Access the full text.
Sign up today, get DeepDyve free for 14 days.
Loading next page...
/lp/annual-reviews/targeted-protein-degradation-by-small-molecules-7ZTb2o92FA
References (112)
-
V. Landré, B. Rotblat, S. Melino, F. Bernassola, G. Melino (2014)
Screening for E3-Ubiquitin ligase inhibitors: challenges and opportunitiesOncotarget, 5
-
E. Nicodème, K. Jeffrey, Uwe Schaefer, S. Beinke, Scott Dewell, C. Chung, R. Chandwani, Ivan Marazzi, Paul Wilson, H. Coste, Julia White, J. Kirilovsky, C. Rice, J. Lora, R. Prinjha, Kevin Lee, A. Tarakhovsky (2010)
Suppression of inflammation by a synthetic histone mimicNature, 468
-
Daniel Bondeson, A. Mareş, I. Smith, Eunhwa Ko, Sebastien Campos, Afjal Miah, K. Mulholland, Natasha Routly, Dennis Buckley, J. Gustafson, N. Zinn, P. Grandi, S. Shimamura, G. Bergamini, Maria Faelth-Savitski, M. Bantscheff, Carly Cox, D. Gordon, Ryan Willard, J. Flanagan, Linda Casillas, B. Votta, W. Besten, K. Famm, L. Kruidenier, P. Carter, J. Harling, I. Churcher, C. Crews (2015)
Catalytic in vivo protein knockdown by small-molecule PROTACs.Nature chemical biology, 11 8
-
Yu Lin, M. Pratt (2014)
A Dual Small‐Molecule Rheostat for Precise Control of Protein Concentration in Mammalian CellsChemBioChem, 15
-
Liangyu Zhang, Jordan Ward, Ze Cheng, A. Dernburg (2015)
The auxin-inducible degradation (AID) system enables versatile conditional protein depletion in C. elegansDevelopment (Cambridge, England), 142
-
E. Fischer, A. Scrima, K. Böhm, Syota Matsumoto, G. Lingaraju, M. Faty, Takeshi Yasuda, S. Cavadini, M. Wakasugi, F. Hanaoka, S. Iwai, H. Gut, K. Sugasawa, N. Thomä (2011)
The Molecular Basis of CRL4DDB2/CSA Ubiquitin Ligase Architecture, Targeting, and ActivationCell, 147
-
P. Hagner, H. Man, C. Fontanillo, Maria Wang, S. Couto, M. Breider, C. Bjorklund, C. Havens, Gang Lu, E. Rychak, H. Raymon, R. Narla, Leo Barnes, Gody Khambatta, Hsiling Chiu, J. Kosek, Jian Kang, Michael Amantangelo, M. Waldman, A. López-Girona, T. Cai, M. Pourdehnad, M. Trotter, T. Daniel, P. Schafer, A. Klippel, A. Thakurta, R. Chopra, A. Gandhi (2015)
CC-122, a pleiotropic pathway modifier, mimics an interferon response and has antitumor activity in DLBCL.Blood, 126 6
-
Ting Xie, S. Lim, K. Westover, Michael Dodge, D. Ercan, S. Ficarro, Durga Udayakumar, D. Gurbani, H. Tae, Steven Riddle, Taebo Sim, J. Marto, P. Jänne, C. Crews, N. Gray (2014)
Pharmacological Targeting of the Pseudokinase Her3Nature chemical biology, 10
-
A. Russ, S. Lampel (2005)
The druggable genome: an update.Drug discovery today, 10 23-24
-
K. Sekine, K. Takubo, R. Kikuchi, M. Nishimoto, M. Kitagawa, F. Abe, K. Nishikawa, T. Tsuruo, M. Naito (2008)
Small Molecules Destabilize cIAP1 by Activating Auto-ubiquitylation*Journal of Biological Chemistry, 283
-
M. Dimopoulos, A. Spencer, M. Attal, H. Prince, J. Harousseau, A. Dmoszyńska, J. Miguel, A. Hellmann, T. Facon, R. Foà, A. Corso, Z. Masliak, M. Olesnyckyj, Zhinuan Yu, J. Patin, J. Zeldis, R. Knight (2007)
Lenalidomide plus dexamethasone for relapsed or refractory multiple myeloma.The New England journal of medicine, 357 21
-
R. Deshaies, C. Joazeiro (2009)
RING domain E3 ubiquitin ligases.Annual review of biochemistry, 78
-
F. Niesen, H. Berglund, M. Vedadi (2007)
The use of differential scanning fluorimetry to detect ligand interactions that promote protein stabilityNature Protocols, 2
-
D. Fachinetti, Joo Han, Moira McMahon, P. Ly, A. Abdullah, A. Wong, D. Cleveland (2015)
DNA Sequence-Specific Binding of CENP-B Enhances the Fidelity of Human Centromere Function.Developmental cell, 33 3
