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Items: 1 to 50 of 145

1.

BETP degradation simultaneously targets acute myelogenous leukemia stem cells and the microenvironment.

Piya S, Mu H, Bhattacharya S, Lorenzi PL, Davis RE, McQueen T, Ruvolo V, Baran N, Wang Z, Qian Y, Crews CM, Konopleava M, Ishizawa J, You MJ, Kantarjian H, Andreeff M, Borthakur G.

J Clin Invest. 2019 Feb 21;130. pii: 120654. doi: 10.1172/JCI120654.

2.

Evolving Rules for Protein Degradation? Insights from the Zinc Finger Degrome.

Buhimschi AD, Crews CM.

Biochemistry. 2019 Feb 19;58(7):861-864. doi: 10.1021/acs.biochem.8b01307. Epub 2019 Jan 25. No abstract available.

PMID:
30681837
3.

Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase.

Smith BE, Wang SL, Jaime-Figueroa S, Harbin A, Wang J, Hamman BD, Crews CM.

Nat Commun. 2019 Jan 10;10(1):131. doi: 10.1038/s41467-018-08027-7.

4.

Targeting nuclear β-catenin as therapy for post-myeloproliferative neoplasm secondary AML.

Saenz DT, Fiskus W, Manshouri T, Mill CP, Qian Y, Raina K, Rajapakshe K, Coarfa C, Soldi R, Bose P, Borthakur G, Kadia TM, Khoury JD, Masarova L, Nowak AJ, Sun B, Saenz DN, Kornblau SM, Horrigan S, Sharma S, Qiu P, Crews CM, Verstovsek S, Bhalla KN.

Leukemia. 2018 Dec 21. doi: 10.1038/s41375-018-0334-3. [Epub ahead of print]

PMID:
30575820
5.

Addressing Kinase-Independent Functions of Fak via PROTAC-Mediated Degradation.

Cromm PM, Samarasinghe KTG, Hines J, Crews CM.

J Am Chem Soc. 2018 Nov 28. doi: 10.1021/jacs.8b08008. [Epub ahead of print]

PMID:
30444612
6.

Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion.

Burslem GM, Song J, Chen X, Hines J, Crews CM.

J Am Chem Soc. 2018 Nov 19. doi: 10.1021/jacs.8b10320. [Epub ahead of print]

PMID:
30427680
7.

MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53.

Hines J, Lartigue S, Dong H, Qian Y, Crews CM.

Cancer Res. 2019 Jan 1;79(1):251-262. doi: 10.1158/0008-5472.CAN-18-2918. Epub 2018 Nov 1.

PMID:
30385614
8.

Androgen receptor degradation by the proteolysis-targeting chimera ARCC-4 outperforms enzalutamide in cellular models of prostate cancer drug resistance.

Salami J, Alabi S, Willard RR, Vitale NJ, Wang J, Dong H, Jin M, McDonnell DP, Crew AP, Neklesa TK, Crews CM.

Commun Biol. 2018 Aug 2;1:100. doi: 10.1038/s42003-018-0105-8. eCollection 2018.

9.

Efficient Synthesis of Immunomodulatory Drug Analogues Enables Exploration of Structure-Degradation Relationships.

Burslem GM, Ottis P, Jaime-Figueroa S, Morgan A, Cromm PM, Toure M, Crews CM.

ChemMedChem. 2018 Aug 10;13(15):1508-1512. doi: 10.1002/cmdc.201800271. Epub 2018 Jul 4.

PMID:
29870139
10.

Targeted protein unfolding uncovers a Golgi-specific transcriptional stress response.

Serebrenik YV, Hellerschmied D, Toure M, López-Giráldez F, Brookner D, Crews CM.

Mol Biol Cell. 2018 Jun 1;29(11):1284-1298. doi: 10.1091/mbc.E17-11-0693. Epub 2018 Apr 5.

11.

Targeting the C481S Ibrutinib-Resistance Mutation in Bruton's Tyrosine Kinase Using PROTAC-Mediated Degradation.

Buhimschi AD, Armstrong HA, Toure M, Jaime-Figueroa S, Chen TL, Lehman AM, Woyach JA, Johnson AJ, Byrd JC, Crews CM.

Biochemistry. 2018 Jul 3;57(26):3564-3575. doi: 10.1021/acs.biochem.8b00391. Epub 2018 Jun 14.

PMID:
29851337
12.

Protein targeting chimeric molecules specific for bromodomain and extra-terminal motif family proteins are active against pre-clinical models of multiple myeloma.

