-
1
-
-
12344321686
-
The receptor concept: A continuing evolution
-
Limbird, L. E. The receptor concept: a continuing evolution Mol. Interventions 2004, 4, 326-336 10.1124/mi.4.6.6
-
(2004)
Mol. Interventions
, vol.4
, pp. 326-336
-
-
Limbird, L.E.1
-
2
-
-
3142781225
-
Small-molecule inhibitors of protein-protein interactions: Progressing towards the dream
-
Arkin, M. R.; Wells, J. A. Small-molecule inhibitors of protein-protein interactions: progressing towards the dream Nat. Rev. Drug Discovery 2004, 3, 301-317 10.1038/nrd1343
-
(2004)
Nat. Rev. Drug Discovery
, vol.3
, pp. 301-317
-
-
Arkin, M.R.1
Wells, J.A.2
-
3
-
-
84947608741
-
Oligonucleotide therapeutics: Chemistry, delivery and clinical progress
-
Sharma, V. K.; Watts, J. K. Oligonucleotide therapeutics: chemistry, delivery and clinical progress Future Med. Chem. 2015, 7, 2221-2242 10.4155/fmc.15.144
-
(2015)
Future Med. Chem.
, vol.7
, pp. 2221-2242
-
-
Sharma, V.K.1
Watts, J.K.2
-
4
-
-
84986898390
-
Applications of CRISPR technologies in research and beyond
-
Barrangou, R.; Doudna, J. A. Applications of CRISPR technologies in research and beyond Nat. Biotechnol. 2016, 34, 933-941 10.1038/nbt.3659
-
(2016)
Nat. Biotechnol.
, vol.34
, pp. 933-941
-
-
Barrangou, R.1
Doudna, J.A.2
-
5
-
-
85004007274
-
Small molecule-mediated protein knockdown as a new approach to drug discovery
-
Tinworth, C. P.; Lithgow, H.; Churcher, I. Small molecule-mediated protein knockdown as a new approach to drug discovery MedChemComm 2016, 7, 2206-2216 10.1039/C6MD00347H
-
(2016)
MedChemComm
, vol.7
, pp. 2206-2216
-
-
Tinworth, C.P.1
Lithgow, H.2
Churcher, I.3
-
6
-
-
85020454226
-
Targeted protein knockdown using small molecule degraders
-
Raina, K.; Crews, C. M. Targeted protein knockdown using small molecule degraders Curr. Opin. Chem. Biol. 2017, 39, 46-53 10.1016/j.cbpa.2017.05.016
-
(2017)
Curr. Opin. Chem. Biol.
, vol.39
, pp. 46-53
-
-
Raina, K.1
Crews, C.M.2
-
7
-
-
85013058483
-
Targeted protein degradation by PROTACs
-
Neklesa, T. K.; Winkler, J. D.; Crews, C. M. Targeted protein degradation by PROTACs Pharmacol. Ther. 2017, 174, 138-144 10.1016/j.pharmthera.2017.02.027
-
(2017)
Pharmacol. Ther.
, vol.174
, pp. 138-144
-
-
Neklesa, T.K.1
Winkler, J.D.2
Crews, C.M.3
-
8
-
-
84996848891
-
Induced protein degradation: An emerging drug discovery paradigm
-
Lai, A. C.; Crews, C. M. Induced protein degradation: an emerging drug discovery paradigm Nat. Rev. Drug Discovery 2017, 16, 101-114 10.1038/nrd.2016.211
-
(2017)
Nat. Rev. Drug Discovery
, vol.16
, pp. 101-114
-
-
Lai, A.C.1
Crews, C.M.2
-
9
-
-
84961285814
-
Small-molecule PROTACS: New approaches to protein degradation
-
Toure, M.; Crews, C. M. Small-molecule PROTACS: new approaches to protein degradation Angew. Chem., Int. Ed. 2016, 55, 1966-1973 10.1002/anie.201507978
-
(2016)
Angew. Chem., Int. Ed.
, vol.55
, pp. 1966-1973
-
-
Toure, M.1
Crews, C.M.2
-
10
-
-
85021144702
-
Targeted protein degradation: From chemical biology to drug discovery
-
Cromm, P. M.; Crews, C. M. Targeted protein degradation: from chemical biology to drug discovery Cell Chem. Biol. 2017, 24, 1181-1190 10.1016/j.chembiol.2017.05.024
-
(2017)
Cell Chem. Biol.
, vol.24
, pp. 1181-1190
-
-
Cromm, P.M.1
Crews, C.M.2
-
11
-
-
84994353647
-
Emerging Methods in Chemoproteomics with Relevance to Drug Discovery
-
Kasid, U. Clarke, R. Methods in Molecular Biology, Humana Press: New York, NY, DOI
-
Nguyen, C.; West, G. M.; Geoghegan, K. F. Emerging Methods in Chemoproteomics with Relevance to Drug Discovery. In Cancer Gene Networks; Kasid, U.; Clarke, R., Eds.; Methods in Molecular Biology, Vol. 1513; Humana Press: New York, NY, 2017; DOI: 10.1007/978-1-4939-6539-7-2.
-
(2017)
Cancer Gene Networks
, vol.1513
-
-
Nguyen, C.1
West, G.M.2
Geoghegan, K.F.3
-
12
-
-
84979914402
-
The delivery of therapeutic oligonucleotides
-
Juliano, R. L. The delivery of therapeutic oligonucleotides Nucleic Acids Res. 2016, 44, 6518-6548 10.1093/nar/gkw236
-
(2016)
Nucleic Acids Res.
