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Items: 1 to 50 of 98

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.

TAM Family Receptor Kinase Inhibition Reverses MDSC-Mediated Suppression and Augments Anti-PD-1 Therapy in Melanoma.

Holtzhausen A, Harris W, Ubil E, Hunter DM, Zhao J, Zhang Y, Zhang D, Liu Q, Wang X, Graham DK, Frye SV, Earp HS.

Cancer Immunol Res. 2019 Oct;7(10):1672-1686. doi: 10.1158/2326-6066.CIR-19-0008. Epub 2019 Aug 26.

PMID:
31451482
3.

Discovery and Characterization of a Cellular Potent Positive Allosteric Modulator of the Polycomb Repressive Complex 1 Chromodomain, CBX7.

Lamb KN, Bsteh D, Dishman SN, Moussa HF, Fan H, Stuckey JI, Norris JL, Cholensky SH, Li D, Wang J, Sagum C, Stanton BZ, Bedford MT, Pearce KH, Kenakin TP, Kireev DB, Wang GG, James LI, Bell O, Frye SV.

Cell Chem Biol. 2019 Oct 17;26(10):1365-1379.e22. doi: 10.1016/j.chembiol.2019.07.013. Epub 2019 Aug 15.

PMID:
31422906
4.

Kinome profiling of non-Hodgkin lymphoma identifies Tyro3 as a therapeutic target in primary effusion lymphoma.

Wong JP, Stuhlmiller TJ, Giffin LC, Lin C, Bigi R, Zhao J, Zhang W, Bravo Cruz AG, Park SI, Earp HS, Dittmer DP, Frye SV, Wang X, Johnson GL, Damania B.

Proc Natl Acad Sci U S A. 2019 Aug 13;116(33):16541-16550. doi: 10.1073/pnas.1903991116. Epub 2019 Jul 25.

PMID:
31346082
5.

Application of a MYC degradation screen identifies sensitivity to CDK9 inhibitors in KRAS-mutant pancreatic cancer.

Blake DR, Vaseva AV, Hodge RG, Kline MP, Gilbert TSK, Tyagi V, Huang D, Whiten GC, Larson JE, Wang X, Pearce KH, Herring LE, Graves LM, Frye SV, Emanuele MJ, Cox AD, Der CJ.

Sci Signal. 2019 Jul 16;12(590). pii: eaav7259. doi: 10.1126/scisignal.aav7259.

6.

Canonical PRC1 controls sequence-independent propagation of Polycomb-mediated gene silencing.

Moussa HF, Bsteh D, Yelagandula R, Pribitzer C, Stecher K, Bartalska K, Michetti L, Wang J, Zepeda-Martinez JA, Elling U, Stuckey JI, James LI, Frye SV, Bell O.

Nat Commun. 2019 Apr 29;10(1):1931. doi: 10.1038/s41467-019-09628-6.

7.

Discovery of selective activators of PRC2 mutant EED-I363M.

Suh JL, Barnash KD, Abramyan TM, Li F, The J, Engelberg IA, Vedadi M, Brown PJ, Kireev DB, Arrowsmith CH, James LI, Frye SV.

Sci Rep. 2019 Apr 25;9(1):6524. doi: 10.1038/s41598-019-43005-z.

8.

A General TR-FRET Assay Platform for High-Throughput Screening and Characterizing Inhibitors of Methyl-Lysine Reader Proteins.

Rectenwald JM, Hardy PB, Norris-Drouin JL, Cholensky SH, James LI, Frye SV, Pearce KH.

SLAS Discov. 2019 Jul;24(6):693-700. doi: 10.1177/2472555219844569. Epub 2019 Apr 24.

9.

Addendum: A cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1.

Stuckey JI, Dickson BM, Cheng N, Liu Y, Norris JL, Cholensky SH, Tempel W, Qin S, Huber KG, Sagum C, Black K, Li F, Huang XP, Roth BL, Baughman BM, Senisterra G, Pattenden SG, Vedadi M, Brown PJ, TBedford M, Min J, Arrowsmith CH, James LI, Frye SV.

