IndraLab

Statements

Vemurafenib binds BRAF. 10 / 13
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"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
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"Since vemurafenib binds less specifically to mutated BRAF than dabrafenib and binding to wildtype BRAF could inhibit ERK activation in immune cells."
29438368
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"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
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"The small molecule inhibitors vemurafenib and dabrafenib selectively bind the active conformation of BRAF and inhibit signal transduction between BRAF and MEK."
26174532
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"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
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"Thus, vemurafenib can still bind to kinase-dead BRAF and promotes its effect to transactivate wild-type CRAF."
27025703
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"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
Vemurafenib binds BRAF-V600E. 9 / 9
| 9
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"The kinase domain of B-raf V600E has strong structural homology with the kinase domains of hRIPK1 and hRIPK3, which explains the similarities between the crystal structure of Nec-1 bound to RIPK1 and the structure of Vemurafenib bound to B-Raf V600E."
28661484
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"This was also shown to be the case for vemurafenib binding to BRAF V600E."
30926642
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"It has been shown that vemurafenib binding to BRAF V600E paradoxically activates downstream MAPK signaling via dimerization with non mutant RAF family members and allosteric activation of the non mutant partner [XREF_BIBR]."
26405815
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"Comparison of this structure to the inactive conformation seen in the structure of vemurafenib bound to BRAF V600E reveals significant differences in the orientation of alphaC."
26996308
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"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
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"Comparison of alphaC position in the dabrafenib bound and vemurafenib bound BRAF V600E indicates that vemurafenib induces a greater alphaC shift then dabrafenib."
26996308
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"Crystal structures of vemurafenib bound to BRAF V600E reveal a solvent exposed chloride at the para-position on the phenyl ring, which we posited would be ideal for linker addition (PDB : 3OG7) 34."
33568647
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"Based on prior structural data of MEK1-BRAF, vemurafenib bound V600E BRAF, and MEK1-KSR2 and structural alignments of vemurafenib bound V600E BRAF with BRAF or KSR2, we hypothesized a regulatory V600E BRAF- MUT MEK complex where V600E BRAF arginine 662 makes critical contacts with MEK residues in one complex interface (XREF_FIG)."
25600339
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"PLX4032 binds V600E mutant BRAF with high affinity and inhibits ERK signaling output."
24460976
Vemurafenib binds mutated BRAF. 2 / 2
| 2
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"However, the mechanism of this selectivity is not clear since vemurafenib binds BRAF WT as well as BRAF mutants."
33568647
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
Vemurafenib binds BRAF and F595. 1 / 1
| 1
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"The favorable route in the Vemurafenib and BRAF complex proceeded from F595 of the drug bound monomer to I592 and the alphaC-beta4-loop residues (N512, I513) before reaching H510 residue."
27861609
Vemurafenib binds mutated BRAF and V600. 1 / 1
| 1
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"Vemurafenib and dabrafenib bind to the highly active monomeric mutant BRAF (V600) to inhibit its function."
26730180