REFERENCES
1. Sung H, Ferlay J, Siegel RL, et al. Global cancer statistics 2020: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries. CA Cancer J Clin 2021;71:209-49.
2. Lepeltier E, Rijo P, Rizzolio F, et al. Nanomedicine to target multidrug resistant tumors. Drug Resist Updat 2020;52:100704.
3. Gandullo-Sánchez L, Ocaña A, Pandiella A. HER3 in cancer: from the bench to the bedside. J Exp Clin Cancer Res 2022;41:310.
4. Uliano J, Corvaja C, Curigliano G, Tarantino P. Targeting HER3 for cancer treatment: a new horizon for an old target. ESMO Open 2023;8:100790.
5. Appert-Collin A, Hubert P, Crémel G, Bennasroune A. Role of ErbB receptors in cancer cell migration and invasion. Front Pharmacol 2015;6:283.
6. Diwanji D, Trenker R, Thaker TM, et al. Structures of the HER2-HER3-NRG1β complex reveal a dynamic dimer interface. Nature 2021;600:339-43.
7. Montero JC, Rodríguez-Barrueco R, Ocaña A, Díaz-Rodríguez E, Esparís-Ogando A, Pandiella A. Neuregulins and cancer. Clin Cancer Res 2008;14:3237-41.
8. Haikala HM, Jänne PA. Thirty years of HER3: from basic biology to therapeutic interventions. Clin Cancer Res 2021;27:3528-39.
9. Frazier NM, Brand T, Gordan JD, Grandis J, Jura N. Overexpression-mediated activation of MET in the Golgi promotes HER3/ERBB3 phosphorylation. Oncogene 2019;38:1936-50.
10. Kunii K, Davis L, Gorenstein J, et al. FGFR2-amplified gastric cancer cell lines require FGFR2 and Erbb3 signaling for growth and survival. Cancer Res 2008;68:2340-8.
11. Camblin AJ, Tan G, Curley MD, et al. Dual targeting of IGF-1R and ErbB3 as a potential therapeutic regimen for ovarian cancer. Sci Rep 2019;9:16832.
12. Shi F, Telesco SE, Liu Y, Radhakrishnan R, Lemmon MA. ErbB3/HER3 intracellular domain is competent to bind ATP and catalyze autophosphorylation. Proc Natl Acad Sci U S A 2010;107:7692-7.
13. Steinkamp MP, Low-Nam ST, Yang S, Lidke KA, Lidke DS, Wilson BS. erbB3 is an active tyrosine kinase capable of homo- and heterointeractions. Mol Cell Biol 2014;34:965-77.
14. Majumder A. HER3: toward the prognostic significance, therapeutic potential, current challenges, and future therapeutics in different types of cancer. Cells 2023;12:2517.
15. Xue C, Liang F, Mahmood R, et al. ErbB3-dependent motility and intravasation in breast cancer metastasis. Cancer Res 2006;66:1418-26.
16. Gil V, Miranda S, Riisnaes R, et al; PCF/SU2C International Prostate Cancer Dream Team. HER3 is an actionable target in advanced prostate cancer. Cancer Res 2021;81:6207-18.
17. Scharpenseel H, Hanssen A, Loges S, et al. EGFR and HER3 expression in circulating tumor cells and tumor tissue from non-small cell lung cancer patients. Sci Rep 2019;9:7406.
18. Lédel F, Hallström M, Ragnhammar P, Öhrling K, Edler D. HER3 expression in patients with primary colorectal cancer and corresponding lymph node metastases related to clinical outcome. Eur J Cancer 2014;50:656-62.
19. Ueno Y, Sakurai H, Tsunoda S, et al. Heregulin-induced activation of ErbB3 by EGFR tyrosine kinase activity promotes tumor growth and metastasis in melanoma cells. Int J Cancer 2008;123:340-7.
20. Sheng Q, Liu X, Fleming E, et al. An activated ErbB3/NRG1 autocrine loop supports in vivo proliferation in ovarian cancer cells. Cancer Cell 2010;17:298-310.
21. Wang L, Yuan H, Li Y, Han Y. The role of HER3 in gastric cancer. Biomed Pharmacother 2014;68:809-12.
22. Liles JS, Arnoletti JP, Tzeng CW, et al. ErbB3 expression promotes tumorigenesis in pancreatic adenocarcinoma. Cancer Biol Ther 2010;10:555-63.
23. Wang Z, Goto Y, Allevato MM, et al. Disruption of the HER3-PI3K-mTOR oncogenic signaling axis and PD-1 blockade as a multimodal precision immunotherapy in head and neck cancer. Nat Commun 2021;12:2383.
24. Liu X, Liu S, Lyu H, Riker AI, Zhang Y, Liu B. Development of effective therapeutics targeting HER3 for cancer treatment. Biol Proced Online 2019;21:5.
25. Liu R, Chen Y, Liu G, et al. PI3K/AKT pathway as a key link modulates the multidrug resistance of cancers. Cell Death Dis 2020;11:797.
26. Lee L, Ramos-Alvarez I, Moody TW, Mantey SA, Jensen RT. Neuropeptide bombesin receptor activation stimulates growth of lung cancer cells through HER3 with a MAPK-dependent mechanism. Biochim Biophys Acta Mol Cell Res 2020;1867:118625.