Nat Chem Biol. 2019 Aug;15(8):846. doi: 10.1038/s41589-019-0242-5. No abstract available.

PMID:
30842648
10.

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.

11.

Correction to "Quantitative Characterization of Bivalent Probes for a Dual Bromodomain Protein, Transcription Initiation Factor TFIID subunit 1".

Suh JL, Watts B, Stuckey JI, Norris-Drouin JL, Cholensky SH, Dickson BM, An Y, Mathea S, Salah E, Knapp S, Khan A, Adams AT, Strahl BD, Sagum CA, Bedford MT, James LI, Kireev DB, Frye SV.

Biochemistry. 2018 Dec 11;57(49):6806. doi: 10.1021/acs.biochem.8b01187. Epub 2018 Nov 28. No abstract available.

PMID:
30485080
12.

Inhibition of MERTK Promotes Suppression of Tumor Growth in BRAF Mutant and BRAF Wild-Type Melanoma.

Sinik L, Minson KA, Tentler JJ, Carrico J, Bagby SM, Robinson WA, Kami R, Burstyn-Cohen T, Eckhardt SG, Wang X, Frye SV, Earp HS, DeRyckere D, Graham DK.

Mol Cancer Ther. 2019 Feb;18(2):278-288. doi: 10.1158/1535-7163.MCT-18-0456. Epub 2018 Nov 27.

PMID:
30482852
13.

MERTK inhibition alters the PD-1 axis and promotes anti-leukemia immunity.

Lee-Sherick AB, Jacobsen KM, Henry CJ, Huey MG, Parker RE, Page LS, Hill AA, Wang X, Frye SV, Earp HS, Jordan CT, DeRyckere D, Graham DK.

JCI Insight. 2018 Nov 2;3(21). pii: 97941. doi: 10.1172/jci.insight.97941.

14.

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
15.

MERTK Promotes Resistance to Irreversible EGFR Tyrosine Kinase Inhibitors in Non-small Cell Lung Cancers Expressing Wild-type EGFR Family Members.

Yan D, Parker RE, Wang X, Frye SV, Earp HS 3rd, DeRyckere D, Graham DK.

Clin Cancer Res. 2018 Dec 15;24(24):6523-6535. doi: 10.1158/1078-0432.CCR-18-0040. Epub 2018 Sep 7.

PMID:
30194074
16.

MERTK Mediates Intrinsic and Adaptive Resistance to AXL-targeting Agents.

McDaniel NK, Cummings CT, Iida M, Hülse J, Pearson HE, Vasileiadi E, Parker RE, Orbuch RA, Ondracek OJ, Welke NB, Kang GH, Davies KD, Wang X, Frye SV, Earp HS, Harari PM, Kimple RJ, DeRyckere D, Graham DK, Wheeler DL.

Mol Cancer Ther. 2018 Nov;17(11):2297-2308. doi: 10.1158/1535-7163.MCT-17-1239. Epub 2018 Aug 9.

17.

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.

18.

Donated chemical probes for open science.

Müller S, Ackloo S, Arrowsmith CH, Bauser M, Baryza JL, Blagg J, Böttcher J, Bountra C, Brown PJ, Bunnage ME, Carter AJ, Damerell D, Dötsch V, Drewry DH, Edwards AM, Edwards J, Elkins JM, Fischer C, Frye SV, Gollner A, Grimshaw CE, IJzerman A, Hanke T, Hartung IV, Hitchcock S, Howe T, Hughes TV, Laufer S, Li VM, Liras S, Marsden BD, Matsui H, Mathias J, O'Hagan RC, Owen DR, Pande V, Rauh D, Rosenberg SH, Roth BL, Schneider NS, Scholten C, Singh Saikatendu K, Simeonov A, Takizawa M, Tse C, Thompson PR, Treiber DK, Viana AY, Wells CI, Willson TM, Zuercher WJ, Knapp S, Mueller-Fahrnow A.