-
Congcong He, D. Klionsky (2009)
Regulation mechanisms and signaling pathways of autophagy.Annual review of genetics, 43
-
R. Coffey, Yuntao Shi, M. Long, M. Marr, L. Hedstrom (2016)
Ubiquilin-mediated Small Molecule Inhibition of Mammalian Target of Rapamycin Complex 1 (mTORC1) Signaling*The Journal of Biological Chemistry, 291
-
Karen Kieser, D. Kim, K. Carlson, B. Katzenellenbogen, J. Katzenellenbogen (2010)
Characterization of the pharmacophore properties of novel selective estrogen receptor downregulators (SERDs).Journal of medicinal chemistry, 53 8
-
Ya-Ling Wu, Xiaojing Yang, Zhong Ren, D. McDonnell, J. Norris, T. Willson, G. Greene (2005)
Structural basis for an unexpected mode of SERM-mediated ER antagonism.Molecular cell, 18 4
-
R. Patch, L. Searle, Alexander Kim, D. De, Xizhen Zhu, H. Askari, J. O'Neill, M. Abad, D. Rentzeperis, Jianying Liu, M. Kemmerer, Ling Lin, Jyotsna Kasturi, J. Geisler, J. Lenhard, M. Player, M. Gaul (2011)
Identification of diaryl ether-based ligands for estrogen-related receptor α as potential antidiabetic agents.Journal of medicinal chemistry, 54 3
-
Keiichiro Okuhira, Yosuke Demizu, T. Hattori, Nobumichi Ohoka, N. Shibata, M. Kurihara, M. Naito (2016)
Molecular Design, Synthesis, and Evaluation of SNIPER(ER) That Induces Proteasomal Degradation of ERα.Methods in molecular biology, 1366
-
K. Nishimura, T. Fukagawa, H. Takisawa, T. Kakimoto, Masato Kanemaki (2009)
An auxin-based degron system for the rapid depletion of proteins in nonplant cellsNature Methods, 6
-
Ashton Lai, M. Toure, D. Hellerschmied, J. Salami, S. Jaime-Figueroa, Eunhwa Ko, J. Hines, C. Crews (2016)
Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL.Angewandte Chemie, 55 2
-
Citation Delmore, J. E., G. Issa, M. Lemieux, P. Rahl, Junwei Shi, H. Jacobs, Jake Delmore, E. Kastritis, Timothy Gilpatrick, Ronald Paranal, J. Qi, M. Chesi, Anna Schinzel, M. Mckeown, T. Heffernan, C. Vakoc, P. Bergsagel, I. Ghobrial, P. Richardson, R. Young, W. Hahn, K. Anderson, A. Kung, J. Bradner, C. Mitsiades (2011)
BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-MycCell, 146
-
Susmita Kaushik, A. Cuervo (2012)
Chaperone-mediated autophagy: a unique way to enter the lysosome world.Trends in cell biology, 22 8
-
E. Auffenberg, A. Jurik, Corinna Mattusch, R. Stoffel, A. Genewsky, Christian Namendorf, R. Schmid, G. Rammes, M. Biel, M. Uhr, S. Moosmang, S. Michalakis, C. Wotjak, C. Thoeringer (2016)
Remote and reversible inhibition of neurons and circuits by small molecule induced potassium channel stabilizationScientific Reports, 6
-
Shusuke Tomoshige, M. Naito, Y. Hashimoto, M. Ishikawa (2015)
Degradation of HaloTag-fused nuclear proteins using bestatin-HaloTag ligand hybrid molecules.Organic & biomolecular chemistry, 13 38
-
M. Aghajan, Nao Jonai, K. Flick, Fei Fu, Manlin Luo, Xiaolu Cai, I. Ouni, N. Pierce, Xiaobo Tang, B. Lomenick, R. Damoiseaux, R. Hao, Pierre Moral, R. Verma, Ying Li, Cheng Li, K. Houk, M. Jung, N. Zheng, Lan Huang, R. Deshaies, P. Kaiser, Jing Huang (2010)
Chemical genetics screen for enhancers of rapamycin identifies a specific inhibitor of an SCF family E3 ubiquitin ligase.Nature biotechnology, 28 7
-
J. Huss, I. Torra, B. Staels, V. Giguère, D. Kelly (2004)
Estrogen-Related Receptor α Directs Peroxisome Proliferator-Activated Receptor α Signaling in the Transcriptional Control of Energy Metabolism in Cardiac and Skeletal MuscleMolecular and Cellular Biology, 24
-
J. Conde, N. Artzi (2015)
Are RNAi and miRNA therapeutics truly dead?Trends in biotechnology, 33 3