27. Lee S, Rauch J, Kolch W. Targeting MAPK signaling in cancer: mechanisms of drug resistance and sensitivity. Int J Mol Sci 2020;21:1102.
28. Huang XL, Khan MI, Wang J, et al. Role of receptor tyrosine kinases mediated signal transduction pathways in tumor growth and angiogenesis - New insight and futuristic vision. Int J Biol Macromol 2021;180:739-52.
29. Erjala K, Sundvall M, Junttila TT, et al. Signaling via ErbB2 and ErbB3 associates with resistance and epidermal growth factor receptor (EGFR) amplification with sensitivity to EGFR inhibitor gefitinib in head and neck squamous cell carcinoma cells. Clin Cancer Res 2006;12:4103-11.
30. Huang X, Gao L, Wang S, et al. Heterotrimerization of the growth factor receptors erbB2, erbB3, and insulin-like growth factor-i receptor in breast cancer cells resistant to herceptin. Cancer Res 2010;70:1204-14.
31. Yang L, Li Y, Shen E, et al. NRG1-dependent activation of HER3 induces primary resistance to trastuzumab in HER2-overexpressing breast cancer cells. Int J Oncol 2017;51:1553-62.
32. Ye P, Wang Y, Li R, Chen W, Wan L, Cai P. The HER family as therapeutic targets in colorectal cancer. Crit Rev Oncol Hematol 2022;174:103681.
33. Tao JJ, Castel P, Radosevic-Robin N, et al. Antagonism of EGFR and HER3 enhances the response to inhibitors of the PI3K-Akt pathway in triple-negative breast cancer. Sci Signal 2014;7:ra29.
34. Zhang Y, Liang S, Xiao B, et al. MiR-323a regulates ErbB3/EGFR and blocks gefitinib resistance acquisition in colorectal cancer. Cell Death Dis 2022;13:256.
35. Engelman JA, Zejnullahu K, Mitsudomi T, et al. MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science 2007;316:1039-43.
36. Wang S, Huang X, Lee CK, Liu B. Elevated expression of erbB3 confers paclitaxel resistance in erbB2-overexpressing breast cancer cells via upregulation of Survivin. Oncogene 2010;29:4225-36.
37. Knuefermann C, Lu Y, Liu B, et al. HER2/PI-3K/Akt activation leads to a multidrug resistance in human breast adenocarcinoma cells. Oncogene 2003;22:3205-12.
38. Bezler M, Hengstler JG, Ullrich A. Inhibition of doxorubicin-induced HER3-PI3K-AKT signalling enhances apoptosis of ovarian cancer cells. Mol Oncol 2012;6:516-29.
39. He G, Di X, Yan J, Zhu C, Sun X, Zhang S. Silencing human epidermal growth factor receptor-3 radiosensitizes human luminal A breast cancer cells. Cancer Sci 2018;109:3774-82.
40. Shou J, Massarweh S, Osborne CK, et al. Mechanisms of tamoxifen resistance: increased estrogen receptor-HER2/neu cross-talk in ER/HER2-positive breast cancer. J Natl Cancer Inst 2004;96:926-35.
41. Liu B, Ordonez-Ercan D, Fan Z, Edgerton SM, Yang X, Thor AD. Downregulation of erbB3 abrogates erbB2-mediated tamoxifen resistance in breast cancer cells. Int J Cancer 2007;120:1874-82.
42. Papadimitropoulou A, Vellon L, Atlas E, et al. Heregulin drives endocrine resistance by altering IL-8 expression in ER-positive breast cancer. Int J Mol Sci 2020;21:7737.
43. Frogne T, Benjaminsen RV, Sonne-Hansen K, et al. Activation of ErbB3, EGFR and Erk is essential for growth of human breast cancer cell lines with acquired resistance to fulvestrant. Breast Cancer Res Treat 2009;114:263-75.
44. Jathal MK, Chen L, Mudryj M, Ghosh PM. Targeting ErbB3: the new RTK(id) on the prostate cancer block. Immunol Endocr Metab Agents Med Chem 2011;11:131-49.
45. Zhang Z, Karthaus WR, Lee YS, et al. Tumor microenvironment-derived NRG1 promotes antiandrogen resistance in prostate cancer. Cancer Cell 2020;38:279-96.e9.
46. Drago JZ, Ferraro E, Abuhadra N, Modi S. Beyond HER2: targeting the ErbB receptor family in breast cancer. Cancer Treat Rev 2022;109:102436.
47. Malm M, Frejd FY, Ståhl S, Löfblom J. Targeting HER3 using mono- and bispecific antibodies or alternative scaffolds. MAbs 2016;8:1195-209.
48. Forster MD, Dillon MT, Kocsis J, et al. Patritumab or placebo, with cetuximab plus platinum therapy in recurrent or metastatic squamous cell carcinoma of the head and neck: a randomised phase II study. Eur J Cancer 2019;123:36-47.
49. Sequist LV, Gray JE, Harb WA, et al. Randomized phase II trial of seribantumab in combination with erlotinib in patients with EGFR wild-type non-small cell lung cancer. Oncologist 2019;24:1095-102.
50. Cleary JM, Mcree AJ, O’neil BH, et al. A phase 1 study of MM-121 (a fully human monoclonal antibody targeting the epidermal growth factor receptor family member ErbB3) in combination with cetuximab and irinotecan in patients with advanced cancers. J Clin Oncol 2014;32:3076.