Elife. 2018 Apr 20;7. pii: e34311. doi: 10.7554/eLife.34311.

19.

Quantitative Characterization of Bivalent Probes for a Dual Bromodomain Protein, Transcription Initiation Factor TFIID Subunit 1.

Suh JL, Watts B, Stuckey JI, Norris-Drouin JL, Cholensky SH, Dickson BM, An Y, Mathea S, Salah E, Knapp S, Khan A, Adams AT, Strahl BD, Sagum CA, Bedford MT, James LI, Kireev DB, Frye SV.

Biochemistry. 2018 Apr 10;57(14):2140-2149. doi: 10.1021/acs.biochem.8b00150. Epub 2018 Mar 28. Erratum in: Biochemistry. 2018 Dec 11;57(49):6806.

20.

Retraction of "The L3MBTL3 Methyl-Lysine Reader Domain Functions As a Dimer".

Baughman BM, Pattenden SG, Norris JL, James LI, Frye SV.

ACS Chem Biol. 2018 Jan 19;13(1):281. doi: 10.1021/acschembio.7b01061. Epub 2017 Dec 19. No abstract available.

21.

The small-molecule MERTK inhibitor UNC2025 decreases platelet activation and prevents thrombosis.

Branchford BR, Stalker TJ, Law L, Acevedo G, Sather S, Brzezinski C, Wilson KM, Minson K, Lee-Sherick AB, Davizon-Castillo P, Ng C, Zhang W, Neeves KB, Lentz SR, Wang X, Frye SV, Shelton Earp H 3rd, DeRyckere D, Brass LF, Graham DK, Di Paola JA.

J Thromb Haemost. 2018 Feb;16(2):352-363. doi: 10.1111/jth.13875. Epub 2018 Jan 12.

22.

Target class drug discovery.

Barnash KD, James LI, Frye SV.

Nat Chem Biol. 2017 Sep 19;13(10):1053-1056. doi: 10.1038/nchembio.2473. No abstract available.

23.

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.

24.

MerTK as a therapeutic target in glioblastoma.

Wu J, Frady LN, Bash RE, Cohen SM, Schorzman AN, Su YT, Irvin DM, Zamboni WC, Wang X, Frye SV, Ewend MG, Sulman EP, Gilbert MR, Earp HS, Miller CR.

Neuro Oncol. 2018 Jan 10;20(1):92-102. doi: 10.1093/neuonc/nox111.

25.

Discovery of Peptidomimetic Ligands of EED as Allosteric Inhibitors of PRC2.

Barnash KD, The J, Norris-Drouin JL, Cholensky SH, Worley BM, Li F, Stuckey JI, Brown PJ, Vedadi M, Arrowsmith CH, Frye SV, James LI.

ACS Comb Sci. 2017 Mar 13;19(3):161-172. doi: 10.1021/acscombsci.6b00174. Epub 2017 Feb 22.

26.

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.

27.

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.

28.

MERTK Inhibition Induces Polyploidy and Promotes Cell Death and Cellular Senescence in Glioblastoma Multiforme.

Sufit A, Lee-Sherick AB, DeRyckere D, Rupji M, Dwivedi B, Varella-Garcia M, Pierce AM, Kowalski J, Wang X, Frye SV, Earp HS, Keating AK, Graham DK.

PLoS One. 2016 Oct 26;11(10):e0165107. doi: 10.1371/journal.pone.0165107. eCollection 2016.

29.

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.

30.

UNC2025, a MERTK Small-Molecule Inhibitor, Is Therapeutically Effective Alone and in Combination with Methotrexate in Leukemia Models.

DeRyckere D, Lee-Sherick AB, Huey MG, Hill AA, Tyner JW, Jacobsen KM, Page LS, Kirkpatrick GG, Eryildiz F, Montgomery SA, Zhang W, Wang X, Frye SV, Earp HS, Graham DK.

Clin Cancer Res. 2017 Mar 15;23(6):1481-1492. doi: 10.1158/1078-0432.CCR-16-1330. Epub 2016 Sep 20. Erratum in: Clin Cancer Res. 2017 Jul 15;23 (14 ):3971-3972.