, vol.44
, pp. 6518-6548
-
-
Juliano, R.L.1
-
13
-
-
84856373151
-
Proteasome inhibitors: An expanding army attacking a unique target
-
Kisselev, A. F.; van der Linden, W. A.; Overkleeft, H. S. Proteasome inhibitors: an expanding army attacking a unique target Chem. Biol. 2012, 19, 99-115 10.1016/j.chembiol.2012.01.003
-
(2012)
Chem. Biol.
, vol.19
, pp. 99-115
-
-
Kisselev, A.F.1
Van Der Linden, W.A.2
Overkleeft, H.S.3
-
14
-
-
79251473377
-
Will the ubiquitin system furnish as many drug targets as protein kinases?
-
Cohen, P.; Tcherpakov, M. Will the ubiquitin system furnish as many drug targets as protein kinases? Cell 2010, 143, 686-693 10.1016/j.cell.2010.11.016
-
(2010)
Cell
, vol.143
, pp. 686-693
-
-
Cohen, P.1
Tcherpakov, M.2
-
15
-
-
78650824534
-
Ubiquitin-like protein conjugation and the ubiquitin-proteasome system as drug targets
-
Bedford, L.; Lowe, J.; Dick, L. R.; Mayer, R. J.; Brownell, J. E. Ubiquitin-like protein conjugation and the ubiquitin-proteasome system as drug targets Nat. Rev. Drug Discovery 2011, 10, 29-46 10.1038/nrd3321
-
(2011)
Nat. Rev. Drug Discovery
, vol.10
, pp. 29-46
-
-
Bedford, L.1
Lowe, J.2
Dick, L.R.3
Mayer, R.J.4
Brownell, J.E.5
-
16
-
-
80051978811
-
The predator becomes the prey: Regulating the ubiquitin system by ubiquitylation and degradation
-
Weissman, A. M.; Shabek, N.; Ciechanover, A. The predator becomes the prey: regulating the ubiquitin system by ubiquitylation and degradation Nat. Rev. Mol. Cell Biol. 2011, 12, 605-620 10.1038/nrm3173
-
(2011)
Nat. Rev. Mol. Cell Biol.
, vol.12
, pp. 605-620
-
-
Weissman, A.M.1
Shabek, N.2
Ciechanover, A.3
-
17
-
-
11244309014
-
Proteolysis: From the lysosome to ubiquitin and the proteasome
-
Ciechanover, A. Proteolysis: from the lysosome to ubiquitin and the proteasome Nat. Rev. Mol. Cell Biol. 2005, 6, 79-87 10.1038/nrm1552
-
(2005)
Nat. Rev. Mol. Cell Biol.
, vol.6
, pp. 79-87
-
-
Ciechanover, A.1
-
18
-
-
0026663539
-
The ubiquitin system for protein degradation
-
Hershko, A.; Ciechanover, A. The ubiquitin system for protein degradation Annu. Rev. Biochem. 1992, 61, 761-807 10.1146/annurev.bi.61.070192.003553
-
(1992)
Annu. Rev. Biochem.
, vol.61
, pp. 761-807
-
-
Hershko, A.1
Ciechanover, A.2
-
19
-
-
84901466274
-
Perilous journey: A tour of the ubiquitin-proteasome system
-
Kleiger, G.; Mayor, T. Perilous journey: a tour of the ubiquitin-proteasome system Trends Cell Biol. 2014, 24, 352-359 10.1016/j.tcb.2013.12.003
-
(2014)
Trends Cell Biol.
, vol.24
, pp. 352-359
-
-
Kleiger, G.1
Mayor, T.2
-
20
-
-
70350150000
-
The emerging complexity of protein ubiquitination
-
Komander, D. The emerging complexity of protein ubiquitination Biochem. Soc. Trans. 2009, 37, 937-953 10.1042/BST0370937
-
(2009)
Biochem. Soc. Trans.
, vol.37
, pp. 937-953
-
-
Komander, D.1
-
21
-
-
84876720161
-
A comprehensive mathematical model for three-body binding equilibria
-
Douglass, E. F.; Miller, C. J.; Sparer, G.; Shapiro, H.; Spiegel, D. A. A comprehensive mathematical model for three-body binding equilibria J. Am. Chem. Soc. 2013, 135, 6092-6099 10.1021/ja311795d
-
(2013)
J. Am. Chem. Soc.
, vol.135
, pp. 6092-6099
-
-
Douglass, E.F.1
Miller, C.J.2
Sparer, G.3
Shapiro, H.4
Spiegel, D.A.5
-
22
-
-
85015018807
-
Structural basis of PROTAC cooperative recognition for selective protein degradation
-
Gadd, M. S.; Testa, A.; Lucas, X.; Chan, K. H.; Chen, W.; Lamont, D. J.; Zengerle, M.; Ciulli, A. Structural basis of PROTAC cooperative recognition for selective protein degradation Nat. Chem. Biol. 2017, 13, 514-521 10.1038/nchembio.2329
-
(2017)
Nat. Chem. Biol.
, vol.13
, pp. 514-521
-
-
Gadd, M.S.1
Testa, A.2
Lucas, X.3
Chan, K.H.4
Chen, W.5
Lamont, D.J.6
Zengerle, M.7
Ciulli, A.8
-
23
-
-
33751247917
-
Evaluation of a diffusion-driven mechanism for substrate ubiquitination by the SCF-Cdc34 ubiquitin ligase complex
-
Petroski, M. D.; Kleiger, G.; Deshaies, R. J. Evaluation of a diffusion-driven mechanism for substrate ubiquitination by the SCF-Cdc34 ubiquitin ligase complex Mol. Cell 2006, 24, 523-534 10.1016/j.molcel.2006.10.010
-
(2006)
Mol. Cell
, vol.24
, pp. 523-534
-
-
Petroski, M.D.1
Kleiger, G.2
Deshaies, R.J.3
-
24
-
-
68049084674
-
Breaking the chains: Structure and function of the deubiquitinases
-
Komander, D.; Clague, M. J.; Urbe, S. Breaking the chains: structure and function of the deubiquitinases Nat. Rev. Mol. Cell Biol. 2009, 10, 550-563 10.1038/nrm2731
-
(2009)
Nat. Rev. Mol. Cell Biol.