51. Cejalvo JM, Jacob W, Fleitas Kanonnikoff T, et al. A phase Ib/II study of HER3-targeting lumretuzumab in combination with carboplatin and paclitaxel as first-line treatment in patients with advanced or metastatic squamous non-small cell lung cancer. ESMO Open 2019;4:e000532.
52. Mirschberger C, Schiller CB, Schräml M, et al. RG7116, a therapeutic antibody that binds the inactive HER3 receptor and is optimized for immune effector activation. Cancer Res 2013;73:5183-94.
53. Jhaveri K, Drago JZ, Shah PD, et al. A phase I study of alpelisib in combination with trastuzumab and LJM716 in patients with PIK3CA-mutated HER2-positive metastatic breast cancer. Clin Cancer Res 2021;27:3867-75.
54. Hong M, Yoo Y, Kim M, et al. A novel therapeutic anti-ErbB3, ISU104 Exhibits potent antitumorigenic activity by inhibiting ligand binding and ErbB3 heterodimerization. Mol Cancer Ther 2021;20:1142-52.
55. Duvvuri U, George J, Kim S, et al. Molecular and clinical activity of CDX-3379, an anti-ErbB3 Monoclonal antibody, in head and neck squamous cell carcinoma patients. Clin Cancer Res 2019;25:5752-8.
56. Meetze K, Vincent S, Tyler S, et al. Neuregulin 1 expression is a predictive biomarker for response to AV-203, an ERBB3 inhibitory antibody, in human tumor models. Clin Cancer Res 2015;21:1106-14.
57. Menke-van der Houven van Oordt CW, McGeoch A, Bergstrom M, et al. Immuno-PET imaging to assess target engagement: experience from 89Zr-Anti-HER3 mAb (GSK2849330) in patients with solid tumors. J Nucl Med 2019;60:902-9.
58. Sala G, Rapposelli IG, Ghasemi R, et al. Consorzio Interuniversitario Nazionale per la Bio-Oncologia (CINBO). EV20, a novel anti-ErbB-3 humanized antibody, promotes ErbB-3 down-regulation and inhibits tumor growth in vivo. Transl Oncol 2013;6:676-84.
59. Wang Q, Zhang X, Shen E, et al. The anti-HER3 antibody in combination with trastuzumab exerts synergistic antitumor activity in HER2-positive gastric cancer. Cancer Lett 2016;380:20-30.
60. Lazrek Y, Dubreuil O, Garambois V, et al. Anti-HER3 domain 1 and 3 antibodies reduce tumor growth by hindering HER2/HER3 dimerization and AKT-induced MDM2, XIAP, and FoxO1 phosphorylation. Neoplasia 2013;15:335-47.
61. Turowec JP, Lau EWT, Wang X, et al. Functional genomic characterization of a synthetic anti-HER3 antibody reveals a role for ubiquitination by RNF41 in the anti-proliferative response. J Biol Chem 2019;294:1396-409.
62. Schmitt LC, Rau A, Seifert O, et al. Inhibition of HER3 activation and tumor growth with a human antibody binding to a conserved epitope formed by domain III and IV. MAbs 2017;9:831-43.
63. Thakkar D, Sancenon V, Taguiam MM, et al. 10D1F, an anti-HER3 antibody that uniquely blocks the receptor heterodimerization interface, potently inhibits tumor growth across a broad panel of tumor models. Mol Cancer Ther 2020;19:490-501.
64. LoRusso P, Jänne PA, Oliveira M, et al. Phase I study of U3-1287, a fully human anti-HER3 monoclonal antibody, in patients with advanced solid tumors. Clin Cancer Res 2013;19:3078-87.
65. Shimizu T, Yonesaka K, Hayashi H, et al. Phase 1 study of new formulation of patritumab (U3-1287) Process 2, a fully human anti-HER3 monoclonal antibody in combination with erlotinib in Japanese patients with advanced non-small cell lung cancer. Cancer Chemother Pharmacol 2017;79:489-95.
66. Yonesaka K, Hirotani K, Kawakami H, et al. Anti-HER3 monoclonal antibody patritumab sensitizes refractory non-small cell lung cancer to the epidermal growth factor receptor inhibitor erlotinib. Oncogene 2016;35:878-86.
67. Kawakami H, Okamoto I, Yonesaka K, et al. The anti-HER3 antibody patritumab abrogates cetuximab resistance mediated by heregulin in colorectal cancer cells. Oncotarget 2014;5:11847-56.
68. Li C, Brand TM, Iida M, et al. Human epidermal growth factor receptor 3 (HER3) blockade with U3-1287/AMG888 enhances the efficacy of radiation therapy in lung and head and neck carcinoma. Discov Med 2013;16:79-92.
69. Denlinger CS, Keedy VL, Moyo V, MacBeath G, Shapiro GI. Phase 1 dose escalation study of seribantumab (MM-121), an anti-HER3 monoclonal antibody, in patients with advanced solid tumors. Invest New Drugs 2021;39:1604-12.
70. Rathore M, Zhang W, Wright M, et al. Liver endothelium promotes HER3-mediated cell survival in colorectal cancer with wild-type and mutant KRAS. Mol Cancer Res 2022;20:996-1008.