31.

Structure-Activity Relationships and Kinetic Studies of Peptidic Antagonists of CBX Chromodomains.

Stuckey JI, Simpson C, Norris-Drouin JL, Cholensky SH, Lee J, Pasca R, Cheng N, Dickson BM, Pearce KH, Frye SV, James LI.

J Med Chem. 2016 Oct 13;59(19):8913-8923. Epub 2016 Sep 19.

32.

Design, synthesis, and protein methyltransferase activity of a unique set of constrained amine containing compounds.

Zhou H, Che X, Bao G, Wang N, Peng L, Barnash KD, Frye SV, James LI, Bai X.

Bioorg Med Chem Lett. 2016 Sep 15;26(18):4436-4440. doi: 10.1016/j.bmcl.2016.08.004. Epub 2016 Aug 3.

33.

Chromodomain Ligand Optimization via Target-Class Directed Combinatorial Repurposing.

Barnash KD, Lamb KN, Stuckey JI, Norris JL, Cholensky SH, Kireev DB, Frye SV, James LI.

ACS Chem Biol. 2016 Sep 16;11(9):2475-83. doi: 10.1021/acschembio.6b00415. Epub 2016 Jul 14.

34.

Chemical probes for methyl lysine reader domains.

James LI, Frye SV.

Curr Opin Chem Biol. 2016 Aug;33:135-41. doi: 10.1016/j.cbpa.2016.06.004. Epub 2016 Jun 25. Review.

35.

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.

36.

Novel Therapeutics Targeting Epigenetics: New Molecules, New Methods.

Frye SV, Jin J.

ACS Med Chem Lett. 2016 Feb 11;7(2):123. doi: 10.1021/acsmedchemlett.6b00037. eCollection 2016 Feb 11. No abstract available.

37.

High-throughput small molecule screen identifies inhibitors of aberrant chromatin accessibility.

Pattenden SG, Simon JM, Wali A, Jayakody CN, Troutman J, McFadden AW, Wooten J, Wood CC, Frye SV, Janzen WP, Davis IJ.

Proc Natl Acad Sci U S A. 2016 Mar 15;113(11):3018-23. doi: 10.1073/pnas.1521827113. Epub 2016 Feb 29.

38.

A cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1.

Stuckey JI, Dickson BM, Cheng N, Liu Y, Norris JL, Cholensky SH, Tempel W, Qin S, Huber KG, Sagum C, Black K, Li F, Huang XP, Roth BL, Baughman BM, Senisterra G, Pattenden SG, Vedadi M, Brown PJ, Bedford MT, Min J, Arrowsmith CH, James LI, Frye SV.

Nat Chem Biol. 2016 Mar;12(3):180-7. doi: 10.1038/nchembio.2007. Epub 2016 Jan 25. Erratum in: Nat Chem Biol. 2019 Aug;15(8):846.

39.

Corrigendum: The promise and peril of chemical probes.

Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frederiksen M, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O'Hagan RC, Overington JP, Owen DR, Rosenberg SH, Ross R, Roth B, Schapira M, Schreiber SL, Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ.

Nat Chem Biol. 2015 Nov;11(11):887. doi: 10.1038/nchembio1115-887c. No abstract available.

PMID:
26485080
40.

Unlocking the potential of chemical probes for methyl-lysine reader proteins.

Frye SV.

Future Med Chem. 2015;7(14):1831-3. doi: 10.4155/fmc.15.119. Epub 2015 Sep 22. No abstract available.

41.

Tackling reproducibility in academic preclinical drug discovery.

Frye SV, Arkin MR, Arrowsmith CH, Conn PJ, Glicksman MA, Hull-Ryde EA, Slusher BS.

Nat Rev Drug Discov. 2015 Nov;14(11):733-4. doi: 10.1038/nrd4737. Epub 2015 Sep 21.

PMID:
26388229
42.

