IndraLab

Statements

EGFR binds ERBB2 and ERBB4. 33 / 33
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"Neratinib is a third-generation orally available ERBB1/2/4 inhibitor that irreversibly binds to ERBB1, ERBB2 and ERBB4."
29163826
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"Afatinib binds to EGFR, HER2 and HER4, irreversibly inhibiting tyrosine kinase autophosphorylation; it also inhibits transphosphorylation of HER3."
27197880
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"Secondly, the ability of the antibodies to bind HER1, HER2 and HER4 peptides was tested in a competitive enzyme-linked immunosorbent assay (ELISA)."
22092409
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"Some studies have reported that ERBB4 regulated cell differentiation and cell survival via the Mek/Erk pathway [ xref , xref ] and lapatinib inhibited the interaction of ERBB4 with EGFR and ERBB2 [ xref ]."
26907936
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"Neratinib is an irreversible EGFR, HER2, and HER4 inhibitor that forms a covalent adduct with the conserved cysteine corresponding to the 797 position on the EGFR kinase [ xref ]."
33187135
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"Dacomitinib binds irreversibly to EGFR, Her2 and Her4."
26371045
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"The different family members interact with each other, i.e., HER3, which lacks intrinsic kinase activity, can form heterodimers with HER1, HER2, and HER4 [ xref ]."
33327495
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"In contrast, afatinib irreversibly binds to EGFR, ERBB2, and ERBB4 and blocks transphosphorylation of ERBB3 to inhibit all ERBB family signaling xref ."
33953280
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"Neratinib interacts with the catalytic domain of HER1, HER2, and HER4 [ xref ]."
32947780
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"In cancer, ErbB3 activation is driven by a ligand-dependent mechanism through the formation of heterodimers with EGFR, ErbB2, or ErbB4 or via a ligand-independent process through heterodimerization with ErbB2 overexpressed in breast tumors or other cancers."
26460020
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"Autodock Vina xref was applied to get the starting structures for Saquinavir and Indinavir when bound to EGFR, ErbB2 and ErbB4."
21552547
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"Afatinib is an irreversible ErbB family blocker that covalently binds to EGFR, HER2 and HER4, and inhibits signalling from all ErbB family homo- and heterodimers ( xref ; xref )."
29337963
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"SIGNIFICANCE STATEMENT: This articles reviews ERBB4 function in the context of the mechanistic model that ERBB4 homodimers function as tumor suppressors, whereas ERBB4-EGFR or ERBB4-ERBB2 heterodimers act as oncogenes."
34987087
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"Neratinib is an oral irreversible small-molecule TKI that binds to and inhibits HER1, HER2, and HER4 and that received FDA approval in 2017 for extended adjuvant therapy of HER2-positive early-stage breast cancer after 1 year of trastuzumab [ xref – xref ]."
31073788
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"The ErbB family of receptor tyrosine kinases is represented in mammals by EGFR kinase (ErbB1) and ErbB2–ErbB4, which form homo- and heterodimers ( xref ; xref )."
16505146
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"Preclinical studies indicate that afatinib inhibits the kinase activity of wild type and mutant forms of EGFR, HER2 and ErbB4 [11,13] ."
23664448
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"The covalent binding of afatinib to EGFR, HER2, and HER4 irreversibly inhibits the tyrosine kinase activity of these receptors, resulting in reduced auto- and transphosphorylation within the ErbB dimers and inhibition of important steps in the signal transduction of all ErbB receptor family members [ xref , xref ]."
27470518
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"Neratinib (MM: 557 Da) is a tyrosine kinase inhibitor that together with their active metabolites irreversibly binds to EGFR, HER2, and HER4 reducing autophosphorylation of the receptors, and, as a consequence, blocks signal transduction."
32508921
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"The selectivity of afatinib was confirmed by independent investigators assessing the binding properties of afatinib in 442 kinases covering more than 80 % of the human kinome (Davis et al. xref ): it interacted significantly (low nanomolar range; 0.25 nM <  K d  < 6.3 nM) only with EGFR, HER2 and ErbB4; except for GAK, BLK, IRAK1, EpHA6, HIPK4, PhKG2 and phosphorylated Abl-1 kinase (79 nM <  K d  < 570 nM), all other K d values were above 1,000 nM, illustrating the high selectivity of afatinib on the human kinome."
24643470
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"Dacomitinib is an orally bioavailable, highly selective, second-generation small-molecule inhibitor of EGFR, HER2 and HER4, that specifically and irreversibly binds to and inhibits these receptors, re[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
29734047
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"HER3 belongs to the epidermal growth factor receptor (EGFR) family and is known to form an active heterodimer with other three family members EGFR, HER2, and HER4."
34184091
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"The calculated MM/GBSA binding free energies for Saquinavir are -8.51, -10.12 and -9.37 kcal/mol when bound to EGFR, ErbB2 and ErbB4, respectively and -1.11, -1.68 and -2.51 kcal/mol, respectively, for Indinavir."
21552547
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"In this way, activation of this receptor is achieved only through the formation of heterodimers with EGFR, ERBB2 or ERBB4 [ xref – xref ]."
25248370
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"In addition to gefitinib and erlotinib, a second-generation EGFR/HER-TKI afatinib is approved as a first-line treatment for the advanced NSCLC harboring act EGFR m in the US, Europe, Taiwan, Japan, and other countries. xref Afatinib is an ATP-competitive aniline-quinazoline derivate containing a reactive acrylamide group, covalently binding to EGFR, HER2, and HER4 and irreversibly inhibiting HER-family phosphorylation and signal transduction. xref The theoretical advantages and promising preclinical data indicated that afatinib irreversibly inhibited the enzymatic activation of wt EGFR , EGFR L858R , EGFR L858R/T790M , EGFR L858R/T854A , wt HER2 , HER2 amplification, and wt HER4 , as well as showed antitumor activities in both EGFR/HER-TKI-naive and resistant tumor cells and xenograft models. xref , xref "
27660463
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"In contrast, we did not find any association of ErbB2 or ErbB4 with EGFR during the infection (Figure xref ), although ErbB2 is widely reported to be a heterodimerization partner for EGFR (Graus-Porta et al., xref ), suggesting that ErbB3 might be recruited to EGFR during its phosphorylation."
30687645
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"Afatinib covalently binds to EGFR, HER2, and HER4, and irreversibly inhibits tyrosine kinase autophosphorylation and downregulates ErbB signaling."
32143669
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"Since HER3 lacks intrinsic kinase activity, induction of signal occurs through formation of Heterodimers with EGFR, HER2 and HER4 ( xref )."
26734469
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"We also investigated the effects of trastuzumab and pertuzumab on five different heterodimers in vitro: HER2-EGFR, HER2-HER4, HER2-HER3, HER3-HER4, HER3-EGFR."
35158800
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"Since ERBB3 lacks intrinsic kinase activity, signal transduction occurs through formation of heterodimers with EGFR, ERBB2, and ERBB4."
18454306
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"The signals of the HER1, HER2, and HER4 homodimers are weak compared with that of the HER2 heterodimer."
33034269
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"Afatinib covalently binds to EGFR, HER2, and ErbB4 [ xref ]."
26123538
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"Afatinib was more likely to be related to adverse events, as expected because of its irreversible binding to ATP site of EGFR, HER2 and HER4, in contrast to the reversible nature of binding of gefitinib and erlotinib. [ xref – xref ]."
29545937
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"Afatinib is an ATP-competitive aniline-quinazoline derivate which covalently binds to EGFR, HER2, and HER4 and irreversibly inhibits HER-family phosphorylation and signal transduction ( xref )."
29872644