, vol.10
, pp. 550-563
-
-
Komander, D.1
Clague, M.J.2
Urbe, S.3
-
25
-
-
84871995188
-
The lysine48-based polyubiquitin chain proteasomal signal: Not a single child anymore
-
Kravtsova-Ivantsiv, Y.; Sommer, T.; Ciechanover, A. The lysine48-based polyubiquitin chain proteasomal signal: not a single child anymore Angew. Chem., Int. Ed. 2013, 52, 192-198 10.1002/anie.201205656
-
(2013)
Angew. Chem., Int. Ed.
, vol.52
, pp. 192-198
-
-
Kravtsova-Ivantsiv, Y.1
Sommer, T.2
Ciechanover, A.3
-
26
-
-
84947760173
-
Regulation of proteasomal degradation by modulating proteasomal initiation regions
-
Takahashi, K.; Matouschek, A.; Inobe, T. Regulation of proteasomal degradation by modulating proteasomal initiation regions ACS Chem. Biol. 2015, 10, 2537-2543 10.1021/acschembio.5b00554
-
(2015)
ACS Chem. Biol.
, vol.10
, pp. 2537-2543
-
-
Takahashi, K.1
Matouschek, A.2
Inobe, T.3
-
27
-
-
84978924611
-
Ubiquitin-like domains can target to the proteasome but proteolysis requires a disordered region
-
Yu, H.; Kago, G.; Yellman, C. M.; Matouschek, A. Ubiquitin-like domains can target to the proteasome but proteolysis requires a disordered region EMBO J. 2016, 35, 1522-1536 10.15252/embj.201593147
-
(2016)
EMBO J.
, vol.35
, pp. 1522-1536
-
-
Yu, H.1
Kago, G.2
Yellman, C.M.3
Matouschek, A.4
-
28
-
-
84878270699
-
Rad23 escapes degradation because it lacks a proteasome initiation region
-
Fishbain, S.; Prakash, S.; Herrig, A.; Elsasser, S.; Matouschek, A. Rad23 escapes degradation because it lacks a proteasome initiation region Nat. Commun. 2011, 2, 192 10.1038/ncomms1194
-
(2011)
Nat. Commun.
, vol.2
, pp. 192
-
-
Fishbain, S.1
Prakash, S.2
Herrig, A.3
Elsasser, S.4
Matouschek, A.5
-
29
-
-
59449085150
-
Global analysis of cellular protein translation by pulsed SILAC
-
Schwanhausser, B.; Gossen, M.; Dittmar, G.; Selbach, M. Global analysis of cellular protein translation by pulsed SILAC Proteomics 2009, 9, 205-209 10.1002/pmic.200800275
-
(2009)
Proteomics
, vol.9
, pp. 205-209
-
-
Schwanhausser, B.1
Gossen, M.2
Dittmar, G.3
Selbach, M.4
-
30
-
-
79956322553
-
Global quantification of mammalian gene expression control
-
Schwanhausser, B.; Busse, D.; Li, N.; Dittmar, G.; Schuchhardt, J.; Wolf, J.; Chen, W.; Selbach, M. Global quantification of mammalian gene expression control Nature 2011, 473, 337-342 10.1038/nature10098
-
(2011)
Nature
, vol.473
, pp. 337-342
-
-
Schwanhausser, B.1
Busse, D.2
Li, N.3
Dittmar, G.4
Schuchhardt, J.5
Wolf, J.6
Chen, W.7
Selbach, M.8
-
31
-
-
0029075876
-
Redirecting the specificity of ubiquitination by modifying ubiquitin-conjugating enzymes
-
Gosink, M. M.; Vierstra, R. D. Redirecting the specificity of ubiquitination by modifying ubiquitin-conjugating enzymes Proc. Natl. Acad. Sci. U. S. A. 1995, 92, 9117-9121 10.1073/pnas.92.20.9117
-
(1995)
Proc. Natl. Acad. Sci. U. S. A.
, vol.92
, pp. 9117-9121
-
-
Gosink, M.M.1
Vierstra, R.D.2
-
33
-
-
0035902475
-
Protacs: Chimeric molecules that target proteins to the Skp1-Cullin-F box complex for ubiquitination and degradation
-
Sakamoto, K. M.; Kim, K. B.; Kumagai, A.; Mercurio, F.; Crews, C. M.; Deshaies, R. J. Protacs: chimeric molecules that target proteins to the Skp1-Cullin-F box complex for ubiquitination and degradation Proc. Natl. Acad. Sci. U. S. A. 2001, 98, 8554-8559 10.1073/pnas.141230798
-
(2001)
Proc. Natl. Acad. Sci. U. S. A.