-
A. Wakeling, M. Dukes, J. Bowler (1991)
A potent specific pure antiestrogen with clinical potential.Cancer research, 51 15
-
Zibo Zhao, Lu Wang, Youngeun Jung, Ikyon Kim, R. Tan, Wei Xu (2015)
Reciprocal Regulation of ERα and ERβ Stability and Activity by Diptoindonesin G.Chemistry & biology, 22 12
-
Jeffrey Gustafson, T. Neklesa, Carly Cox, Anke Roth, Dennis Buckley, Hyun Tae, Thomas Sundberg, D. Stagg, J. Hines, D. McDonnell, J. Norris, C. Crews (2015)
Small-Molecule-Mediated Degradation of the Androgen Receptor through Hydrophobic Tagging.Angewandte Chemie, 54 33
-
J. Hines, J. Gough, T. Corson, C. Crews (2013)
Posttranslational protein knockdown coupled to receptor tyrosine kinase activation with phosphoPROTACsProceedings of the National Academy of Sciences, 110
-
Yibin Yang, A. Shaffer, N. Emre, M. Ceribelli, Meili Zhang, George Wright, Wenming Xiao, J. Powell, John Platig, H. Kohlhammer, R. Young, Hong Zhao, Yandan Yang, Weihong Xu, J. Buggy, S. Balasubramanian, Lesley Mathews, P. Shinn, R. Guha, M. Ferrer, Craig Thomas, T. Waldmann, L. Staudt (2012)
Exploiting synthetic lethality for the therapy of ABC diffuse large B cell lymphoma.Cancer cell, 21 6
-
S. Govek, Johnny Nagasawa, Karensa Douglas, Andiliy Lai, M. Kahraman, C. Bonnefous, Anna Aparicio, B. Darimont, Kate Grillot, James Joseph, Josh Kaufman, Kyoung-jin Lee, Nhin Lu, Michael Moon, R. Prudente, J. Sensintaffar, P. Rix, J. Hager, N. Smith (2015)
Optimization of an indazole series of selective estrogen receptor degraders: Tumor regression in a tamoxifen-resistant breast cancer xenograft.Bioorganic & medicinal chemistry letters, 25 22
-
J. Schneekloth, F. Fonseca, Michael Koldobskiy, A. Mandal, R. Deshaies, K. Sakamoto, C. Crews (2004)
Chemical genetic control of protein levels: selective in vivo targeted degradation.Journal of the American Chemical Society, 126 12
-
Michael Zengerle, Kwok-Ho Chan, A. Ciulli (2015)
Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4ACS Chemical Biology, 10
-
H. Lau, Junko Yaegashi, Balyn Zaro, M. Pratt (2010)
Precise control of protein concentration in living cells.Angewandte Chemie, 49 45
-
H. Tae, Thomas Sundberg, T. Neklesa, Devin Noblin, J. Gustafson, A. Roth, Kanak Raina, C. Crews (2012)
Identification of Hydrophobic Tags for the Degradation of Stabilized ProteinsChemBioChem, 13
-
J. Dvorin, D. Martyn, Saurabh Patel, J. Grimley, C. Collins, Christine Hopp, A. Bright, S. Westenberger, E. Winzeler, M. Blackman, D. Baker, T. Wandless, M. Duraisingh (2010)
A Plant-Like Kinase in Plasmodium falciparum Regulates Parasite Egress from ErythrocytesScience, 328
-
S. Dauvois, P. Danielian, Roger White, Malcolm Parker (1992)
Antiestrogen ICI 164,384 reduces cellular estrogen receptor content by increasing its turnover.Proceedings of the National Academy of Sciences of the United States of America, 89
-
S. Degorce, Andrew Bailey, R. Callis, C. savi, R. Ducray, G. Lamont, P. Macfaul, M. Maudet, Scott Martin, R. Morgentin, R. Norman, A. Peru, J. Pink, P. Plé, Bryan Roberts, James Scott (2015)
Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators.Journal of medicinal chemistry, 58 8
-
J. Krönke, J. Krönke, E. Fink, E. Fink, P. Hollenbach, K. Macbeth, Slater Hurst, N. Udeshi, P. Chamberlain, D. Mani, Man Wah, A. Gandhi, Tanya Svinkina, R. Schneider, M. McConkey, M. Järås, E. Griffiths, M. Wetzler, L. Bullinger, B. Cathers, S. Carr, R. Chopra, B. Ebert, B. Ebert (2015)
Lenalidomide induces ubiquitination and degradation of CK1α in del(5q) MDSNature, 523
-
