IndraLab

Statements

Vemurafenib binds BRAF. 21 / 22
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"The movement of the αC-helix allows for the binding of vemurafenib to B-Raf as described in Section 6 ."
30118796
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"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
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"B-Raf exists in an inactive αC out configuration with DFG-D in and the overall classification of the B-Raf – vemurafenib complex conforms to that of a type I½A antagonist [25] ."
30877063
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"However, the mechanism of this selectivity is not clear since vemurafenib binds BRAF WT as well as BRAF mutants."
33568647
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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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"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
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"B-Raf exists in an inactive αC out configuration with DFG-D in and the overall classification of the B-Raf–vemurafenib complex conforms to that of a type I½A antagonist [52] ."
33971270
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"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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"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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"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
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"The structures of standard ligands vemurafenib, trametinib, and dasatinib that selectively bind to BRAF (1UWH), MEK (4U7Z), ACK-1 (5ZXB), and SCR (3F3V) were downloaded from the PDB database, where they were determined as reference ligands binding to the target kinases."
| PMC
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"A binding mode of LN3162 was elaborated (Figure 2D) based on intra-protein methyl-methyl and intermolecular protein ligand NOE cross-peaks, as well as available crystal structures of vemurafenib-bound BRAF and ZAK (PDB: 3OG7, 4RZV, and 5HES)."
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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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"Vemurafenib binding to the wild type BRAF inhibits BRAF but causes transactivation of CRAF, leading to MEK and ERK activation rather than inhibition."
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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)."
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"Fig. 4B shows allosteric Inhibitor PLX4032 bound to BRaf."
28149177
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"We treated cells expressing BRAF (figure S6A) or BRAF (figure S6B), embedded in our sensor construct, with the inhibitor vemurafenib, which selectively binds the active conformation of the BRAF kinase domain ."
38106090
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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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"Notably, variants at the same position were generally either all sensitized or all resistant, suggesting that susceptibility to degradation by SJF0628 is largely defined by the position of a mutation rather than its identity.We explored the structural basis for the location dependence of BRaf variant PROTAC sensitivity by projecting position-averaged degradation scores onto the structure of Vemurafenib-bound BRaf (Extended Data Fig. 9f)."
38659825
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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."
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"We treated cells expressing BRAF (Figure S6A) or BRAF (Figure S6B), embedded in our sensor construct, with the inhibitor vemurafenib, which selectively binds the active conformation of the BRAF kinase domain (Joseph et al., 2010)."
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