, vol.98
, pp. 8554-8559
-
-
Sakamoto, K.M.1
Kim, K.B.2
Kumagai, A.3
Mercurio, F.4
Crews, C.M.5
Deshaies, R.J.6
-
34
-
-
1642285590
-
Development of Protacs to target cancer-promoting proteins for ubiquitination and degradation
-
Sakamoto, K. M.; Kim, K. B.; Verma, R.; Ransick, A.; Stein, B.; Crews, C. M.; Deshaies, R. J. Development of Protacs to target cancer-promoting proteins for ubiquitination and degradation Mol. Cell. Proteomics 2003, 2, 1350-1358 10.1074/mcp.T300009-MCP200
-
(2003)
Mol. Cell. Proteomics
, vol.2
, pp. 1350-1358
-
-
Sakamoto, K.M.1
Kim, K.B.2
Verma, R.3
Ransick, A.4
Stein, B.5
Crews, C.M.6
Deshaies, R.J.7
-
35
-
-
55549137044
-
Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics
-
Schneekloth, A. R.; Pucheault, M.; Tae, H. S.; Crews, C. M. Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics Bioorg. Med. Chem. Lett. 2008, 18, 5904-5908 10.1016/j.bmcl.2008.07.114
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 5904-5908
-
-
Schneekloth, A.R.1
Pucheault, M.2
Tae, H.S.3
Crews, C.M.4
-
36
-
-
84887454928
-
Characterization of a new class of androgen receptor antagonists with potential therapeutic application in advanced prostate cancer
-
Li, H.; Hassona, M. D. H.; Lack, N. A.; Axerio-Cilies, P.; Leblanc, E.; Tavassoli, P.; Kanaan, N.; Frewin, K.; Singh, K.; Adomat, H.; Boehm, K. J.; Prinz, H.; Guns, E. T.; Rennie, P. S.; Cherkasov, A. Characterization of a new class of androgen receptor antagonists with potential therapeutic application in advanced prostate cancer Mol. Cancer Ther. 2013, 12, 2425-2435 10.1158/1535-7163.MCT-13-0267
-
(2013)
Mol. Cancer Ther.
, vol.12
, pp. 2425-2435
-
-
Li, H.1
Hassona, M.D.H.2
Lack, N.A.3
Axerio-Cilies, P.4
Leblanc, E.5
Tavassoli, P.6
Kanaan, N.7
Frewin, K.8
Singh, K.9
Adomat, H.10
Boehm, K.J.11
Prinz, H.12
Guns, E.T.13
Rennie, P.S.14
Cherkasov, A.15
-
37
-
-
0035289779
-
Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
-
Lipinski, C. A.; Lombardo, F.; Dominy, B. W.; Feeney, P. J. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings Adv. Drug Delivery Rev. 1997, 23, 3-25 10.1016/S0169-409X(96)00423-1
-
(1997)
Adv. Drug Delivery Rev.
, vol.23
, pp. 3-25
-
-
Lipinski, C.A.1
Lombardo, F.2
Dominy, B.W.3
Feeney, P.J.4
-
38
-
-
84856405594
-
Going further than Lipinski's rule in drug design
-
Walters, W. P. Going further than Lipinski's rule in drug design Expert Opin. Drug Discovery 2012, 7, 99-107 10.1517/17460441.2012.648612
-
(2012)
Expert Opin. Drug Discovery
, vol.7
, pp. 99-107
-
-
Walters, W.P.1
-
39
-
-
84868522211
-
Small-molecule inhibitors of the interaction between the E3 ligase VHL and HIF1α
-
Buckley, D. L.; Gustafson, J. L.; Van Molle, I.; Roth, A. G.; Tae, H. S.; Gareiss, P. C.; Jorgensen, W. L.; Ciulli, A.; Crews, C. M. Small-molecule inhibitors of the interaction between the E3 ligase VHL and HIF1α Angew. Chem., Int. Ed. 2012, 51, 11463-11467 10.1002/anie.201206231
-
(2012)
Angew. Chem., Int. Ed.
, vol.51
, pp. 11463-11467
-
-
Buckley, D.L.1
Gustafson, J.L.2
Van Molle, I.3
Roth, A.G.4
Tae, H.S.5
Gareiss, P.C.6
Jorgensen, W.L.7
Ciulli, A.8
Crews, C.M.9
-
40
-
-
84858201095
-
Targeting the von Hippel-Lindau E3 ubiquitin ligase using small molecules to disrupt the VHL/HIF-1α interaction
-
Buckley, D. L.; Van Molle, I.; Gareiss, P. C.; Tae, H. S.; Michel, J.; Noblin, D. J.; Jorgensen, W. L.; Ciulli, A.; Crews, C. M. Targeting the von Hippel-Lindau E3 ubiquitin ligase using small molecules to disrupt the VHL/HIF-1α interaction J. Am. Chem. Soc. 2012, 134, 4465-4468 10.1021/ja209924v
-
(2012)
J. Am. Chem. Soc.
, vol.134
, pp. 4465-4468
-
-
Buckley, D.L.1
Van Molle, I.2
Gareiss, P.C.3
Tae, H.S.4
Michel, J.5
Noblin, D.J.6
Jorgensen, W.L.7
Ciulli, A.8
Crews, C.M.9
-
41
-
-
84939794726
-
HaloPROTACS: Use of small molecule PROTACs to induce degradation of HaloTag fusion proteins
-
Buckley, D. L.; Raina, K.; Darricarrere, N.; Hines, J.; Gustafson, J. L.; Smith, I. E.; Miah, A. H.; Harling, J. D.; Crews, C. M. HaloPROTACS: Use of small molecule PROTACs to induce degradation of HaloTag fusion proteins ACS Chem. Biol. 2015, 10, 1831-1837 10.1021/acschembio.5b00442
-
(2015)
ACS Chem. Biol.
, vol.10
, pp. 1831-1837
-
-
Buckley, D.L.1
Raina, K.2
Darricarrere, N.3
Hines, J.4
Gustafson, J.L.5
Smith, I.E.6
Miah, A.H.7
Harling, J.D.8
Crews, C.M.9
-
42
-
-
84937534394
-
-
WO2013/106646A2
-
Crews, C. M.; Buckley, D. L.; Ciulli, A.; Jorgensen, W.; Gareiss, P. C.; Van Molle, I.; Gustafson, J.; Tae, H.-S.; Michel, J.; Hoyer, D. W.; Roth, A. G.; Harling, J. D.; Smith, I. E. D.; Miah, A. H.; Campos, S. A.; Le, J. Compounds and Methods for the Inhibition of VCB E3 Ubiquitin Ligase. WO2013/106646A2, 2013.