A. Gandhi, Jian Kang, C. Havens, Thomas Conklin, Y. Ning, Lei Wu, Takumi Ito, H. Ando, M. Waldman, A. Thakurta, A. Klippel, H. Handa, T. Daniel, P. Schafer, R. Chopra (2013)
Immunomodulatory agents lenalidomide and pomalidomide co-stimulate T cells by inducing degradation of T cell repressors Ikaros and Aiolos via modulation of the E3 ubiquitin ligase complex CRL4CRBNBritish Journal of Haematology, 164
-
S. Loddick, S. Ross, A. Thomason, David Robinson, G. Walker, T. Dunkley, S. Brave, Nicola Broadbent, Natalie Stratton, D. Trueman, E. Mouchet, Fadhel Shaheen, V. Jacobs, M. Cumberbatch, Joanne Wilson, Rhys Jones, R. Bradbury, A. Rabow, L. Gaughan, C. Womack, S. Barry, C. Robson, S. Critchlow, S. Wedge, A. Brooks (2013)
AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function In Vitro and In VivoMolecular Cancer Therapeutics, 12
-
Yukihiro Itoh, Risa Kitaguchi, M. Ishikawa, M. Naito, Y. Hashimoto (2011)
Design, synthesis and biological evaluation of nuclear receptor-degradation inducers.Bioorganic & medicinal chemistry, 19 22
-
Jung-Hyun Min, Haifeng Yang, M. Ivan, F. Gertler, W. Kaelin, N. Pavletich (2002)
Structure of an HIF-1α-pVHL Complex: Hydroxyproline Recognition in SignalingScience, 296
-
F. Garner, Maysoun Shomali, D. Paquin, Richard Lyttle, G. Hattersley (2015)
RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft modelsAnti-Cancer Drugs, 26
-
Xuelai Fan, W. Jin, Jie Lu, Jin Wang, Y. Wang (2014)
Rapid and reversible knockdown of endogenous proteins by peptide-directed lysosomal degradationNature neuroscience, 17
-
C. savi, R. Bradbury, A. Rabow, R. Norman, Camila Almeida, D. Andrews, P. Ballard, D. Buttar, R. Callis, G. Currie, J. Curwen, Chris Davies, Craig Donald, Lyman Feron, H. Gingell, S. Glossop, B. Hayter, S. Hussain, Galith Karoutchi, Scott Lamont, P. Macfaul, T. Moss, S. Pearson, Michael Tonge, G. Walker, H. Weir, Zena Wilson (2015)
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist.Journal of medicinal chemistry, 58 20
-
Dennis Buckley, Kanak Raina, N. Darricarrère, J. Hines, J. Gustafson, I. Smith, Afjal Miah, J. Harling, C. Crews (2015)
HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins.ACS chemical biology, 10 8
-
K. Sakamoto, K. Kim, A. Kumagai, F. Mercurio, C. Crews, R. Deshaies (2001)
Protacs: Chimeric molecules that target proteins to the Skp1–Cullin–F box complex for ubiquitination and degradationProceedings of the National Academy of Sciences of the United States of America, 98
-
H. Chung, Conor Jacobs, Yunwen Huo, Jin Yang, S. Krumm, Richard Plemper, R. Tsien, Michael Lin (2015)
Tunable and reversible drug control of protein production via a self-excising degronNature chemical biology, 11
-
Ukrae Cho, Stephanie Zimmerman, Ling-chun Chen, Elliot Owen, Jesse Kim, Stuart Kim, T. Wandless (2013)
Rapid and Tunable Control of Protein Stability in Caenorhabditis elegans Using a Small MoleculePLoS ONE, 8
-
M. Clague, Claire Heride, S. Urbé (2015)
The demographics of the ubiquitin system.Trends in cell biology, 25 7
-
Dennis Buckley, I. Molle, Peter Gareiss, H. Tae, J. Michel, Devin Noblin, W. Jorgensen, A. Ciulli, C. Crews (2012)
Targeting the von Hippel–Lindau E3 Ubiquitin Ligase Using Small Molecules To Disrupt the VHL/HIF-1α InteractionJournal of the American Chemical Society, 134
-
Selvakumar Elangovan, S. Ramachandran, N. Venkatesan, S. Ananth, Jaya Gnana-Prakasam, Pamela Martin, D. Browning, P. Schoenlein, P. Prasad, V. Ganapathy, M. Thangaraju (2011)
SIRT1 is essential for oncogenic signaling by estrogen/estrogen receptor α in breast cancer.Cancer research, 71 21
-