71. Thavaneswaran S, Chan WY, Asghari R, et al. Clinical response to seribantumab, an anti-human epidermal growth factor receptor-3 immunoglobulin 2 monoclonal antibody, in a patient with metastatic pancreatic ductal adenocarcinoma harboring an NRG1 fusion. JCO Precis Oncol 2022;6:e2200263.
72. Odintsov I, Lui AJW, Sisso WJ, et al. The anti-HER3 mAb seribantumab effectively inhibits growth of patient-derived and isogenic cell line and xenograft models with oncogenic NRG1 fusions. Clin Cancer Res 2021;27:3154-66.
73. Rendell A, Thomas-Bland I, McCuish L, Taylor C, Binju M, Yu Y. Targeting tyrosine kinases in ovarian cancer: small molecule inhibitor and monoclonal antibody, where are we now? Biomedicines 2022;10:2113.
74. Steele TM, Tsamouri MM, Siddiqui S, et al. Cisplatin-induced increase in heregulin 1 and its attenuation by the monoclonal ErbB3 antibody seribantumab in bladder cancer. Sci Rep 2023;13:9617.
75. Abramson VG, Supko JG, Ballinger T, et al. Phase Ib study of safety and pharmacokinetics of the PI3K inhibitor SAR245408 with the HER3-neutralizing human antibody SAR256212 in patients with solid tumors. Clin Cancer Res 2017;23:3520-8.
76. Huang J, Wang S, Lyu H, et al. The anti-erbB3 antibody MM-121/SAR256212 in combination with trastuzumab exerts potent antitumor activity against trastuzumab-resistant breast cancer cells. Mol Cancer 2013;12:134.
77. Liles JS, Arnoletti JP, Kossenkov AV, et al. Targeting ErbB3-mediated stromal-epithelial interactions in pancreatic ductal adenocarcinoma. Br J Cancer 2011;105:523-33.
78. Jiang N, Wang D, Hu Z, et al. Combination of anti-HER3 antibody MM-121/SAR256212 and cetuximab inhibits tumor growth in preclinical models of head and neck squamous cell carcinoma. Mol Cancer Ther 2014;13:1826-36.
79. Liu JF, Ray-Coquard I, Selle F, et al. Randomized phase II trial of seribantumab in combination with paclitaxel in patients with advanced platinum-resistant or -refractory ovarian cancer. J Clin Oncol 2016;34:4345-53.
80. Kawakami H, Yonesaka K. HER3 and its ligand, heregulin, as targets for cancer therapy. Recent Pat Anticancer Drug Discov 2016;11:267-74.
81. Meulendijks D, Jacob W, Voest EE, et al. Phase Ib study of lumretuzumab plus cetuximab or erlotinib in solid tumor patients and evaluation of HER3 and heregulin as potential biomarkers of clinical activity. Clin Cancer Res 2017;23:5406-15.
82. Schneeweiss A, Park-Simon TW, Albanell J, et al. Phase Ib study evaluating safety and clinical activity of the anti-HER3 antibody lumretuzumab combined with the anti-HER2 antibody pertuzumab and paclitaxel in HER3-positive, HER2-low metastatic breast cancer. Invest New Drugs 2018;36:848-59.
83. Meulendijks D, Jacob W, Martinez-Garcia M, et al. First-in-human phase i study of lumretuzumab, a glycoengineered humanized anti-HER3 monoclonal antibody, in patients with metastatic or advanced HER3-positive solid tumors. Clin Cancer Res 2016;22:877-85.
85. Labrijn AF, Janmaat ML, Reichert JM, Parren PWHI. Bispecific antibodies: a mechanistic review of the pipeline. Nat Rev Drug Discov 2019;18:585-608.
86. Schram AM, Odintsov I, Espinosa-Cotton M, et al. Zenocutuzumab, a HER2xHER3 bispecific antibody, is effective therapy for tumors driven by NRG1 gene rearrangements. Cancer Discov 2022;12:1233-47.
87. Alsina M, Boni V, Schellens JH, et al. First-in-human phase 1/2 study of MCLA-128, a full length IgG1 bispecific antibody targeting HER2 and HER3: final phase 1 data and preliminary activity in HER2+ metastatic breast cancer (MBC). J Clin Oncol 2017;35:2522.
88. Denlinger CS, Alsina Maqueda M, Watkins DJ, et al. Randomized phase 2 study of paclitaxel (PTX), trastuzumab (T) with or without MM-111 in HER2 expressing gastroesophageal cancers (GEC). J Clin Oncol 2016;34:4043.
89. Kundranda M, Gracian AC, Zafar SF, et al. Randomized, double-blind, placebo-controlled phase II study of istiratumab (MM-141) plus nab-paclitaxel and gemcitabine versus nab-paclitaxel and gemcitabine in front-line metastatic pancreatic cancer (CARRIE). Ann Oncol 2020;31:79-87.
90. Lieu CH, Hidalgo M, Berlin JD, et al. A phase Ib dose-escalation study of the safety, tolerability, and pharmacokinetics of cobimetinib and duligotuzumab in patients with previously treated locally advanced or metastatic cancers with mutant KRAS. Oncologist 2017;22:1024-e89.
91. Juric D, Dienstmann R, Cervantes A, et al. Safety and pharmacokinetics/pharmacodynamics of the first-in-class dual action HER3/EGFR antibody MEHD7945A in locally advanced or metastatic epithelial tumors. Clin Cancer Res 2015;21:2462-70.