-
(2013)
Compounds and Methods for the Inhibition of VCB E3 Ubiquitin Ligase
-
-
Crews, C.M.1
Buckley, D.L.2
Ciulli, A.3
Jorgensen, W.4
Gareiss, P.C.5
Van Molle, I.6
Gustafson, J.7
Tae, H.-S.8
Michel, J.9
Hoyer, D.W.10
Roth, A.G.11
Harling, J.D.12
Smith, I.E.D.13
Miah, A.H.14
Campos, S.A.15
Le, J.16
-
43
-
-
84868026890
-
Dissecting fragment-based lead discovery at the von Hippel-Lindau protein:hypoxia inducible factor 1α protein-protein interface
-
Van Molle, I.; Thomann, A.; Buckley, D. L.; So, E. C.; Lang, S.; Crews, C. M.; Ciulli, A. Dissecting fragment-based lead discovery at the von Hippel-Lindau protein:hypoxia inducible factor 1α protein-protein interface Chem. Biol. 2012, 19, 1300-1312 10.1016/j.chembiol.2012.08.015
-
(2012)
Chem. Biol.
, vol.19
, pp. 1300-1312
-
-
Van Molle, I.1
Thomann, A.2
Buckley, D.L.3
So, E.C.4
Lang, S.5
Crews, C.M.6
Ciulli, A.7
-
44
-
-
84908373179
-
Structure-guided design and optimization of small molecules targeting the protein-protein interaction between the von Hippel-Lindau (VHL) E3 ubiquitin ligase and the hypoxia inducible factor (HIF) alpha subunit with in vitro nanomolar affinities
-
Galdeano, C.; Gadd, M. S.; Soares, P.; Scaffidi, S.; Van Molle, I.; Birced, I.; Hewitt, S.; Dias, D. M.; Ciulli, A. Structure-guided design and optimization of small molecules targeting the protein-protein interaction between the von Hippel-Lindau (VHL) E3 ubiquitin ligase and the hypoxia inducible factor (HIF) alpha subunit with in vitro nanomolar affinities J. Med. Chem. 2014, 57, 8657-8663 10.1021/jm5011258
-
(2014)
J. Med. Chem.
, vol.57
, pp. 8657-8663
-
-
Galdeano, C.1
Gadd, M.S.2
Soares, P.3
Scaffidi, S.4
Van Molle, I.5
Birced, I.6
Hewitt, S.7
Dias, D.M.8
Ciulli, A.9
-
45
-
-
84937514576
-
Catalytic in vivo protein knockdown by small-molecule PROTACs
-
Bondeson, D. P.; Mares, A.; Smith, I. E.; Ko, E.; Campos, S.; Miah, A. H.; Mulholland, K. E.; Routly, N.; Buckley, D. L.; Gustafson, J. L.; Zinn, N.; Grandi, P.; Shimamura, S.; Bergamini, G.; Faelth-Savitski, M.; Bantscheff, M.; Cox, C.; Gordon, D. A.; Willard, R. R.; Flanagan, J. J.; Casillas, L. N.; Votta, B. J.; den Besten, W.; Famm, K.; Kruidenier, L.; Carter, P. S.; Harling, J. D.; Churcher, I.; Crews, C. M. Catalytic in vivo protein knockdown by small-molecule PROTACs Nat. Chem. Biol. 2015, 11, 611-617 10.1038/nchembio.1858
-
(2015)
Nat. Chem. Biol.
, vol.11
, pp. 611-617
-
-
Bondeson, D.P.1
Mares, A.2
Smith, I.E.3
Ko, E.4
Campos, S.5
Miah, A.H.6
Mulholland, K.E.7
Routly, N.8
Buckley, D.L.9
Gustafson, J.L.10
Zinn, N.11
Grandi, P.12
Shimamura, S.13
Bergamini, G.14
Faelth-Savitski, M.15
Bantscheff, M.16
Cox, C.17
Gordon, D.A.18
Willard, R.R.19
Flanagan, J.J.20
Casillas, L.N.21
Votta, B.J.22
Den Besten, W.23
Famm, K.24
Kruidenier, L.25
Carter, P.S.26
Harling, J.D.27
Churcher, I.28
Crews, C.M.29
more..
-
46
-
-
84932634729
-
Phthalimide conjugation as a strategy for in vivo target protein degradation
-
Winter, G. E.; Buckley, D. L.; Paulk, J.; Roberts, J. M.; Souza, A.; Dhe-Paganon, S.; Bradner, J. E. Phthalimide conjugation as a strategy for in vivo target protein degradation Science 2015, 348, 1376-1381 10.1126/science.aab1433
-
(2015)
Science
, vol.348
, pp. 1376-1381
-
-
Winter, G.E.1
Buckley, D.L.2
Paulk, J.3
Roberts, J.M.4
Souza, A.5
Dhe-Paganon, S.6
Bradner, J.E.7
-
47
-
-
84931560527
-
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, J. D.; Crew, A. P.; Coleman, K.; Crews, C. M. Hijacking the E3 ubiquitin ligase cereblon to efficiently target BRD4 Chem. Biol. 2015, 22, 755-763 10.1016/j.chembiol.2015.05.009
-
(2015)
Chem. Biol.