T. Neklesa, H. Tae, A. Schneekloth, M. Stulberg, T. Corson, Thomas Sundberg, Kanak Raina, S. Holley, C. Crews (2011)
Small-Molecule Hydrophobic Tagging Induced Degradation of HaloTag Fusion ProteinsNature chemical biology, 7
-
W. Gray, S. Kepinski, D. Rouse, O. Leyser, M. Estelle (2001)
Auxin regulates SCFTIR1-dependent degradation of AUX/IAA proteinsNature, 414
-
Kanak Raina, Devin Noblin, Yevgeniy Serebrenik, Alison Adams, Connie Zhao, C. Crews (2014)
Targeted Protein Destabilization Reveals an Estrogen-mediated ER Stress ResponseNature chemical biology, 10
-
L. Milroy, T. Grossmann, S. Hennig, L. Brunsveld, C. Ottmann (2014)
Modulators of protein-protein interactions.Chemical reviews, 114 9
-
Keiichiro Okuhira, Nobumichi Ohoka, K. Sai, T. Nishimaki‐Mogami, Yukihiro Itoh, M. Ishikawa, Y. Hashimoto, M. Naito (2011)
Specific degradation of CRABP‐II via cIAP1‐mediated ubiquitylation induced by hybrid molecules that crosslink cIAP1 and the target proteinFEBS Letters, 585
-
R. Copeland (2015)
The drug–target residence time model: a 10-year retrospectiveNature Reviews Drug Discovery, 15
-
Dong Zhang, S. Baek, A. Ho, K. Kim (2004)
Degradation of target protein in living cells by small-molecule proteolysis inducer.Bioorganic & medicinal chemistry letters, 14 3
-
Dan Yan, Marco Weisshaar, K. Lamb, H. Chung, Michael Lin, Richard Plemper (2015)
Replication-Competent Influenza Virus and Respiratory Syncytial Virus Luciferase Reporter Strains Engineered for Co-Infections Identify Antiviral Compounds in Combination Screens.Biochemistry, 54 36
-
T. Hirota, Jae Lee, Peter John, Mariko Sawa, K. Iwaisako, Takako Noguchi, Pagkapol Pongsawakul, Tim Sonntag, D. Welsh, D. Brenner, F. Doyle, P. Schultz, S. Kay (2012)
Identification of Small Molecule Activators of CryptochromeScience, 337
-
S. Lim, Ting Xie, K. Westover, S. Ficarro, H. Tae, D. Gurbani, Taebo Sim, J. Marto, P. Jänne, C. Crews, N. Gray (2015)
Development of small molecules targeting the pseudokinase Her3.Bioorganic & medicinal chemistry letters, 25 16
-
A. Ciechanover (2015)
The unravelling of the ubiquitin systemNature Reviews Molecular Cell Biology, 16
-
J. Bartlett, K. Dredge, A. Dalgleish (2004)
The evolution of thalidomide and its IMiD derivatives as anticancer agentsNature Reviews Cancer, 4
-
G. Petzold, E. Fischer, N. Thomä (2016)
Structural basis of lenalidomide-induced CK1α degradation by the CRL4CRBN ubiquitin ligaseNature, 532
-
M. Morawska, H. Ulrich (2013)
An expanded tool kit for the auxin-inducible degron system in budding yeastYeast (Chichester, England), 30
-
Kara McKinley, N. Sekulić, Lucie Guo, T. Tsinman, B. Black, I. Cheeseman (2015)
The CENP-L-N Complex Forms a Critical Node in an Integrated Meshwork of Interactions at the Centromere-Kinetochore Interface.Molecular cell, 60 6
-
Haojian Zhang, C. Peng, Yiguo Hu, Huawei Li, Z. Sheng, Yaoyu Chen, C. Sullivan, J. Černý, L. Hutchinson, A. Higgins, P. Miron, Xueqing Zhang, M. Brehm, Dongguang Li, Michael Green, Shaoguang Li (2012)
The Blk pathway functions as a tumor suppressor in chronic myeloid leukemia stem cellsNature genetics, 44
-
S. Orlicky, Xiaojing Tang, Victor Neduva, Nadine Elowe, E. Brown, F. Sicheri, M. Tyers (2010)
An allosteric inhibitor of substrate recognition by the SCFCdc4 ubiquitin ligaseNature Biotechnology, 28
-
James Scott, Andrew Bailey, Robert Davies, S. Degorce, P. Macfaul, H. Gingell, T. Moss, R. Norman, J. Pink, A. Rabow, Bryan Roberts, Peter Smith (2016)
Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat.ACS medicinal chemistry letters, 7 1
-
