro-10-methoxy-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.

Elmore SW, Coghlan MJ, Anderson DD, Pratt JK, Green BE, Wang AX, Stashko MA, Lin CW, Tyree CM, Miner JN, Jacobson PB, Wilcox DM, Lane BC.

J Med Chem. 2001 Dec 6;44(25):4481-91.

PMID:
11728194
35.

Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity.

Coghlan MJ, Kym PR, Elmore SW, Wang AX, Luly JR, Wilcox D, Stashko M, Lin CW, Miner J, Tyree C, Nakane M, Jacobson P, Lane BC.

J Med Chem. 2001 Aug 30;44(18):2879-85.

PMID:
11520196
36.

In vitro enzymatic assays of protein tyrosine phosphatase 1B.

Lubben T, Clampit J, Stashko M, Trevillyan J, Jirousek MR.

Curr Protoc Pharmacol. 2001 Aug;Chapter 3:Unit3.8. doi: 10.1002/0471141755.ph0308s13.

PMID:
21959757
37.

Minor structural differences in Boc-CCK-4 derivatives dictate affinity and selectivity for CCK-A and CCK-B receptors.

Shiosaki K, Lin CW, Kopecka H, Bianchi B, Miller T, Stashko M, Witte D.

J Med Chem. 1997 Mar 28;40(7):1169-72.

PMID:
9089338
38.

Persistent activation of the dopamine D1 receptor contributes to prolonged receptor desensitization: studies with A-77636.

Lin CW, Bianchi BR, Miller TR, Stashko MA, Wang SS, Curzon P, Bednarz L, Asin KE, Britton DR.

J Pharmacol Exp Ther. 1996 Mar;276(3):1022-9.

PMID:
8786531
39.

ABT-431: the diacetyl prodrug of A-86929, a potent and selective dopamine D1 receptor agonist: in vitro characterization and effects in animal models of Parkinson's disease.

Shiosaki K, Jenner P, Asin KE, Britton DR, Lin CW, Michaelides M, Smith L, Bianchi B, Didomenico S, Hodges L, Hong Y, Mahan L, Mikusa J, Miller T, Nikkel A, Stashko M, Witte D, Williams M.

J Pharmacol Exp Ther. 1996 Jan;276(1):150-60.

PMID:
8558425
40.

Characterization of cloned human dopamine D1 receptor-mediated calcium release in 293 cells.

Lin CW, Miller TR, Witte DG, Bianchi BR, Stashko M, Manelli AM, Frail DE.

Mol Pharmacol. 1995 Jan;47(1):131-9.

PMID:
7838121
41.

CCK-A-selective tetrapeptides containing lys(N epsilon)-amide residues: favorable in vivo and in vitro effects of N-methylation at the aspartyl residue.

Bennett MJ, Nikkel AL, Bianchi BR, Miller TR, Bednarz L, Witte DG, Stashko M, Wang SS, Gore PA, Asin KE, et al.

J Med Chem. 1994 May 27;37(11):1569-71.

PMID:
8201591
42.

Novel Asp32-replacement tetrapeptide analogues as potent and selective CCK-A agonists.

Elliott RL, Kopecka H, Tufano MD, Shue YK, Gauri AJ, Lin CW, Bianchi BR, Miller TR, Witte DG, Stashko MA, et al.

J Med Chem. 1994 May 27;37(11):1562-8.

PMID:
8201590
43.

Tetrapeptide CCK agonists: structure-activity studies on modifications at the N-terminus.

Elliott RL, Kopecka H, Bennett MJ, Shue YK, Craig R, Lin CW, Bianchi BR, Miller TR, Witte DG, Stashko MA, et al.

J Med Chem. 1994 Jan 21;37(2):309-13.

PMID:
8295219
44.

Double bond isosteres of the peptide bond: synthesis and biological activity of cholecystokinin (CCK) C-terminal hexapeptide analogs.

Shue YK, Tufano MD, Carrera GM Jr, Kopecka H, Kuyper SL, Holladay MW, Lin CW, Witte DG, Miller TR, Stashko M, et al.

Bioorg Med Chem. 1993 Sep;1(3):161-71.

PMID:
8081848
45.

Development of potent and selective CCK-A receptor agonists from Boc-CCK-4: tetrapeptides containing Lys(N epsilon)-amide residues.

Shiosaki K, Lin CW, Kopecka H, Craig RA, Bianchi BR, Miller TR, Witte DG, Stashko M, Nadzan AM.

J Med Chem. 1992 May 29;35(11):2007-14.

PMID:
1375964
46.

Cholecystokinin antagonists: (R)-tryptophan-based hybrid antagonists of high affinity and selectivity for CCK-A receptors.

Kerwin JF Jr, Wagenaar F, Kopecka H, Lin CW, Miller T, Witte D, Stashko M, Nadzan AM.

J Med Chem. 1991 Dec;34(12):3350-9.

PMID:
1766000

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