, vol.22
, pp. 755-763
-
-
Lu, J.1
Qian, Y.2
Altieri, M.3
Dong, H.4
Wang, J.5
Raina, K.6
Hines, J.7
Winkler, J.D.8
Crew, A.P.9
Coleman, K.10
Crews, C.M.11
-
48
-
-
84939788143
-
Selective small molecule induced degradation of the BET bromodomain Protein BRD4
-
Zengerle, M.; Chan, K. H.; Ciulli, A. Selective small molecule induced degradation of the BET bromodomain Protein BRD4 ACS Chem. Biol. 2015, 10, 1770-1777 10.1021/acschembio.5b00216
-
(2015)
ACS Chem. Biol.
, vol.10
, pp. 1770-1777
-
-
Zengerle, M.1
Chan, K.H.2
Ciulli, A.3
-
49
-
-
9944261150
-
Trial of thalidomide in insomnia associated with the third trimester
-
Nulsen, R. O. Trial of thalidomide in insomnia associated with the third trimester Am. J. Obstet. Gynecol. 1961, 81, 1245-1248 10.1016/S0002-9378(15)33360-3
-
(1961)
Am. J. Obstet. Gynecol.
, vol.81
, pp. 1245-1248
-
-
Nulsen, R.O.1
-
50
-
-
84905568369
-
Structure of the DDB1-CRBN E3 ubiquitin ligase in complex with thalidomide
-
Fischer, E. S.; Bohm, K.; Lydeard, J. R.; Yang, H.; Stadler, M. B.; Cavadini, S.; Nagel, J.; Serluca, F.; Acker, V.; Lingaraju, G. M.; Tichkule, R. B.; Schebesta, M.; Forrester, W. C.; Schirle, M.; Hassiepen, U.; Ottl, J.; Hild, M.; Beckwith, R. E.; Harper, J. W.; Jenkins, J. L.; Thoma, N. H. Structure of the DDB1-CRBN E3 ubiquitin ligase in complex with thalidomide Nature 2014, 512, 49-53 10.1038/nature13527
-
(2014)
Nature
, vol.512
, pp. 49-53
-
-
Fischer, E.S.1
Bohm, K.2
Lydeard, J.R.3
Yang, H.4
Stadler, M.B.5
Cavadini, S.6
Nagel, J.7
Serluca, F.8
Acker, V.9
Lingaraju, G.M.10
Tichkule, R.B.11
Schebesta, M.12
Forrester, W.C.13
Schirle, M.14
Hassiepen, U.15
Ottl, J.16
Hild, M.17
Beckwith, R.E.18
Harper, J.W.19
Jenkins, J.L.20
Thoma, N.H.21
more..
-
51
-
-
84916880505
-
Structure of the human Cereblon-DDB1-lenalidomide complex reveals basis for responsiveness to thalidomide analogs
-
Chamberlain, P. P.; Lopez-Girona, A.; Miller, K.; Carmel, G.; Pagarigan, B.; Chie-Leon, B.; Rychak, E.; Corral, L. G.; Ren, Y. J.; Wang, M.; Riley, M.; Delker, S. L.; Ito, T.; Ando, H.; Mori, T.; Hirano, Y.; Handa, H.; Hakoshima, T.; Daniel, T. O.; Cathers, B. E. Structure of the human Cereblon-DDB1-lenalidomide complex reveals basis for responsiveness to thalidomide analogs Nat. Struct. Mol. Biol. 2014, 21, 803-809 10.1038/nsmb.2874
-
(2014)
Nat. Struct. Mol. Biol.
, vol.21
, pp. 803-809
-
-
Chamberlain, P.P.1
Lopez-Girona, A.2
Miller, K.3
Carmel, G.4
Pagarigan, B.5
Chie-Leon, B.6
Rychak, E.7
Corral, L.G.8
Ren, Y.J.9
Wang, M.10
Riley, M.11
Delker, S.L.12
Ito, T.13
Ando, H.14
Mori, T.15
Hirano, Y.16
Handa, H.17
Hakoshima, T.18
Daniel, T.O.19
Cathers, B.E.20
more..
-
52
-
-
84921727040
-
Getting across the cell membrane: An overview for small molecules, peptides, and proteins
-
Yang, N. J.; Hinner, M. J. Getting across the cell membrane: an overview for small molecules, peptides, and proteins Methods Mol. Biol. 2015, 1266, 29-53 10.1007/978-1-4939-2272-7-3
-
(2015)
Methods Mol. Biol.
, vol.1266
, pp. 29-53
-
-
Yang, N.J.1
Hinner, M.J.2
-
53
-
-
0032714220
-
Polar molecular surface as a dominating determinant for oral absorption and brain penetration of drugs
-
Kelder, J.; Grootenhuis, P. D.; Bayada, D. M.; Delbressine, L. P.; Ploemen, J. P. Polar molecular surface as a dominating determinant for oral absorption and brain penetration of drugs Pharm. Res. 1999, 16, 1514-1519 10.1023/A:1015040217741
-
(1999)
Pharm. Res.
, vol.16
, pp. 1514-1519
-
-
Kelder, J.1
Grootenhuis, P.D.2
Bayada, D.M.3
Delbressine, L.P.4
Ploemen, J.P.5
-
54
-
-
79954471349
-
GABA-A receptor subtype-selective modulators. II. Alpha5-selective inverse agonists for cognition enhancement
-
Atack, J. R. GABA-A receptor subtype-selective modulators. II. alpha5-selective inverse agonists for cognition enhancement Curr. Top. Med. Chem. 2011, 11, 1203-1214 10.2174/156802611795371314
-
(2011)
Curr. Top. Med. Chem.
, vol.11
, pp. 1203-1214
-
-
Atack, J.R.1
-
55
-
-
84958748153
-
Modular PROTAC design for the degradation of oncogenic BCR-ABL
-
Lai, A. C.; Toure, M.; Hellerschmied, D.; Salami, J.; Jaime-Figueroa, S.; Ko, E.; Hines, J.; Crews, C. M. Modular PROTAC design for the degradation of oncogenic BCR-ABL Angew. Chem., Int. Ed. 2016, 55, 807-810 10.1002/anie.201507634
-
(2016)
Angew. Chem., Int. Ed.