92. Xue J, Kong D, Yao Y, et al. Prediction of human pharmacokinetics and clinical effective dose of SI-B001, an EGFR/HER3 Bi-specific monoclonal antibody. J Pharm Sci 2020;109:3172-80.
93. Gu J, Yang J, Chang Q, Liu Z, Ghayur T, Gu J. Identification of anti-EGFR and anti-ErbB3 dual variable domains immunoglobulin (DVD-Ig) proteins with unique activities. PLoS One 2015;10:e0124135.
94. Rau A, Lieb WS, Seifert O, et al. Inhibition of tumor cell growth and cancer stem cell expansion by a bispecific antibody targeting EGFR and HER3. Mol Cancer Ther 2020;19:1474-85.
95. Rau A, Kocher K, Rommel M, et al. A bivalent, bispecific Dab-Fc antibody molecule for dual targeting of HER2 and HER3. MAbs 2021;13:1902034.
96. Hassani D, Amiri MM, Mohammadi M, et al. A novel tumor inhibitory hybridoma monoclonal antibody with dual specificity for HER3 and HER2. Curr Res Transl Med 2021;69:103277.
97. de Vries Schultink AHM, Doornbos RP, Bakker ABH, et al. Translational PK-PD modeling analysis of MCLA-128, a HER2/HER3 bispecific monoclonal antibody, to predict clinical efficacious exposure and dose. Invest New Drugs 2018;36:1006-15.
98. McDonagh CF, Huhalov A, Harms BD, et al. Antitumor activity of a novel bispecific antibody that targets the ErbB2/ErbB3 oncogenic unit and inhibits heregulin-induced activation of ErbB3. Mol Cancer Ther 2012;11:582-93.
99. Richards DA, Braiteh FS, Garcia AA, et al. A phase 1 study of MM-111, a bispecific HER2/HER3 antibody fusion protein, combined with multiple treatment regimens in patients with advanced HER2-positive solid tumors. J Clin Oncol 2014;32:651.
100. Yu S, Liu Q, Han X, et al. Development and clinical application of anti-HER2 monoclonal and bispecific antibodies for cancer treatment. Exp Hematol Oncol 2017;6:31.
101. Fitzgerald JB, Johnson BW, Baum J, et al. MM-141, an IGF-IR- and ErbB3-directed bispecific antibody, overcomes network adaptations that limit activity of IGF-IR inhibitors. Mol Cancer Ther 2014;13:410-25.
102. Camblin AJ, Pace EA, Adams S, et al. Dual inhibition of IGF-1R and ErbB3 enhances the activity of gemcitabine and nab-paclitaxel in preclinical models of pancreatic cancer. Clin Cancer Res 2018;24:2873-85.
103. Schaefer G, Haber L, Crocker LM, et al. A two-in-one antibody against HER3 and EGFR has superior inhibitory activity compared with monospecific antibodies. Cancer Cell 2011;20:472-86.
104. Jimeno A, Machiels JP, Wirth L, et al. Phase Ib study of duligotuzumab (MEHD7945A) plus cisplatin/5-fluorouracil or carboplatin/paclitaxel for first-line treatment of recurrent/metastatic squamous cell carcinoma of the head and neck. Cancer 2016;122:3803-11.
105. Huang S, Li C, Armstrong EA, et al. Dual targeting of EGFR and HER3 with MEHD7945A overcomes acquired resistance to EGFR inhibitors and radiation. Cancer Res 2013;73:824-33.
106. De Pauw I, Wouters A, Van den Bossche J, et al. Dual targeting of epidermal growth factor receptor and HER3 by MEHD7945A as monotherapy or in combination with cisplatin partially overcomes cetuximab resistance in head and neck squamous cell carcinoma cell lines. Cancer Biother Radiopharm 2017;32:229-38.
107. Laterza MM, Ciaramella V, Facchini BA, et al. Enhanced antitumor effect of trastuzumab and duligotuzumab or ipatasertib combination in HER-2 positive gastric cancer cells. Cancers 2021;13:2339.
108. Hill AG, Findlay MP, Burge ME, et al. Phase II study of the dual EGFR/HER3 inhibitor duligotuzumab (MEHD7945A) versus cetuximab in combination with FOLFIRI in second-line RAS wild-type metastatic colorectal cancer. Clin Cancer Res 2018;24:2276-84.
109. Marks JA, Wilgucki M, Liu SV, Reuss JE. Antibody-drug conjugates in non-small cell lung cancer: emergence of a novel therapeutic class. Curr Oncol Rep 2022;24:1829-41.
110. Hashimoto Y, Koyama K, Kamai Y, et al. A novel HER3-targeting antibody-drug conjugate, U3-1402, exhibits potent therapeutic efficacy through the delivery of cytotoxic payload by efficient internalization. Clin Cancer Res 2019;25:7151-61.
111. Fu Z, Li S, Han S, Shi C, Zhang Y. Antibody drug conjugate: the “biological missile” for targeted cancer therapy. Signal Transduct Target Ther 2022;7:93.
113. Wymant JM, Sayers EJ, Muir D, Jones AT. Strategic trastuzumab mediated crosslinking driving concomitant HER2 and HER3 endocytosis and degradation in breast cancer. J Cancer 2020;11:3288-302.
