Synonyms: (S)-JQ-35 | (S)-JQ35 | RG6146 | Ro-6870810 | RO-6870810 | RO6870810 | TEN010
Compound class:
Synthetic organic
Comment: TEN-010 (RO6870810) is a BET inhibitor [3]. Structurally it is an analogue of (+)-JQ1, with optimised chemical and biological properties. Development of TEN-010 was progressed by Roche, who acquired the originating biotech firm Tensha Therapeutics. Tensha claimed several bromodomain inhibitors in patent WO2016069578 [1].
BET inhibitors bind to the bromodomains of the bromodomain and extra-terminal motif (BET) proteins BRD2, BRD3, BRD4, and BRDT. This mechanism acts to prevent protein-protein interaction between BET proteins and acetylated histones and transcription factors. The action disrupts chromatin remodeling and inhibits expression of some growth-promoting genes which slows proliferation in susceptible tumours. |
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References |
1. Landau SB, Kagey M. (2016)
Bromodomain inhibitors. Patent number: WO2016069578. Assignee: Tensha Therapeutics, Inc.. Priority date: 27/10/2014. Publication date: 06/05/2016. |
2. Roboz GJ, Desai P, Lee S, Ritchie EK, Winer ES, DeMario M, Brennan B, Nüesch E, Chesne E, Brennan L et al.. (2021)
A dose escalation study of RO6870810/TEN-10 in patients with acute myeloid leukemia and myelodysplastic syndrome. Leuk Lymphoma, 62 (7): 1740-1748. [PMID:33586590] |
3. Shapiro GI, LoRusso P, Dowlati A, T Do K, Jacobson CA, Vaishampayan U, Weise A, Caimi PF, Eder JP, French CA et al.. (2021)
A Phase 1 study of RO6870810, a novel bromodomain and extra-terminal protein inhibitor, in patients with NUT carcinoma, other solid tumours, or diffuse large B-cell lymphoma. Br J Cancer, 124 (4): 744-753. [PMID:33311588] |