Zhang X, Lee HC, Shirazi F, Baladandayuthapani V, Lin H, Kuiatse I, Wang H, Jones RJ, Berkova Z, Singh RK, Lu J, Qian Y, Raina K, Coleman KG, Crews CM, Li B, Wang H, Hailemichael Y, Thomas SK, Wang Z, Davis RE, Orlowski RZ.

Leukemia. 2018 Oct;32(10):2224-2239. doi: 10.1038/s41375-018-0044-x. Epub 2018 Mar 27.

13.

Regeneration writ large.

Flowers GP, Crews CM.

Nature. 2018 Feb 1;554(7690):34-35. doi: 10.1038/d41586-017-09008-4. No abstract available.

PMID:
29388980
14.

Inducing Protein Degradation as a Therapeutic Strategy.

Crews CM.

J Med Chem. 2018 Jan 25;61(2):403-404. doi: 10.1021/acs.jmedchem.7b01333. Epub 2017 Nov 22. No abstract available.

PMID:
29164885
15.

Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead.

Bondeson DP, Smith BE, Burslem GM, Buhimschi AD, Hines J, Jaime-Figueroa S, Wang J, Hamman BD, Ishchenko A, Crews CM.

Cell Chem Biol. 2018 Jan 18;25(1):78-87.e5. doi: 10.1016/j.chembiol.2017.09.010. Epub 2017 Nov 9.

16.

The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study.

Burslem GM, Smith BE, Lai AC, Jaime-Figueroa S, McQuaid DC, Bondeson DP, Toure M, Dong H, Qian Y, Wang J, Crew AP, Hines J, Crews CM.

Cell Chem Biol. 2018 Jan 18;25(1):67-77.e3. doi: 10.1016/j.chembiol.2017.09.009. Epub 2017 Nov 9.

17.

Lineage tracing of genome-edited alleles reveals high fidelity axolotl limb regeneration.

Flowers GP, Sanor LD, Crews CM.

Elife. 2017 Sep 16;6. pii: e25726. doi: 10.7554/eLife.25726.

18.

The Proteasome in Modern Drug Discovery: Second Life of a Highly Valuable Drug Target.

Cromm PM, Crews CM.

ACS Cent Sci. 2017 Aug 23;3(8):830-838. doi: 10.1021/acscentsci.7b00252. Epub 2017 Aug 7. Review.

19.

Expeditious Synthesis of Isoquinolones and Isocoumarins with a Vinyl Borane as an Acetylene Equivalent.

Toure M, Jaime-Figueroa S, Burslem GM, Crews CM.

European J Org Chem. 2016 Aug;2016(24):4171-4175. doi: 10.1002/ejoc.201600575. Epub 2016 Jul 26.

20.

Small-Molecule Modulation of Protein Homeostasis.

Burslem GM, Crews CM.

Chem Rev. 2017 Sep 13;117(17):11269-11301. doi: 10.1021/acs.chemrev.7b00077. Epub 2017 Aug 4. Review.

PMID:
28777566
21.

Assessing Different E3 Ligases for Small Molecule Induced Protein Ubiquitination and Degradation.

Ottis P, Toure M, Cromm PM, Ko E, Gustafson JL, Crews CM.

ACS Chem Biol. 2017 Oct 20;12(10):2570-2578. doi: 10.1021/acschembio.7b00485. Epub 2017 Sep 5.

PMID:
28767222
22.

Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1.

Crew AP, Raina K, Dong H, Qian Y, Wang J, Vigil D, Serebrenik YV, Hamman BD, Morgan A, Ferraro C, Siu K, Neklesa TK, Winkler JD, Coleman KG, Crews CM.

J Med Chem. 2018 Jan 25;61(2):583-598. doi: 10.1021/acs.jmedchem.7b00635. Epub 2017 Jul 10.

PMID:
28692295
23.

BET protein proteolysis targeting chimera (PROTAC) exerts potent lethal activity against mantle cell lymphoma cells.

Sun B, Fiskus W, Qian Y, Rajapakshe K, Raina K, Coleman KG, Crew AP, Shen A, Saenz DT, Mill CP, Nowak AJ, Jain N, Zhang L, Wang M, Khoury JD, Coarfa C, Crews CM, Bhalla KN.

Leukemia. 2018 Feb;32(2):343-352. doi: 10.1038/leu.2017.207. Epub 2017 Jun 30.

PMID:
28663582
24.

Targeted Protein Degradation: from Chemical Biology to Drug Discovery.

Cromm PM, Crews CM.