114. Janne PA, Yu HA, Johnson ML, et al. Safety and preliminary antitumor activity of U3-1402: a HER3-targeted antibody drug conjugate in EGFR TKI-resistant, EGFRm NSCLC. J Clin Oncol 2019;37:9010.
115. Capone E, Giansanti F, Ponziani S, et al. EV20-Sap, a novel anti-HER-3 antibody-drug conjugate, displays promising antitumor activity in melanoma. Oncotarget 2017;8:95412-24.
116. Capone E, Tryggvason T, Cela I, et al. HER-3 surface expression increases in advanced colorectal cancer representing a potential therapeutic target. Cell Death Discov 2023;9:400.
117. D’Agostino D, Gentile R, Ponziani S, et al. EV20-sss-vc/MMAF, an HER-3 targeting antibody-drug conjugate displays antitumor activity in liver cancer. Oncol Rep 2021;45:776-85.
118. Capone E, Lattanzio R, Gasparri F, et al. EV20/NMS-P945, a novel thienoindole based antibody-drug conjugate targeting HER-3 for solid tumors. Pharmaceutics 2021;13:483.
119. Bourillon L, Bourgier C, Gaborit N, et al. An auristatin-based antibody-drug conjugate targeting HER3 enhances the radiation response in pancreatic cancer. Int J Cancer 2019;145:1838-51.
120. Weng W, Meng T, Pu J, et al. AMT-562, a novel HER3-targeting antibody-drug conjugate, demonstrates a potential to broaden therapeutic opportunities for HER3-expressing tumors. Mol Cancer Ther 2023;22:1013-27.
121. Yonesaka K, Takegawa N, Watanabe S, et al. An HER3-targeting antibody-drug conjugate incorporating a DNA topoisomerase I inhibitor U3-1402 conquers EGFR tyrosine kinase inhibitor-resistant NSCLC. Oncogene 2019;38:1398-409.
122. Koganemaru S, Kuboki Y, Koga Y, et al. U3-1402, a novel HER3-targeting antibody-drug conjugate, for the treatment of colorectal cancer. Mol Cancer Ther 2019;18:2043-50.
123. Haikala HM, Lopez T, Köhler J, et al. EGFR inhibition enhances the cellular uptake and antitumor-activity of the HER3 antibody-drug conjugate HER3-DXd. Cancer Res 2022;82:130-41.
124. Yonesaka K, Tanizaki J, Maenishi O, et al. HER3 augmentation via blockade of EGFR/AKT signaling enhances anticancer activity of HER3-targeting patritumab deruxtecan in EGFR-mutated non-small cell lung cancer. Clin Cancer Res 2022;28:390-403.
125. Haratani K, Yonesaka K, Takamura S, et al. U3-1402 sensitizes HER3-expressing tumors to PD-1 blockade by immune activation. J Clin Invest 2020;130:374-88.
126. Jänne PA, Baik C, Su WC, et al. Efficacy and safety of patritumab deruxtecan (HER3-DXd) in EGFR inhibitor-resistant, EGFR-mutated non-small cell lung cancer. Cancer Discov 2022;12:74-89.
127. Yu HA, Goto Y, Hayashi H, et al. HERTHENA-Lung01, a phase II trial of patritumab deruxtecan (HER3-DXd) in epidermal growth factor receptor-mutated non-small-cell lung cancer after epidermal growth factor receptor tyrosine kinase inhibitor therapy and platinum-based chemotherapy. J Clin Oncol 2023;41:5363-75.
128. Masuda N, Yonemori K, Takahashi S, et al. Abstract PD1-03: single agent activity of U3-1402, a HER3-targeting antibody-drug conjugate, in HER3-overexpressing metastatic breast cancer: updated results of a phase 1/2 trial. Cancer Res 2019;79:PD1-03.
129. Capone E, Lamolinara A, D’Agostino D, et al. EV20-mediated delivery of cytotoxic auristatin MMAF exhibits potent therapeutic efficacy in cutaneous melanoma. J Control Release 2018;277:48-56.
130. Gandullo-Sánchez L, Capone E, Ocaña A, Iacobelli S, Sala G, Pandiella A. HER3 targeting with an antibody-drug conjugate bypasses resistance to anti-HER2 therapies. EMBO Mol Med 2020;12:e11498.
131. Wang M, Hu Y, Yu T, Ma X, Wei X, Wei Y. Pan-HER-targeted approach for cancer therapy: mechanisms, recent advances and clinical prospect. Cancer Lett 2018;439:113-30.
132. Jacobsen HJ, Poulsen TT, Dahlman A, et al. Pan-HER, an antibody mixture simultaneously targeting EGFR, HER2, and HER3, effectively overcomes tumor heterogeneity and plasticity. Clin Cancer Res 2015;21:4110-22.
133. Sampera A, Sánchez-Martín FJ, Arpí O, et al. HER-family ligands promote acquired resistance to trastuzumab in gastric cancer. Mol Cancer Ther 2019;18:2135-45.
134. Hickinson DM, Klinowska T, Speake G, et al. AZD8931, an equipotent, reversible inhibitor of signaling by epidermal growth factor receptor, ERBB2 (HER2), and ERBB3: a unique agent for simultaneous ERBB receptor blockade in cancer. Clin Cancer Res 2010;16:1159-69.