R. Callis, A. Rabow, Michael Tonge, R. Bradbury, Mairi Challinor, K. Roberts, K. Jones, G. Walker (2015)
A Screening Assay Cascade to Identify and Characterize Novel Selective Estrogen Receptor Downregulators (SERDs)Journal of Biomolecular Screening, 20
-
A. Holland, D. Fachinetti, Joo Han, D. Cleveland (2012)
Inducible, reversible system for the rapid and complete degradation of proteins in mammalian cellsProceedings of the National Academy of Sciences, 109
-
C. Huggins, C. Hodges (2002)
Studies on prostatic cancer. I. The effect of castration, of estrogen and of androgen injection on serum phosphatases in metastatic carcinoma of the prostate. 1941.The Journal of urology, 167 2 Pt 2
-
G. Lu, R. Middleton, Huahang Sun, MarkVic Naniong, Christopher Ott, C. Mitsiades, Kwok-kin Wong, J. Bradner, W. Kaelin (2014)
The Myeloma Drug Lenalidomide Promotes the Cereblon-Dependent Destruction of Ikaros ProteinsScience, 343
-
R. Bradbury, N. Hales, A. Rabow, G. Walker, D. Acton, D. Andrews, P. Ballard, N. Brooks, N. Colclough, Alan Girdwood, Urs Hancox, O. Jones, David Jude, S. Loddick, A. Mortlock (2011)
Small-molecule androgen receptor downregulators as an approach to treatment of advanced prostate cancer.Bioorganic & medicinal chemistry letters, 21 18
-
C. Galdeano, M. Gadd, P. Soares, S. Scaffidi, I. Molle, Ipek Birced, S. Hewitt, David Dias, A. Ciulli (2014)
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 AffinitiesJournal of Medicinal Chemistry, 57
-
Georg Winter, Dennis Buckley, Joshiawa Paulk, Justin Roberts, Amanda Souza, S. Dhe-Paganon, J. Bradner (2015)
Phthalimide conjugation as a strategy for in vivo target protein degradationScience, 348
-
Jing Lu, Y. Qian, M. Altieri, Hanqing Dong, Jing Wang, Kanak Raina, J. Hines, J. Winkler, A. Crew, K. Coleman, C. Crews (2015)
Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4.Chemistry & biology, 22 6
-
I. Molle, A. Thomann, Dennis Buckley, E. So, S. Lang, C. Crews, A. Ciulli (2012)
Dissecting fragment-based lead discovery at the von Hippel-Lindau protein:hypoxia inducible factor 1α protein-protein interface.Chemistry & biology, 19 10
-
Peter Cimermancic, Patrick Weinkam, T. Rettenmaier, T. Rettenmaier, L. Bichmann, D. Keedy, R. Woldeyes, D. Schneidman-Duhovny, Omar Demerdash, Julie Mitchell, J. Wells, J. Fraser, Andrej Sali, Andrej Sali (2016)
CryptoSite: Expanding the Druggable Proteome by Characterization and Prediction of Cryptic Binding Sites.Journal of molecular biology, 428 4
-
T. Neklesa, Devin Noblin, Alexander Kuzin, S. Lew, J. Seetharaman, T. Acton, G. Kornhaber, R. Xiao, G. Montelione, L. Tong, C. Crews (2013)
A bidirectional system for the dynamic small molecule control of intracellular fusion proteins.ACS chemical biology, 8 10
-
Marcus Long, D. Gollapalli, L. Hedstrom (2012)
Inhibitor mediated protein degradation.Chemistry & biology, 19 5
-
Takumi Ito, H. Ando, Takayuki Suzuki, T. Ogura, K. Hotta, Y. Imamura, Y. Yamaguchi, H. Handa (2010)
Identification of a Primary Target of Thalidomide TeratogenicityScience, 327
-
J. Miguel, K. Weisel, P. Moreau, M. Lacy, K. Song, M. Delforge, L. Karlin, H. Goldschmidt, A. Banos, A. Oriol, A. Alegre, Christine Chen, M. Cavo, L. Garderet, V. Ivanova, J. Martínez-López, A. Belch, A. Palumbo, S. Schey, P. Sonneveld, Xin Yu, L. Sternås, C. Jacques, M. Zaki, M. Dimopoulos (2013)
Pomalidomide plus low-dose dexamethasone versus high-dose dexamethasone alone for patients with relapsed and refractory multiple myeloma (MM-003): a randomised, open-label, phase 3 trial.The Lancet. Oncology, 14 11
-
Jing Liang, Y. Shang (2013)