, vol.55
, pp. 807-810
-
-
Lai, A.C.1
Toure, M.2
Hellerschmied, D.3
Salami, J.4
Jaime-Figueroa, S.5
Ko, E.6
Hines, J.7
Crews, C.M.8
-
56
-
-
85010950530
-
Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cells
-
Saenz, D. T.; Fiskus, W.; Qian, Y.; Manshouri, T.; Rajapakshe, K.; Raina, K.; Coleman, K. G.; Crew, A. P.; Shen, A.; Mill, C. P.; Sun, B.; Qiu, P.; Kadia, T. M.; Pemmaraju, N.; DiNardo, C.; Kim, M. S.; Nowak, A. J.; Coarfa, C.; Crews, C. M.; Verstovsek, S.; Bhalla, K. N. Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cells Leukemia 2017, 31, 1951-1961 10.1038/leu.2016.393
-
(2017)
Leukemia
, vol.31
, pp. 1951-1961
-
-
Saenz, D.T.1
Fiskus, W.2
Qian, Y.3
Manshouri, T.4
Rajapakshe, K.5
Raina, K.6
Coleman, K.G.7
Crew, A.P.8
Shen, A.9
Mill, C.P.10
Sun, B.11
Qiu, P.12
Kadia, T.M.13
Pemmaraju, N.14
DiNardo, C.15
Kim, M.S.16
Nowak, A.J.17
Coarfa, C.18
Crews, C.M.19
Verstovsek, S.20
Bhalla, K.N.21
more..
-
57
-
-
84976614642
-
PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer
-
Raina, K.; Lu, J.; Qian, Y.; Altieri, M.; Gordon, D.; Rossi, A. M.; Wang, J.; Chen, X.; Dong, H.; Siu, K.; Winkler, J. D.; Crew, A. P.; Crews, C. M.; Coleman, K. G. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer Proc. Natl. Acad. Sci. U. S. A. 2016, 113, 7124-7129 10.1073/pnas.1521738113
-
(2016)
Proc. Natl. Acad. Sci. U. S. A.
, vol.113
, pp. 7124-7129
-
-
Raina, K.1
Lu, J.2
Qian, Y.3
Altieri, M.4
Gordon, D.5
Rossi, A.M.6
Wang, J.7
Chen, X.8
Dong, H.9
Siu, K.10
Winkler, J.D.11
Crew, A.P.12
Crews, C.M.13
Coleman, K.G.14
-
58
-
-
85015296681
-
In vivo knockdown of pathogenic proteins via specific and nongenetic inhibitor of apoptosis protein (IAP)-dependent protein erasers (SNIPERs)
-
Ohoka, N.; Okuhira, K.; Ito, M.; Nagai, K.; Shibata, N.; Hattori, T.; Ujikawa, O.; Shimokawa, K.; Sano, O.; Koyama, R.; Fujita, H.; Teratani, M.; Matsumoto, H.; Imaeda, Y.; Nara, H.; Cho, N.; Naito, M. In vivo knockdown of pathogenic proteins via specific and nongenetic inhibitor of apoptosis protein (IAP)-dependent protein erasers (SNIPERs) J. Biol. Chem. 2017, 292, 4556-4570 10.1074/jbc.M116.768853
-
(2017)
J. Biol. Chem.
, vol.292
, pp. 4556-4570
-
-
Ohoka, N.1
Okuhira, K.2
Ito, M.3
Nagai, K.4
Shibata, N.5
Hattori, T.6
Ujikawa, O.7
Shimokawa, K.8
Sano, O.9
Koyama, R.10
Fujita, H.11
Teratani, M.12
Matsumoto, H.13
Imaeda, Y.14
Nara, H.15
Cho, N.16
Naito, M.17
-
59
-
-
85018850840
-
Degradation of the BAF complex factor BRD9 by heterobifunctional ligands
-
Remillard, D.; Buckley, D. L.; Paulk, J.; Brien, G. L.; Sonnett, M.; Seo, H. S.; Dastjerdi, S.; Wuhr, M.; Dhe-Paganon, S.; Armstrong, S. A.; Bradner, J. E. Degradation of the BAF complex factor BRD9 by heterobifunctional ligands Angew. Chem., Int. Ed. 2017, 56, 5738-5743 10.1002/anie.201611281
-
(2017)
Angew. Chem., Int. Ed.
, vol.56
, pp. 5738-5743
-
-
Remillard, D.1
Buckley, D.L.2
Paulk, J.3
Brien, G.L.4
Sonnett, M.5
Seo, H.S.6
Dastjerdi, S.7
Wuhr, M.8
Dhe-Paganon, S.9
Armstrong, S.A.10
Bradner, J.E.11
-
60
-
-
85041109499
-
-
WO2016118666A1
-
Jin, M.; Crew, A. P.; Dong, H.; Wang, J.; Siu, K.; Ferraro, C.; Chen, X.; Qian, Y. Preparation of Thioxoimidazolidinone Compounds and Methods for the Targeted Degradation of the Androgen Receptor. WO2016118666A1, 2016.
-
(2016)
Preparation of Thioxoimidazolidinone Compounds and Methods for the Targeted Degradation of the Androgen Receptor
-
-
Jin, M.1
Crew, A.P.2
Dong, H.3
Wang, J.4
Siu, K.5
Ferraro, C.6
Chen, X.7
Qian, Y.8
-
61
-
-
41549105366
-
Factors affecting therapeutic compliance: A review from the patient's perspective
-
Jin, J.; Sklar, G. E.; Oh, V. M. S.; Li, S. C. Factors affecting therapeutic compliance: A review from the patient's perspective Ther. Clin. Risk Manage. 2008, 4, 269-286 10.2147/TCRM.S1458
-
(2008)
Ther. Clin. Risk Manage.