135. Mu Z, Klinowska T, Dong X, et al. AZD8931, an equipotent, reversible inhibitor of signaling by epidermal growth factor receptor (EGFR), HER2, and HER3: preclinical activity in HER2 non-amplified inflammatory breast cancer models. J Exp Clin Cancer Res 2014;33:47.
136. Propper DJ, Gao F, Saunders MP, et al. PANTHER: AZD8931, inhibitor of EGFR, ERBB2 and ERBB3 signalling, combined with FOLFIRI: a Phase I/II study to determine the importance of schedule and activity in colorectal cancer. Br J Cancer 2023;128:245-54.
137. Thomas A, Virdee PS, Eatock M, et al. Dual Erb B Inhibition in Oesophago-gastric Cancer (DEBIOC): a phase I dose escalating safety study and randomised dose expansion of AZD8931 in combination with oxaliplatin and capecitabine chemotherapy in patients with oesophagogastric adenocarcinoma. Eur J Cancer 2020;124:131-41.
138. Ellebaek S, Brix S, Grandal M, et al. Pan-HER-An antibody mixture targeting EGFR, HER2 and HER3 abrogates preformed and ligand-induced EGFR homo- and heterodimers. Int J Cancer 2016;139:2095-105.
139. Rabia E, Garambois V, Hubert J, et al. Anti-tumoral activity of the Pan-HER (Sym013) antibody mixture in gemcitabine-resistant pancreatic cancer models. MAbs 2021;13:1914883.
140. Reddy TP, Choi DS, Anselme AC, et al. Simultaneous targeting of HER family pro-survival signaling with Pan-HER antibody mixture is highly effective in TNBC: a preclinical trial with PDXs. Breast Cancer Res 2020;22:48.
141. Rau A, Janssen N, Kühl L, et al. Triple targeting of HER receptors overcomes heregulin-mediated resistance to EGFR blockade in colorectal cancer. Mol Cancer Ther 2022;21:799-809.
142. Berlin J, Tolcher AW, Ding C, et al. First-in-human trial exploring safety, antitumor activity, and pharmacokinetics of Sym013, a recombinant pan-HER antibody mixture, in advanced epithelial malignancies. Invest New Drugs 2022;40:586-95.
143. Osada T, Hartman ZC, Wei J, et al. Polyfunctional anti-human epidermal growth factor receptor 3 (anti-HER3) antibodies induced by HER3 vaccines have multiple mechanisms of antitumor activity against therapy resistant and triple negative breast cancers. Breast Cancer Res 2018;20:90.
144. Osada T, Morse MA, Hobeika A, et al. Vaccination targeting human HER3 alters the phenotype of infiltrating T cells and responses to immune checkpoint inhibition. Oncoimmunology 2017;6:e1315495.
145. Miller MJ, Foy KC, Overholser JP, Nahta R, Kaumaya PT. HER-3 peptide vaccines/mimics: combined therapy with IGF-1R, HER-2, and HER-1 peptides induces synergistic antitumor effects against breast and pancreatic cancer cells. Oncoimmunology 2014;3:e956012.
146. Kaumaya PT. B-cell epitope peptide cancer vaccines: a new paradigm for combination immunotherapies with novel checkpoint peptide vaccine. Future Oncol 2020;16:1767-91.
147. Lipkowitz S. The role of the ubiquitination-proteasome pathway in breast cancer: ubiquitin mediated degradation of growth factor receptors in the pathogenesis and treatment of cancer. Breast Cancer Res 2003;5:8-15.
148. Fan Q, Wang Q, Cai R, Yuan H, Xu M. The ubiquitin system: orchestrating cellular signals in non-small-cell lung cancer. Cell Mol Biol Lett 2020;25:1.
149. Pinilla-Macua I, Sorkin A. Cbl and Cbl-b independently regulate EGFR through distinct receptor interaction modes. Mol Biol Cell 2023;34:ar134.
150. Luan H, Bailey TA, Clubb RJ, et al. CHIP/STUB1 ubiquitin ligase functions as a negative regulator of ErbB2 by promoting its early post-biosynthesis degradation. Cancers 2021;13:3936.
151. Feng SM, Muraoka-Cook RS, Hunter D, et al. The E3 ubiquitin ligase WWP1 selectively targets HER4 and its proteolytically derived signaling isoforms for degradation. Mol Cell Biol 2009;29:892-906.
152. Qiu XB, Goldberg AL. Nrdp1/FLRF is a ubiquitin ligase promoting ubiquitination and degradation of the epidermal growth factor receptor family member, ErbB3. Proc Natl Acad Sci U S A 2002;99:14843-8.
153. Shi H, Gong H, Cao K, et al. Nrdp1-mediated ErbB3 degradation inhibits glioma cell migration and invasion by reducing cytoplasmic localization of p27(Kip1). J Neurooncol 2015;124:357-64.
154. Yen L, Cao Z, Wu X, et al. Loss of Nrdp1 enhances ErbB2/ErbB3-dependent breast tumor cell growth. Cancer Res 2006;66:11279-86.
155. Huang Z, Choi BK, Mujoo K, et al. The E3 ubiquitin ligase NEDD4 negatively regulates HER3/ErbB3 level and signaling. Oncogene 2015;34:1105-15.
156. Verma N, Müller AK, Kothari C, et al. Targeting of PYK2 synergizes with EGFR antagonists in basal-like TNBC and circumvents HER3-associated resistance via the NEDD4-NDRG1 axis. Cancer Res 2017;77:86-99.