Estrogen and cancer.Annual review of physiology, 75
-
R. Schneider, V. Adema, D. Heckl, M. Järås, M. Mallo, Allegra Lord, L. Chu, M. McConkey, R. Kramann, A. Mullally, R. Bejar, F. Solé, B. Ebert (2014)
Role of casein kinase 1A1 in the biology and targeted therapy of del(5q) MDS.Cancer cell, 26 4
-
A. Shaffer, N. Emre, L. Lamy, V. Ngo, George Wright, Wenming Xiao, J. Powell, S. Dave, Xin Yu, Hong Zhao, Yuxin Zeng, Bangzheng Chen, J. Epstein, L. Staudt (2008)
IRF4 addiction in multiple myelomaNature, 454
-
A. Froschauer, L. Kube, A. Kegler, C. Rieger, H. Gutzeit (2015)
Tunable Protein Stabilization In Vivo Mediated by Shield-1 in Transgenic MedakaPLoS ONE, 10
-
Francesca Mattiroli, T. Sixma (2014)
Lysine-targeting specificity in ubiquitin and ubiquitin-like modification pathwaysNature Structural &Molecular Biology, 21
-
E. Fischer, K. Böhm, J. Lydeard, Haidi Yang, Michael Stadler, S. Cavadini, J. Nagel, F. Serluca, Vincent Acker, G. Lingaraju, R. Tichkule, M. Schebesta, W. Forrester, M. Schirle, U. Hassiepen, J. Ottl, M. Hild, Rohan Beckwith, J. Harper, J. Jenkins, N. Thomä (2014)
Structure of the DDB1-CRBN E3 ubiquitin ligase in complex with thalidomideNature, 512
-
Derek Abbott, A. Wilkins, J. Asara, L. Cantley (2004)
The Crohn's Disease Protein, NOD2, Requires RIP2 in Order to Induce Ubiquitinylation of a Novel Site on NEMOCurrent Biology, 14
-
A. Corbin, A. Agarwal, M. Loriaux, J. Cortes, M. Deininger, B. Druker (2011)
Human chronic myeloid leukemia stem cells are insensitive to imatinib despite inhibition of BCR-ABL activity.The Journal of clinical investigation, 121 1
-
Sungjin Park, Ioanna Ntai, Paul Thomas, Evgeniia Konishcheva, N. Kelleher, Alexander Statsuk (2012)
Mechanism-based small molecule cross-linkers of HECT E3 ubiquitin ligase-substrate pairs.Biochemistry, 51 42
-
N. Philip, A. Waters (2015)
Conditional Degradation of Plasmodium Calcineurin Reveals Functions in Parasite Colonization of both Host and VectorCell Host & Microbe, 18
-
N. Suzuki, Xiaoping Liu, Y. Laxmi, Kanako Okamoto, Hyo Kim, Guangxiang Zhang, John Chen, Yoshinori Okamoto, S. Shibutani (2011)
Anti‐breast cancer potential of SS5020, a novel benzopyran antiestrogenInternational Journal of Cancer, 128
-
Koichi Kobayashi, N. Inohara, L. Hernandez, J. Galán, G. Núñez, C. Janeway, R. Medzhitov, R. Flavell (2002)
RICK/Rip2/CARDIAK mediates signalling for receptors of the innate and adaptive immune systemsNature, 416
-
P. Chamberlain, A. López-Girona, Karen Miller, G. Carmel, B. Pagarigan, B. Chie-Leon, E. Rychak, L. Corral, Y. Ren, Maria Wang, Mariko Riley, S. Delker, Takumi Ito, H. Ando, Tomoyuki Mori, Y. Hirano, H. Handa, T. Hakoshima, T. Daniel, B. Cathers (2014)
Structure of the human Cereblon–DDB1–lenalidomide complex reveals basis for responsiveness to thalidomide analogsNature Structural &Molecular Biology, 21
-
Andiliy Lai, M. Kahraman, S. Govek, Johnny Nagasawa, C. Bonnefous, J. Julien, Karensa Douglas, J. Sensintaffar, Nhin Lu, Kyoung-jin Lee, Anna Aparicio, Josh Kaufman, J. Qian, G. Shao, R. Prudente, Michael Moon, James Joseph, B. Darimont, D. Brigham, Kate Grillot, R. Heyman, P. Rix, J. Hager, N. Smith (2015)
Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts.Journal of medicinal chemistry, 58 12
-
P. Filippakopoulos, J. Qi, S. Picaud, Yao Shen, William Smith, O. Fedorov, Elizabeth Morse, T. Keates, T. Hickman, I. Felletár, M. Philpott, S. Munro, M. Mckeown, Yuchuan Wang, A. Christie, N. West, M. Cameron, Brian Schwartz, T. Heightman, N. Thangue, C. French, O. Wiest, A. Kung, S. Knapp, J. Bradner (2010)
