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Cell Cycle Volume 12, 2013 - Issue 14
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Carboxamide SIRT1 inhibitors block DBC1 binding via an acetylation-independent mechanism

Basil P Hubbard Department of Genetics; Harvard Medical School; Boston, MA USA
,
Christine Loh Sirtris, a GSK Company; Cambridge, MA USA
,
Ana P Gomes Department of Genetics; Harvard Medical School; Boston, MA USA
,
Jun Li Department of Genetics; Harvard Medical School; Boston, MA USA
,
Quinn Lu GlaxoSmithKline; Collegeville, PA USA
,
Taylor LG Doyle GlaxoSmithKline; Collegeville, PA USA
,
Jeremy S Disch Sirtris, a GSK Company; Cambridge, MA USA
,
Sean M Armour Department of Genetics; Harvard Medical School; Boston, MA USA
,
James L Ellis Sirtris, a GSK Company; Cambridge, MA USA
,
George P Vlasuk Sirtris, a GSK Company; Cambridge, MA USA
&
David A Sinclair Department of Genetics; Harvard Medical School; Boston, MA USA; Department of Pharmacology; University of New South Wales; Sydney, NSW AustraliaCorrespondence[email protected]
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Pages 2233-2240 | Received 01 Jun 2013, Accepted 03 Jun 2013, Published online: 20 Jun 2013

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Sylvain Broussy, Hanna Laaroussi & Michel Vidal. (2020) Biochemical mechanism and biological effects of the inhibition of silent information regulator 1 (SIRT1) by EX-527 (SEN0014196 or selisistat). Journal of Enzyme Inhibition and Medicinal Chemistry 35:1, pages 1124-1136.
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Hong Zheng, Leixiang Yang, Lirong Peng, Victoria Izumi, John Koomen, Edward Seto & Jiandong Chen. (2013) hMOF Acetylation of DBC1/CCAR2 Prevents Binding and Inhibition of SirT1. Molecular and Cellular Biology 33:24, pages 4960-4970.
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Articles from other publishers (14)

Marzieh Ramezani Farani, Maryam Sarlak, Amir Gholami, Maryam Azaraian, Maryam Moradi Binabaj, Sareh Kakavandi, Murtaza M. Tambuwala, Afshin Taheriazam, Mehrdad Hashemi & Sorayya Ghasemi. (2023) Epigenetic drugs as new emerging therapeutics: What is the scale's orientation of application and challenges?. Pathology - Research and Practice 248, pages 154688.
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Aliabbas Zia, Faezeh Sahebdel, Tahereh Farkhondeh, Milad Ashrafizadeh, Ali Zarrabi, Kiavash Hushmandi & Saeed Samarghandian. (2021) A review study on the modulation of SIRT1 expression by miRNAs in aging and age-associated diseases. International Journal of Biological Macromolecules 188, pages 52-61.
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Miao WangHening Lin. (2021) Understanding the Function of Mammalian Sirtuins and Protein Lysine Acylation. Annual Review of Biochemistry 90:1, pages 245-285.
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Ramu Manjula, Kumari Anuja & Francisco J. Alcain. (2021) SIRT1 and SIRT2 Activity Control in Neurodegenerative Diseases. Frontiers in Pharmacology 11.
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Evan M. Kerek, Kevin H. Yoon, Shu Y. Luo, Jerry Chen, Robert Valencia, Olivier Julien, Andrew J. Waskiewicz & Basil P. Hubbard. (2021) A conserved acetylation switch enables pharmacological control of tubby-like protein stability. Journal of Biological Chemistry 296, pages 100073.
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Gavin S. Johnson, Praveen Rajendran & Roderick H. Dashwood. (2020) CCAR1 and CCAR2 as gene chameleons with antagonistic duality: Preclinical, human translational, and mechanistic basis . Cancer Science 111:10, pages 3416-3425.
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Troy C. Krzysiak, Laurel Thomas, You-Jin Choi, Sylvain Auclair, Yiqi Qian, Shan Luan, Stephanie M. Krasnow, Laura L. Thomas, Leonardus M.I. Koharudin, Panayiotis V. Benos, Daniel L. Marks, Angela M. Gronenborn & Gary Thomas. (2018) An Insulin-Responsive Sensor in the SIRT1 Disordered Region Binds DBC1 and PACS-2 to Control Enzyme Activity. Molecular Cell 72:6, pages 985-998.e7.
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Martina Magni, Giacomo Buscemi & Laura Zannini. (2018) Cell cycle and apoptosis regulator 2 at the interface between DNA damage response and cell physiology. Mutation Research/Reviews in Mutation Research 776, pages 1-9.
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Hyeog Kang, Shinichi Oka, Duck-Yeon Lee, Junhong Park, Angel M. Aponte, Young-Sang Jung, Jacob Bitterman, Peiyong Zhai, Yi He, Hamed Kooshapur, Rodolfo Ghirlando, Nico Tjandra, Sean B. Lee, Myung K. Kim, Junichi Sadoshima & Jay H. Chung. (2017) Sirt1 carboxyl-domain is an ATP-repressible domain that is transferrable to other proteins. Nature Communications 8:1.
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H. Dai, J.L. Ellis, D.A. Sinclair & B.P. Hubbard. 2016. Enzymes of Epigenetics, Part B. Enzymes of Epigenetics, Part B 213 244 .
Martina Magni, Vincenzo Ruscica, Michela Restelli, Enrico Fontanella, Giacomo Buscemi & Laura Zannini. (2015) CCAR2/DBC1 is required for Chk2-dependent KAP1 phosphorylation and repair of DNA damage. Oncotarget 6:19, pages 17817-17831.
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Jessica Brunquell, Jia Yuan, Aqeela Erwin, Sandy D. Westerheide & Bin Xue. (2014) DBC1/CCAR2 and CCAR1 Are Largely Disordered Proteins that Have Evolved from One Common Ancestor. BioMed Research International 2014, pages 1-13.
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John R. P. Knight, Simon J. Allison & Jo Milner. (2013) Active regulator of SIRT1 is required for cancer cell survival but not for SIRT1 activity. Open Biology 3:11, pages 130130.
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Ladislav Mrzljak & Ignacio Munoz-Sanjuan. 2015. Behavioral Neurobiology of Huntington's Disease and Parkinson's Disease. Behavioral Neurobiology of Huntington's Disease and Parkinson's Disease 161 201 .

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