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Items: 1 to 20 of 143

1.

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.

2.

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
3.

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
4.

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
5.

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
6.

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.

7.

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
8.

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.

9.

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
10.

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.

11.

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
12.

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
13.

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.

PMID:
29129718
14.

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.

PMID:
29129716
15.

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.

16.

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.

17.

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.

18.

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
19.

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
20.

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

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