159088-48-9 Usage
Description
RAS INHIBITORY PEPTIDE, also known as RAS inhibitory peptide, is a synthetic peptide that contains the sequence PVPPR. This sequence corresponds to a region within the Son of sevenless homolog 1 (Sos1) protein, which is a guanine nucleotide exchange factor (GEF). RAS INHIBITORY PEPTIDE specifically blocks the interaction of the GEF with the SH3 domain of growth factor receptor-bound protein 2 (Grb2), preventing an interaction that is essential for Ras activation by receptor tyrosine kinases, such as the epidermal growth factor receptor.
Uses
Used in Pharmaceutical Industry:
RAS INHIBITORY PEPTIDE is used as a therapeutic agent for inhibiting the activation of the Ras protein, which plays a crucial role in cell signaling and is often mutated in various types of cancer. By blocking the interaction between Sos1 and Grb2, RAS INHIBITORY PEPTIDE can potentially prevent the uncontrolled cell growth and proliferation associated with cancer.
Used in Research Applications:
RAS INHIBITORY PEPTIDE is used as a research tool for studying the molecular mechanisms underlying Ras activation and its role in cell signaling pathways. It can be employed in various experimental setups, such as cell culture assays, to investigate the effects of Ras inhibition on cellular processes and to identify potential targets for therapeutic intervention in cancer and other diseases.
Used in Drug Development:
RAS INHIBITORY PEPTIDE serves as a lead compound in the development of novel drugs targeting the Ras signaling pathway. Its ability to specifically block the interaction between Sos1 and Grb2 can be leveraged to design and synthesize new molecules with improved potency, selectivity, and pharmacokinetic properties, ultimately leading to the development of more effective anti-cancer drugs.
Check Digit Verification of cas no
The CAS Registry Mumber 159088-48-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,5,9,0,8 and 8 respectively; the second part has 2 digits, 4 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 159088-48:
(8*1)+(7*5)+(6*9)+(5*0)+(4*8)+(3*8)+(2*4)+(1*8)=169
169 % 10 = 9
So 159088-48-9 is a valid CAS Registry Number.
159088-48-9Relevant articles and documents
High affinity Grb2-SH3 domain ligand incorporating Cβ-substituted prolines in a Sos-derived decapeptide
Jacquot, Yves,Broutin, Isabelle,Miclet, Emeric,Nicaise, Magali,Lequin, Olivier,Goasdoue, Nicole,Joss, Charlotte,Karoyan, Philippe,Desmadril, Michel,Ducruix, Arnaud,Lavielle, Solange
, p. 1439 - 1447 (2007)
Peptide ligands that disrupt MAPK pathways are of great interest for a better understanding of these signalling cascades and represent therefore an attractive target to control cell degenerative processes. In that context, selective disruption of the upstream Grb2/Sos complex in the Ras/MAPK cascade has focused extensive work. The Sos PPII decapeptide, which interacts with the Grb2-SH3 domains, has been modified in various positions and the best inhibitors designed so far are either dimeric ligands or peptoid analogues of the VPPPVPPRRR sequence. We report the synthesis of new Grb2 ligands in which the key Val5 residue has been replaced by a cis Cβ-substituted proline. Both fluorescence and ITC assays have been employed to measure the affinity of these substituted peptides for a recombinant Grb2 protein. Whereas proline in position 5 completely abolished the binding potency, a cis Cβ-methyl-L-proline restored the affinity. Other cis Cβ-proline substituents led to a complete loss of binding potency. Combining the best modifications: a cis Cβ-methylproline 5, N-acetylation, C-carboxamide and dimerization yielded a 560-fold affinity enhancement compared to the wild-type VPPPVPPRRR sequence. This study shows that Cβ-substituted prolines may constitute a new alternative for PPII ligands, combining entropy and enthalpy beneficial effects.
