Hypoxia-inducible factor prolyl hydroxylase inhibitors (HIF-PHIs) are a novel class of oral medications developed for the treatment of anemia in chronic kidney disease (CKD).

促红细胞生成素（EPO）的生成是由低氧诱导因子（HIF）调节，而HIF又是被脯氨酰羟化酶（PH）所调节。 在常氧状态下，HIF-PH的活动将会快速降解HIF；而在低氧条件下，HIF-PH的活动被抑制，使得1）HIF能够积累并刺激内源EPO的生成；2）上调运铁蛋白受体的表达；3）增加红细胞对铁的吸收；4）促进富含血红蛋白的红细胞成熟 [3]。 HIF-PH抑制剂的原理是通过抑制脯氨酰羟化酶（PH）的作用，从而固定肾脏和肝脏中的HIF，增加内源促红细胞生成素的生成 [3] …

缺氧诱导因子(HIF) 是一种关键转录因子,主要参与细胞调节和氧输送效率。 其初步状态包括组成性表达的核结合β 亚基和胞浆α亚基的三种亚型(HIF-1α、HIF-2α 和HIF-3α)。 HIF-1α 和HIF-2 α是低氧防御机制的主要调节因子, 通过刺激多种基因增强氧输送。

The hypoxia-inducible factor (HIF)–prolyl hydroxylase domain (PHD) pathway regulates cellular responses to hypoxia and is involved in multiple diseases, including anemia, polycythemia, ischemic diseases, pulmonary arterial hypertension, and cancer. 10 HIF-PHD inhibitors (HIF-PHIs) are a new class of drugs that activate HIF transcription ...

Hypoxia-inducible factor (HIF) prolyl hydroxylase (PH) enzyme inhibitors are a new class of agents for the treatment of anemia in CKD. These agents work by stabilizing the HIF complex and stimulating endogenous erythropoietin production even in patients with end-stage kidney disease.

2017年6月1日 · Hypoxia-inducible factor (HIF) prolyl hydroxylase (PH) enzyme inhibitors are a new class of agents for the treatment of anemia in CKD. These agents work by stabilizing the HIF complex and stimulating endogenous erythropoietin production even in patients with end-stage kidney disease. HIF-PH inhibitors improve iron mobilization to the bone marrow.

In this review, I describe the process of molecular cloning of HIF and HIF-PH, which explains the induction of EPO expression by hypoxia; the development of HIF-PH inhibitors (HIF-PHIs) that artificially activate HIF by inhibiting HIF-PH; medical interventions that utilize HIF-PHIs; and the implications and significance of these interventions ...

Introduction: The hypoxia-inducible factor prolyl hydroxylase (HIF-PH) pathway is responsible for regulating the biosynthesis of erythropoietin (EPO) and maintaining iron homeostasis. Investigational drugs that target the HIF-PH pathway are promising alternatives for treating anemia in Chronic Kidney Disease (CKD).

2024年3月8日 · 低氧诱导因子（HIF） 是一种参与细胞调控和氧气输送效率的关键转录因子，由调节亚基HIF-α和结构亚基HIF-β构成，当两个亚基形成复合物时，能够激活下游信号通路并诱导靶基因表达，例如上调促红细胞生成素（EPO）、EPO受体、转铁蛋白、转铁蛋白受体等因子的 ...

血液中には低酸素誘導因子（HIF：Hypoxia Inducible Factor）と呼ばれる酸素濃度の低下を感知する細胞内の酸素センサー的役割を果たしている物質があるが、慢性腎臓病（CKD）の病態では、このHIFが関わるEPO産生誘導の仕組みがうまく働いていないため、EPO産生が低下する。 HIFは低酸素誘導因子ｰプロリン水酸化酵素（HIF-PH：Hypoxia Inducible...