, vol.4
, pp. 269-286
-
-
Jin, J.1
Sklar, G.E.2
Oh, V.M.S.3
Li, S.C.4
-
62
-
-
85041138832
-
-
US20170095446A1
-
Narayanan, R.; Miller, D. D.; Ponnusamy, T.; Hwang, D.-J.; Pagadala, J.; Duke, C. B.; Coss, C. C.; Dalton, J. T.; He, Y. Preparation of Novel Indole, Indazole, Benzimidazole, Indoline, Quinolone, Isoquinoline, and Carbazole Selective Androgen Receptor Degrader (SARD) Ligands. US20170095446A1, 2017.
-
(2017)
Preparation of Novel Indole, Indazole, Benzimidazole, Indoline, Quinolone, Isoquinoline, and Carbazole Selective Androgen Receptor Degrader (SARD) Ligands
-
-
Narayanan, R.1
Miller, D.D.2
Ponnusamy, T.3
Hwang, D.-J.4
Pagadala, J.5
Duke, C.B.6
Coss, C.C.7
Dalton, J.T.8
He, Y.9
-
63
-
-
84933073465
-
Oral selective estrogen receptor downregulators (SERDs), a breakthrough endocrine therapy for breast cancer
-
McDonnell, D. P.; Wardell, S. E.; Norris, J. D. Oral selective estrogen receptor downregulators (SERDs), a breakthrough endocrine therapy for breast cancer J. Med. Chem. 2015, 58, 4883-4887 10.1021/acs.jmedchem.5b00760
-
(2015)
J. Med. Chem.
, vol.58
, pp. 4883-4887
-
-
McDonnell, D.P.1
Wardell, S.E.2
Norris, J.D.3
-
64
-
-
85019546678
-
The logic of the 26S proteasome
-
Collins, G. A.; Goldberg, A. L. The logic of the 26S proteasome Cell 2017, 169, 792-806 10.1016/j.cell.2017.04.023
-
(2017)
Cell
, vol.169
, pp. 792-806
-
-
Collins, G.A.1
Goldberg, A.L.2
-
65
-
-
84989184483
-
Development of BCR-ABL degradation inducers via the conjugation of an imatinib derivative and a cIAP1 ligand
-
Demizu, Y.; Shibata, N.; Hattori, T.; Ohoka, N.; Motoi, H.; Misawa, T.; Shoda, T.; Naito, M.; Kurihara, M. Development of BCR-ABL degradation inducers via the conjugation of an imatinib derivative and a cIAP1 ligand Bioorg. Med. Chem. Lett. 2016, 26, 4865-4869 10.1016/j.bmcl.2016.09.041
-
(2016)
Bioorg. Med. Chem. Lett.
, vol.26
, pp. 4865-4869
-
-
Demizu, Y.1
Shibata, N.2
Hattori, T.3
Ohoka, N.4
Motoi, H.5
Misawa, T.6
Shoda, T.7
Naito, M.8
Kurihara, M.9
-
66
-
-
44949231368
-
Genome-wide and functional annotation of human E3 ubiquitin ligases identifies MULAN, a mitochondrial E3 that regulates the organelle's dynamics and signaling
-
Li, W.; Bengtson, M. H.; Ulbrich, A.; Matsuda, A.; Reddy, V. A.; Orth, A.; Chanda, S. K.; Batalov, S.; Joazeiro, C. A. P. Genome-wide and functional annotation of human E3 ubiquitin ligases identifies MULAN, a mitochondrial E3 that regulates the organelle's dynamics and signaling PLoS One 2008, 3, e1487 10.1371/journal.pone.0001487
-
(2008)
PLoS One
, vol.3
, pp. e1487
-
-
Li, W.1
Bengtson, M.H.2
Ulbrich, A.3
Matsuda, A.4
Reddy, V.A.5
Orth, A.6
Chanda, S.K.7
Batalov, S.8
Joazeiro, C.A.P.9
-
67
-
-
2442696694
-
Localization to the proteasome is sufficient for degradation
-
Janse, D. M.; Crosas, B.; Finley, D.; Church, G. M. Localization to the proteasome is sufficient for degradation J. Biol. Chem. 2004, 279, 21415-21420 10.1074/jbc.M402954200
-
(2004)
J. Biol. Chem.
, vol.279
, pp. 21415-21420
-
-
Janse, D.M.1
Crosas, B.2
Finley, D.3
Church, G.M.4
-
68
-
-
85016141998
-
Protein degradation by in-cell self-assembly of proteolysis targeting chimeras
-
Lebraud, H.; Wright, D. J.; Johnson, C. N.; Heightman, T. D. Protein degradation by in-cell self-assembly of proteolysis targeting chimeras ACS Cent. Sci. 2016, 2, 927-934 10.1021/acscentsci.6b00280
-
(2016)
ACS Cent. Sci.
, vol.2
, pp. 927-934
-
-
Lebraud, H.1
Wright, D.J.2
Johnson, C.N.3
Heightman, T.D.4
-
69
-
-
85002564019
-
Pharmaceutical amorphous nanoparticles
-
Jog, R.; Burgess, D. J. Pharmaceutical amorphous nanoparticles J. Pharm. Sci. 2017, 106, 39-65 10.1016/j.xphs.2016.09.014
-
(2017)
J. Pharm. Sci.
, vol.106
, pp. 39-65
-
-
Jog, R.1
Burgess, D.J.2
|