IndraLab

Statements

Vemurafenib binds BRAF. 12 / 13
| 11 1
reach
"Consistent with the degree of sequence conservation, the Nec-1a-bound RIP1 structure is quite similar to that of PLX4032 bound B-RAF, with an rmsd of 1.041 A over 140 aligned Calpha atoms."
23473668
reach
"Since vemurafenib binds less specifically to mutated BRAF than dabrafenib and binding to wildtype BRAF could inhibit ERK activation in immune cells."
29438368
reach
"To model this possibility, we created MEMI1.2 in which binding of vemurafenib to monomeric or dimeric BRAF is explicitly specified by separate sentences, allowing the effects of different binding affinities to be explored (Fig XREF_FIG D)."
29175850
reach
"The small molecule inhibitors vemurafenib and dabrafenib selectively bind the active conformation of BRAF and inhibit signal transduction between BRAF and MEK."
26174532
reach
"The second article incorporated United States Food and Drug Administration-approved type 1.5 inhibitor vemurafenib, that binds BRAF as well as class 1, 2, and 3 BRAF mutants, into VHL-recruiting degrader SJF-0628 [3]."
35042023
reach
"The crystal structures of the BRAF and V600E complex with PLX7904 (pdb id 4XV1), the BRAF V600E mutant bound with PLX7922 (pdb id 4XV3), and the BRAF and PLX5568 complex (pdb id 4XV9) have revealed a binding mode and interaction profiles that are highly reminiscent of the BRAF and Vemurafenib complex."
27861609
isi
"Results Several compounds (including anthracyclines) bound with higher affinities than the control drugs (sorafenib and vemurafenib for BRAF and PI-103 and LY-294,002 for PIK3R1)."
33313992
reach
"Thus, vemurafenib can still bind to kinase-dead BRAF and promotes its effect to transactivate wild-type CRAF."
27025703
reach
"In these structures, signaling pathways become more diverse with 45% occupancy for the most optimal path in the Vemurafenib and BRAF complex and 55% occupancy in the PLX7904 and BRAF complex (XREF_FIG)."
27861609
reach
"Vemurafenib binding to the wild type BRAF inhibits BRAF but causes transactivation of CRAF, leading to MEK and ERK activation rather than inhibition."
22340588
reach
"However, the mechanism of this selectivity is not clear since vemurafenib binds BRAF WT as well as BRAF mutants."
33568647
reach
"Additionally, vemurafenib has been found to induce the trans-activation of WT-BRAF or CRAF through hetero-dimerization between vemurafenib bound BRAF V600E and WT-BRAF or CRAF."
28174173