Structure and Inhibition of Microbiome β-Glucuronidases Essential to the Alleviation of Cancer Drug Toxicity.

Wallace BD, Roberts AB, Pollet RM, Ingle JD, Biernat KA, Pellock SJ, Venkatesh MK, Guthrie L, O'Neal SK, Robinson SJ, Dollinger M, Figueroa E, McShane SR, Cohen RD, Jin J, Frye SV, Zamboni WC, Pepe-Ranney C, Mani S, Kelly L, Redinbo MR.

Chem Biol. 2015 Sep 17;22(9):1238-49. doi: 10.1016/j.chembiol.2015.08.005. Epub 2015 Sep 10.

43.

The L3MBTL3 Methyl-Lysine Reader Domain Functions As a Dimer.

Baughman BM, Pattenden SG, Norris JL, James LI, Frye SV.

ACS Chem Biol. 2016 Mar 18;11(3):722-8. doi: 10.1021/acschembio.5b00632. Epub 2015 Sep 2. Retraction in: ACS Chem Biol. 2018 Jan 19;13(1):281.

44.

The promise and peril of chemical probes.

Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frederiksen M, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O'Hagan RC, Overington JP, Owen DR, Rosenberg SH, Roth B, Ross R, Schapira M, Schreiber SL, Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ.

Nat Chem Biol. 2015 Aug;11(8):536-41. doi: 10.1038/nchembio.1867. No abstract available. Erratum in: Nat Chem Biol. 2015 Aug;11(8):541. Roth, Brian [Corrected to Roth, Bryan] and Frederiksen, Mathias [Added]. Nat Chem Biol. 2015 Nov;11(11):887.

45.

Small Molecule Inhibition of MERTK Is Efficacious in Non-Small Cell Lung Cancer Models Independent of Driver Oncogene Status.

Cummings CT, Zhang W, Davies KD, Kirkpatrick GD, Zhang D, DeRyckere D, Wang X, Frye SV, Earp HS, Graham DK.

Mol Cancer Ther. 2015 Sep;14(9):2014-22. doi: 10.1158/1535-7163.MCT-15-0116. Epub 2015 Jul 10.

46.

Tumor Endothelial Cells with Distinct Patterns of TGFβ-Driven Endothelial-to-Mesenchymal Transition.

Xiao L, Kim DJ, Davis CL, McCann JV, Dunleavey JM, Vanderlinden AK, Xu N, Pattenden SG, Frye SV, Xu X, Onaitis M, Monaghan-Benson E, Burridge K, Dudley AC.

Cancer Res. 2015 Apr 1;75(7):1244-54. doi: 10.1158/0008-5472.CAN-14-1616. Epub 2015 Jan 29.

47.

Identification of a fragment-like small molecule ligand for the methyl-lysine binding protein, 53BP1.

Perfetti MT, Baughman BM, Dickson BM, Mu Y, Cui G, Mader P, Dong A, Norris JL, Rothbart SB, Strahl BD, Brown PJ, Janzen WP, Arrowsmith CH, Mer G, McBride KM, James LI, Frye SV.

ACS Chem Biol. 2015 Apr 17;10(4):1072-81. doi: 10.1021/cb500956g. Epub 2015 Jan 28.

48.

Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia.

Xu B, On DM, Ma A, Parton T, Konze KD, Pattenden SG, Allison DF, Cai L, Rockowitz S, Liu S, Liu Y, Li F, Vedadi M, Frye SV, Garcia BA, Zheng D, Jin J, Wang GG.

Blood. 2015 Jan 8;125(2):346-57. doi: 10.1182/blood-2014-06-581082. Epub 2014 Nov 13.

49.

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.

50.

Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8.

Ma A, Yu W, Li F, Bleich RM, Herold JM, Butler KV, Norris JL, Korboukh V, Tripathy A, Janzen WP, Arrowsmith CH, Frye SV, Vedadi M, Brown PJ, Jin J.

J Med Chem. 2014 Aug 14;57(15):6822-33. doi: 10.1021/jm500871s. Epub 2014 Jul 25.

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