Nhắm đến HIF-α bởi phức hợp ubiquitin hóa của von Hippel-Lindau qua Hydroxyl hóa prolyl điều hòa bởi O2

American Association for the Advancement of Science (AAAS) - Tập 292 Số 5516 - Trang 468-472 - 2001
Panu Jaakkola1, David R. Mole2,1, Ya‐Min Tian1, Michael Wilson2,1, Adriana Gielbert3, Simon J. Gaskell3, Alex von Kriegsheim4,5, Holger Hebestreit5, Mridul Mukherji6, Christopher J. Schofield6, Patrick H. Maxwell1, Christopher W. Pugh1, Peter J. Ratcliffe1
1The Henry Wellcome Building of Genomic Medicine, University of Oxford, Roosevelt Drive, Oxford OX3 7BN, UK.
2Deanery of Clinical Sciences
3Michael Barber Centre for Mass Spectrometry, Department of Chemistry, University of Manchester Institute of Science and Technology, Manchester M60 1QD, UK.
4Edinburgh Cancer Research Centre
5Glycobiology Institute, University of Oxford, South Parks Road, Oxford OX1 3QU, UK
6The Oxford Centre for Molecular Sciences and The Dyson Perrins Laboratory, University of Oxford, South Parks Road, Oxford OX1 3QY, UK.

Tóm tắt

HIF (Yếu tố cảm ứng thiếu oxy) là một phức hợp phiên mã đóng vai trò trung tâm trong việc điều chỉnh biểu hiện gen bởi oxy. Trong các tế bào giàu oxy và sắt, các tiểu đơn vị HIF-α bị phá hủy nhanh chóng thông qua một cơ chế liên quan đến quá trình ubiquitylation bởi phức hợp enzyme liên kết E3 pVHL, một chất ức chế khối u của von Hippel–Lindau. Quá trình này bị ức chế bởi tình trạng thiếu oxy và quá trình chelate sắt, từ đó cho phép kích hoạt quá trình phiên mã. Nghiên cứu này chỉ ra rằng sự tương tác giữa pVHL ở người và một miền cụ thể của tiểu đơn vị HIF-1α được điều hòa thông qua quá trình hydroxyl hóa một gốc proline (HIF-1α P564) nhờ vào một enzyme mà chúng tôi gọi là HIF-α prolyl-hydroxylase (HIF-PH). Sự cần thiết tuyệt đối của di-oxygene như một đồng chất nền và sắt như một đồng tố chỉ ra rằng HIF-PH hoạt động trực tiếp như một cảm biến oxy tế bào.

Từ khóa

#HIF #hypoxia #prolyl-hydroxylase #von Hippel–Lindau #ubiquitin #oxy #sắt #pVHL #cảm biến oxy #enzyme #hydroxy hóa #gene expression

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Supported by grants from the Wellcome Trust and the Medical Research Council. P.J. is Junior Research Fellow of the Academy of Finland. We thank J. Myllyharju for performing the prolyl-4-hydroxylase assay; K. Brindle R. Hider K. Kivirikko E. Maher and R. Wolfe for advice; N. Pavletich for GST-VCB expression constructs; and E. Gibson for synthesis of 2-oxoglutarate analogs.