Selective inhibition of BET bromodomainsNature, 468
-
R. Ludlow, M. Verdonk, H. Saini, I. Tickle, H. Jhoti (2015)
Detection of secondary binding sites in proteins using fragment screeningProceedings of the National Academy of Sciences, 112
-
K. Comess, Chaohong Sun, C. Abad-Zapatero, E. Goedken, R. Gum, D. Borhani, M. Argiriadi, D. Groebe, Yong Jia, J. Clampit, D. Haasch, Harriet Smith, Sanyi Wang, D. Song, M. Coen, T. Cloutier, Hua Tang, Xueheng Cheng, C. Quinn, Bo Liu, Zhili Xin, Gang Liu, Elizabeth Fry, V. Stoll, T. Ng, D. Banach, D. Marcotte, D. Burns, D. Calderwood, P. Hajduk (2011)
Discovery and characterization of non-ATP site inhibitors of the mitogen activated protein (MAP) kinases.ACS chemical biology, 6 3
-
Yusuke Miyazaki, Ling-chun Chen, Bernard Chu, T. Swigut, T. Wandless (2015)
Author response: Distinct transcriptional responses elicited by unfolded nuclear or cytoplasmic protein in mammalian cellseLife
-
A. Omlin, Robert Jones, R. Noll, T. Satoh, M. Niwakawa, Susan Smith, Janet Graham, M. Ong, Richard Finkelman, J. Schellens, A. Zivi, M. Crespo, R. Riisnaes, Daniel Nava-Rodrigues, M. Malone, Caroline Dive, R. Sloane, D. Moore, J. Alumkal, A. Dymond, Paul Dickinson, Malcolm Ranson, G. Clack, J. Bono, Tony Elliott (2015)
AZD3514, an oral selective androgen receptor down-regulator in patients with castration-resistant prostate cancer – results of two parallel first-in-human phase I studiesInvestigational New Drugs, 33
-
Bryan Wittmann, A. Sherk, D. McDonnell (2007)
Definition of functionally important mechanistic differences among selective estrogen receptor down-regulators.Cancer research, 67 19
-
J. Krönke, N. Udeshi, A. Narla, Peter Grauman, Slater Hurst, M. McConkey, Tanya Svinkina, D. Heckl, Eamon Comer, Xiaoyu Li, Christie Ciarlo, Emily Hartman, N. Munshi, M. Schenone, S. Schreiber, S. Carr, B. Ebert (2014)
Lenalidomide Causes Selective Degradation of IKZF1 and IKZF3 in Multiple Myeloma CellsScience, 343
-
A. Schneekloth, Mathieu Pucheault, H. Tae, C. Crews (2008)
Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics.Bioorganic & medicinal chemistry letters, 18 22
-
Xu Tan, L. Calderon-Villalobos, M. Sharon, Changxue Zheng, C. Robinson, M. Estelle, N. Zheng (2007)
Mechanism of auxin perception by the TIR1 ubiquitin ligaseNature, 446
- Publisher
- Annual Reviews
- Copyright
- Copyright © 2017 by Annual Reviews. All rights reserved
- ISSN
- 0362-1642
- eISSN
- 1545-4304
- DOI
- 10.1146/annurev-pharmtox-010715-103507
- pmid
- 27732798
- Publisher site
- See Article on Publisher Site
Abstract
Protein homeostasis networks are highly regulated systems responsible for maintaining the health and productivity of cells. Whereas therapeutics have been developed to disrupt protein homeostasis, more recently identified techniques have been used to repurpose homeostatic networks to effect degradation of disease-relevant proteins. Here, we review recent advances in the use of small molecules to degrade proteins in a selective manner. First, we highlight all-small-molecule techniques with direct clinical application. Second, we describe techniques that may find broader acceptance in the biomedical research community that require little or no synthetic chemistry. In addition to serving as innovative research tools, these new approaches to control intracellular protein levels offer the potential to develop novel therapeutics targeting proteins that are not currently pharmaceutically vulnerable.
Journal
Annual Review of Pharmacology and Toxicology – Annual Reviews
Published: Jan 6, 2017