PROFILPELAJAR.COM

VUBI1

VUBI1
Clinical data
Drug classSOS1 activator
Identifiers
  • 6-chloro-2-(2,6-diazaspiro[3.3]heptan-2-yl)-1-[(4-fluoro-3,5-dimethylphenyl)methyl]-4-(4-methylpiperazin-1-yl)benzimidazole
CAS Number
PubChem CID
Chemical and physical data
FormulaC26H32ClFN6
Molar mass483.03 g·mol−1
3D model (JSmol)
  • CC1=CC(=CC(=C1F)C)CN2C3=C(C(=CC(=C3)Cl)N4CCN(CC4)C)N=C2N5CC6(C5)CNC6
  • InChI=1S/C26H32ClFN6/c1-17-8-19(9-18(2)23(17)28)12-34-22-11-20(27)10-21(32-6-4-31(3)5-7-32)24(22)30-25(34)33-15-26(16-33)13-29-14-26/h8-11,29H,4-7,12-16H2,1-3H3
  • Key:JWZAQUXBYYOGFA-UHFFFAOYSA-N

VUBI1 is a drug that acts as an activator of the guanine nucleotide exchange factor protein SOS1, increasing the rate at which it catalyzes the exchange of GDP for GTP on its target protein KRAS. While inhibitors of SOS1 have been more widely researched for the treatment of cancer, under some conditions increasing SOS1 activity can also have an anti-cancer effect by destructive overactivation of cellular signaling processes, so SOS1 activators are also of potential clinical interest, as well as being used for the study of the SOS1-KRAS intercellular pathway.[1][2]


References

  1. ^ Hodges TR, Abbott JR, Little AJ, Sarkar D, Salovich JM, Howes JE, et al. (October 2018). "Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS". Journal of Medicinal Chemistry. 61 (19): 8875–8894. doi:10.1021/acs.jmedchem.8b01108. PMC 8314423. PMID 30205005.
  2. ^ Hamilton G, Stickler S, Rath B (2023). "Targeting of SOS1: from SOS1 Activators to Proteolysis Targeting Chimeras". Current Pharmaceutical Design. 29 (22): 1741–1746. doi:10.2174/1381612829666230418114520. PMID 37073657.

Content Disclaimer

Informasi ini disarikan dari Wikipedia dan disajikan kembali untuk tujuan edukasi. Konten tersedia di bawah lisensi CC BY-SA 3.0. Kami tidak bertanggung jawab atas ketidakakuratan data yang bersumber dari kontribusi publik tersebut.

  1. The information displayed on this website is sourced in part or in whole from Wikipedia and has been adapted for the purpose of restating it. We strive to provide accurate and relevant information, however:
  2. There is no guarantee of absolute accuracy. Wikipedia is an open, collaborative project that can be edited by anyone, so information is subject to change.
  3. It is not intended to constitute professional advice. The content displayed is for informational and educational purposes only. For important decisions (e.g., medical, legal, or financial), please consult a professional.
  4. Content copyright. Wikipedia is licensed under the Creative Commons Attribution-ShareAlike License (CC BY-SA). This means that content may be reused with appropriate attribution and shared under a similar license.
  5. Responsible use. Any risk arising from the use of information from this website is entirely the responsibility of the user.