title: Endothelial epsins as regulators and potential therapeutic targets of tumor angiogenesis.
abstract: VEGF-driven tumor angiogenesis has been validated as a central target in several tumor types deserving of continuous and further considerations to improve the efficacy and selectivity of the current therapeutic paradigms. Epsins, a family of endocytic clathrin adaptors, have been implicated in regulating endothelial cell VEGFR2 signaling, where its inactivation leads to nonproductive leaky neo-angiogenesis and, therefore, impedes tumor development and progression. Targeting endothelial epsins is of special significance due to its lack of affecting other angiogenic-signaling pathways or disrupting normal quiescent vessels, suggesting a selective modulation of tumor angiogenesis. This review highlights seminal findings on the critical role of endothelial epsins in tumor angiogenesis and their underlying molecular events, as well as strategies to prohibit the normal function of endogenous endothelial epsins that capitalize on these newly understood mechanisms.
authors: Vascular Biology Program, Karp Family Research Laboratory, Department of Surgery, Boston Children's Hospital, Harvard Medical School, 12.214, 300 Longwood Avenue, Boston, MA, 02115, USA.
authors: Kai
authors: K
authors: Song
authors: Vascular Biology Program, Karp Family Research Laboratory, Department of Surgery, Boston Children's Hospital, Harvard Medical School, 12.214, 300 Longwood Avenue, Boston, MA, 02115, USA.
authors: Hao
authors: H
authors: Wu
authors: Vascular Biology Program, Karp Family Research Laboratory, Department of Surgery, Boston Children's Hospital, Harvard Medical School, 12.214, 300 Longwood Avenue, Boston, MA, 02115, USA.
authors: H N Ashiqur
authors: HN
authors: Rahman
authors: Vascular Biology Program, Karp Family Research Laboratory, Department of Surgery, Boston Children's Hospital, Harvard Medical School, 12.214, 300 Longwood Avenue, Boston, MA, 02115, USA.
authors: Yunzhou
authors: Y
authors: Dong
authors: Vascular Biology Program, Karp Family Research Laboratory, Department of Surgery, Boston Children's Hospital, Harvard Medical School, 12.214, 300 Longwood Avenue, Boston, MA, 02115, USA.
authors: Aiyun
authors: A
authors: Wen
authors: Vascular Biology Program, Karp Family Research Laboratory, Department of Surgery, Boston Children's Hospital, Harvard Medical School, 12.214, 300 Longwood Avenue, Boston, MA, 02115, USA.
authors: Megan L
authors: ML
authors: Brophy
authors: Vascular Biology Program, Karp Family Research Laboratory, Department of Surgery, Boston Children's Hospital, Harvard Medical School, 12.214, 300 Longwood Avenue, Boston, MA, 02115, USA.
authors: Scott
authors: S
authors: Wong
authors: Vascular Biology Program, Karp Family Research Laboratory, Department of Surgery, Boston Children's Hospital, Harvard Medical School, 12.214, 300 Longwood Avenue, Boston, MA, 02115, USA.
authors: Sukyoung
authors: S
authors: Kwak
authors: Vascular Biology Program, Karp Family Research Laboratory, Department of Surgery, Boston Children's Hospital, Harvard Medical School, 12.214, 300 Longwood Avenue, Boston, MA, 02115, USA.
authors: Diane R
authors: DR
authors: Bielenberg
authors: Vascular Biology Program, Karp Family Research Laboratory, Department of Surgery, Boston Children's Hospital, Harvard Medical School, 12.214, 300 Longwood Avenue, Boston, MA, 02115, USA. hong.chen@childrens.harvard.edu.
authors: Hong
authors: 0000-0002-1906-6611
authors: H
authors: Chen
mesh_terms: D033942:Adaptor Proteins, Vesicular Transport / Q000378:metabolism*; D020533:Angiogenesis Inhibitors / Q000494:pharmacology*; D000818:Animals; D055808:Drug Discovery; D004727:Endothelium / Q000187:drug effects / Q000378:metabolism / Q000473:pathology; D006801:Humans; D058990:Molecular Targeted Therapy; D009369:Neoplasms / Q000098:blood supply* / Q000378:metabolism / Q000473:pathology; D009389:Neovascularization, Pathologic / Q000188:drug therapy* / Q000378:metabolism* / Q000473:pathology; D015398:Signal Transduction / Q000187:drug effects; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000378:metabolism*
chemical_list: D033942:Adaptor Proteins, Vesicular Transport; D020533:Angiogenesis Inhibitors; C114154:epsin; D040301:Vascular Endothelial Growth Factor Receptor-2
keywords: Endocytosis; Epsins; Signaling; Target; Tumor angiogenesis; VEGFR2