157. Cardoso AP, Banerjee M, Nail AN, Lykoudi A, States JC. miRNA dysregulation is an emerging modulator of genomic instability. Semin Cancer Biol 2021;76:120-31.
158. He B, Zhao Z, Cai Q, et al. miRNA-based biomarkers, therapies, and resistance in Cancer. Int J Biol Sci 2020;16:2628-47.
159. Plantamura I, Cataldo A, Cosentino G, Iorio MV. miR-205 in breast cancer: state of the art. Int J Mol Sci 2020;22:27.
160. Iorio MV, Casalini P, Piovan C, et al. microRNA-205 regulates HER3 in human breast cancer. Cancer Res 2009;69:2195-200.
161. Hao Y, Li J, Zhang H, Guan G, Guo Y. MicroRNA-205 targets HER3 and suppresses the growth, chemosensitivity and metastasis of human nasopharyngeal carcinoma cells. J buon 2020;25:350-6.
162. Scott GK, Goga A, Bhaumik D, Berger CE, Sullivan CS, Benz CC. Coordinate suppression of ERBB2 and ERBB3 by enforced expression of micro-RNA miR-125a or miR-125b. J Biol Chem 2007;282:1479-86.
163. Lyu H, Huang J, He Z, Liu B. Targeting of HER3 with functional cooperative miRNAs enhances therapeutic activity in HER2-overexpressing breast cancer cells. Biol Proced Online 2018;20:16.
164. Zhao Z, Li R, Sha S, Wang Q, Mao W, Liu T. Targeting HER3 with miR-450b-3p suppresses breast cancer cells proliferation. Cancer Biol Ther 2014;15:1404-12.
165. Casamassimi A, Ciccodicola A, Rienzo M. Transcriptional regulation and its misregulation in human diseases. Int J Mol Sci 2023;24:8640.
166. Li Y, Azmi AS, Mohammad RM. Deregulated transcription factors and poor clinical outcomes in cancer patients. Semin Cancer Biol 2022;86:122-34.
167. Lourenco C, Resetca D, Redel C, et al. MYC protein interactors in gene transcription and cancer. Nat Rev Cancer 2021;21:579-91.
168. Suen TC, Hung MC. c-myc reverses neu-induced transformed morphology by transcriptional repression. Mol Cell Biol 1991;11:354-62.
169. Sun C, Hobor S, Bertotti A, et al. Intrinsic resistance to MEK inhibition in KRAS mutant lung and colon cancer through transcriptional induction of ERBB3. Cell Rep 2014;7:86-93.
170. Calissi G, Lam EW, Link W. Therapeutic strategies targeting FOXO transcription factors. Nat Rev Drug Discov 2021;20:21-38.
171. Garrett JT, Olivares MG, Rinehart C, et al. Transcriptional and posttranslational up-regulation of HER3 (ErbB3) compensates for inhibition of the HER2 tyrosine kinase. Proc Natl Acad Sci U S A 2011;108:5021-6.
172. Chakrabarty A, Sánchez V, Kuba MG, Rinehart C, Arteaga CL. Feedback upregulation of HER3 (ErbB3) expression and activity attenuates antitumor effect of PI3K inhibitors. Proc Natl Acad Sci U S A 2012;109:2718-23.
173. Abel EV, Aplin AE. FOXD3 is a mutant B-RAF-regulated inhibitor of G(1)-S progression in melanoma cells. Cancer Res 2010;70:2891-900.
174. Han S, Ren Y, He W, et al. ERK-mediated phosphorylation regulates SOX10 sumoylation and targets expression in mutant BRAF melanoma. Nat Commun 2018;9:28.
175. Abel EV, Basile KJ, Kugel CH 3rd, et al. Melanoma adapts to RAF/MEK inhibitors through FOXD3-mediated upregulation of ERBB3. J Clin Invest 2013;123:2155-68.
176. Raap M, Gierendt L, Kreipe HH, Christgen M. Transcription factor AP-2beta in development, differentiation and tumorigenesis. Int J Cancer 2021;149:1221-7.
177. Zhu CH, Domann FE. Dominant negative interference of transcription factor AP-2 causes inhibition of ErbB-3 expression and suppresses malignant cell growth. Breast Cancer Res Treat 2002;71:47-57.
178. Jacob W, James I, Hasmann M, Weisser M. Clinical development of HER3-targeting monoclonal antibodies: perils and progress. Cancer Treat Rev 2018;68:111-23.
179. Wu Y, Zhang Y, Wang M, et al. Downregulation of HER3 by a novel antisense oligonucleotide, EZN-3920, improves the antitumor activity of EGFR and HER2 tyrosine kinase inhibitors in animal models. Mol Cancer Ther 2013;12:427-37.
180. Sarup J, Jin P, Turin L, et al. Human epidermal growth factor receptor (HER-1:HER-3) Fc-mediated heterodimer has broad antiproliferative activity in vitro and in human tumor xenografts. Mol Cancer Ther 2008;7:3223-36.
181. Yonesaka K, Hirotani K, von Pawel J, et al. Circulating heregulin level is associated with the efficacy of patritumab combined with erlotinib in patients with non-small cell lung cancer. Lung Cancer 2017;105:1-6.