Cell Chem Biol. 2017 Sep 21;24(9):1181-1190. doi: 10.1016/j.chembiol.2017.05.024. Epub 2017 Jun 22. Review.

25.

Targeted protein knockdown using small molecule degraders.

Raina K, Crews CM.

Curr Opin Chem Biol. 2017 Aug;39:46-53. doi: 10.1016/j.cbpa.2017.05.016. Epub 2017 Jun 9. Review.

26.

Waste disposal-An attractive strategy for cancer therapy.

Salami J, Crews CM.

Science. 2017 Mar 17;355(6330):1163-1167. doi: 10.1126/science.aam7340. Epub 2017 Mar 16. Review.

PMID:
28302825
27.

Proteolysis-Targeting Chimeras: Induced Protein Degradation as a Therapeutic Strategy.

Ottis P, Crews CM.

ACS Chem Biol. 2017 Apr 21;12(4):892-898. doi: 10.1021/acschembio.6b01068. Epub 2017 Mar 20. Review.

PMID:
28263557
28.

Targeted protein degradation by PROTACs.

Neklesa TK, Winkler JD, Crews CM.

Pharmacol Ther. 2017 Jun;174:138-144. doi: 10.1016/j.pharmthera.2017.02.027. Epub 2017 Feb 14. Review.

PMID:
28223226
29.

Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cells.

Saenz DT, Fiskus W, Qian Y, Manshouri T, Rajapakshe K, Raina K, Coleman KG, Crew AP, Shen A, Mill CP, Sun B, Qiu P, Kadia TM, Pemmaraju N, DiNardo C, Kim MS, Nowak AJ, Coarfa C, Crews CM, Verstovsek S, Bhalla KN.

Leukemia. 2017 Sep;31(9):1951-1961. doi: 10.1038/leu.2016.393. Epub 2017 Feb 2.

30.

Induced protein degradation: an emerging drug discovery paradigm.

Lai AC, Crews CM.

Nat Rev Drug Discov. 2017 Feb;16(2):101-114. doi: 10.1038/nrd.2016.211. Epub 2016 Nov 25. Review.

31.

Targeted Protein Degradation by Small Molecules.

Bondeson DP, Crews CM.

Annu Rev Pharmacol Toxicol. 2017 Jan 6;57:107-123. doi: 10.1146/annurev-pharmtox-010715-103507. Epub 2016 Oct 12. Review.

32.

From Powerful Review Articles to Research Breakthroughs.

Kostic M, Crews CM, Hertweck C, Shokat K, Suga H.

Cell Chem Biol. 2016 Aug 18;23(8):883-4. doi: 10.1016/j.chembiol.2016.08.002. No abstract available.

33.

PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer.

Raina K, Lu J, Qian Y, Altieri M, Gordon D, Rossi AM, Wang J, Chen X, Dong H, Siu K, Winkler JD, Crew AP, Crews CM, Coleman KG.

Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7124-9. doi: 10.1073/pnas.1521738113. Epub 2016 Jun 6.

34.

Inducing Protein Degradation as a Therapeutic Strategy.

Crews CM, Georg G, Wang S.

J Med Chem. 2016 Jun 9;59(11):5129-30. doi: 10.1021/acs.jmedchem.6b00735. Epub 2016 May 20. No abstract available.

PMID:
27199030
35.

Identification of MAC1: A Small Molecule That Rescues Spindle Bipolarity in Monastrol-Treated Cells.

Al-Obaidi N, Mitchison TJ, Crews CM, Mayer TU.

ACS Chem Biol. 2016 Jun 17;11(6):1544-51. doi: 10.1021/acschembio.6b00203. Epub 2016 Apr 28.

36.

Our Advisors, Our Ambassadors, Our Editorial Board Members.

Kostic M, Crews CM, Hertweck C, Shokat K, Suga H.

Cell Chem Biol. 2016 Mar 17;23(3):311-2. doi: 10.1016/j.chembiol.2016.03.004. No abstract available.

37.

Voices of Chemical Biology: Charting the Next Decade.

Kostic M, Crews CM, Hertweck C, Shokat K, Suga H.

Cell Chem Biol. 2016 Feb 18;23(2):199. doi: 10.1016/j.chembiol.2016.02.006. No abstract available.

38.

Cell Chemical Biology: Home of Exciting Chemical Biology.

Kostic M, Crews CM, Hertweck C, Shokat K, Suga H.

Cell Chem Biol. 2016 Jan 21;23(1):1-2. doi: 10.1016/j.chembiol.2016.01.001. No abstract available.

39.

Small-Molecule PROTACS: New Approaches to Protein Degradation.

Toure M, Crews CM.

Angew Chem Int Ed Engl. 2016 Feb 5;55(6):1966-73. doi: 10.1002/anie.201507978. Epub 2016 Jan 12. Review.

PMID:
26756721
40.

Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL.

Lai AC, Toure M, Hellerschmied D, Salami J, Jaime-Figueroa S, Ko E, Hines J, Crews CM.

Angew Chem Int Ed Engl. 2016 Jan 11;55(2):807-10. doi: 10.1002/anie.201507634. Epub 2015 Nov 23.

41.

Development of small molecules targeting the pseudokinase Her3.

Lim SM, Xie T, Westover KD, Ficarro SB, Tae HS, Gurbani D, Sim T, Marto JA, Jänne PA, Crews CM, Gray NS.

Bioorg Med Chem Lett. 2015 Aug 15;25(16):3382-9. doi: 10.1016/j.bmcl.2015.04.103. Epub 2015 May 11.

42.

Small-Molecule-Mediated Degradation of the Androgen Receptor through Hydrophobic Tagging.

Gustafson JL, Neklesa TK, Cox CS, Roth AG, Buckley DL, Tae HS, Sundberg TB, Stagg DB, Hines J, McDonnell DP, Norris JD, Crews CM.

Angew Chem Int Ed Engl. 2015 Aug 10;54(33):9659-62. doi: 10.1002/anie.201503720. Epub 2015 Jun 17.

43.

Catalytic in vivo protein knockdown by small-molecule PROTACs.

Bondeson DP, Mares A, Smith IE, Ko E, Campos S, Miah AH, Mulholland KE, Routly N, Buckley DL, Gustafson JL, Zinn N, Grandi P, Shimamura S, Bergamini G, Faelth-Savitski M, Bantscheff M, Cox C, Gordon DA, Willard RR, Flanagan JJ, Casillas LN, Votta BJ, den Besten W, Famm K, Kruidenier L, Carter PS, Harling JD, Churcher I, Crews CM.

Nat Chem Biol. 2015 Aug;11(8):611-7. doi: 10.1038/nchembio.1858. Epub 2015 Jun 10.

44.

HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins.

Buckley DL, Raina K, Darricarrere N, Hines J, Gustafson JL, Smith IE, Miah AH, Harling JD, Crews CM.

ACS Chem Biol. 2015 Aug 21;10(8):1831-7. doi: 10.1021/acschembio.5b00442. Epub 2015 Jun 23.

45.

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4.

Lu J, Qian Y, Altieri M, Dong H, Wang J, Raina K, Hines J, Winkler JD, Crew AP, Coleman K, Crews CM.

Chem Biol. 2015 Jun 18;22(6):755-63. doi: 10.1016/j.chembiol.2015.05.009. Epub 2015 Jun 4.

46.

Generating and identifying axolotls with targeted mutations using Cas9 RNA-guided nuclease.

Flowers GP, Crews CM.

Methods Mol Biol. 2015;1290:279-95. doi: 10.1007/978-1-4939-2495-0_22.

PMID:
25740494
47.

Pharmacological targeting of the pseudokinase Her3.

Xie T, Lim SM, Westover KD, Dodge ME, Ercan D, Ficarro SB, Udayakumar D, Gurbani D, Tae HS, Riddle SM, Sim T, Marto JA, Jänne PA, Crews CM, Gray NS.

Nat Chem Biol. 2014 Dec;10(12):1006-12. doi: 10.1038/nchembio.1658. Epub 2014 Oct 19.

48.

Targeted protein destabilization reveals an estrogen-mediated ER stress response.

Raina K, Noblin DJ, Serebrenik YV, Adams A, Zhao C, Crews CM.

Nat Chem Biol. 2014 Nov;10(11):957-62. doi: 10.1038/nchembio.1638. Epub 2014 Sep 21.

49.

Highly efficient targeted mutagenesis in axolotl using Cas9 RNA-guided nuclease.

Flowers GP, Timberlake AT, McLean KC, Monaghan JR, Crews CM.

Development. 2014 May;141(10):2165-71. doi: 10.1242/dev.105072. Epub 2014 Apr 24.

50.

Small-molecule control of intracellular protein levels through modulation of the ubiquitin proteasome system.

Buckley DL, Crews CM.

Angew Chem Int Ed Engl. 2014 Feb 24;53(9):2312-30. doi: 10.1002/anie.201307761. Epub 2014 Jan 23. Review.

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