GRK5 is widely expressed throughout the body, but with notably high expression in the lung, heart and placenta, with widespread expression at lower levels. [13] In humans, a GRK5 sequence polymorphism at residue 41 (leucine rather than glutamine) that is most common in individuals with African ancestry leads to elevated GRK5-mediated ...

2024年12月25日 · GRK5 (G Protein-Coupled Receptor Kinase 5) is a Protein Coding gene. Diseases associated with GRK5 include Atrial Fibrillation and Heart Disease. Among its related pathways are GPCR downstream signalling and Myometrial relaxation and contraction pathways.

2024年1月15日 · G protein-coupled receptor kinase 5 (GRK5) is an important drug development target for heart failure, cardiac hypertrophy, and cancer. We have designed and developed a new class of highly selective, potent, and non-covalent GRK5 inhibitors. One of the inhibitors displayed GRK5 IC 50 value of 10 nM and exhibited >100,000-fold selectivity over GRK2.

2020年12月14日 · To delineate how GRKs are regulated by calcium, we set out to determine the molecular basis for GRK5 interaction with Ca 2+ /CaM. Through structural, computational, and functional approaches, we uncover the stepwise mechanism of GRK5 activation by CaM and highlight key elements of GRK5 critical for CaM-mediated regulation.

2024年8月23日 · Background: Our prior genome-wide association study of thrombin-induced platelet aggregation identified a G protein-coupled receptor kinase 5 (GRK5) noncoding variant (rs10886430-G) that is strongly associated with increased platelet reactivity to thrombin. This variant predisposes to increased risk of stroke, pulmonary embolism, and venous ...

GRK5 is localized in the centrosome and regulates microtubule nucleation and normal cell cycle progression. GRK5 is a transcriptional modifier of a subset of Galphaq-downregulated genes, acting in opposition to the pathological effects of Galphaq …

2017年1月1日 · In humans, the Grk5 gene is located on chromosome 10q26.11 (Aken et al. 2016). The gene contains 16 exons and encodes a 590 amino acid–long protein with a molecular weight of ~67.7 kDa (Kunapuli and Benovic 1993). GRK5 exhibits high homology to the Drosophila GPRK-2 and human IT11 proteins (Kunapuli and Benovic 1993).

本研究首次探讨了grk5对血管新生(angiogenesis)的影响.血管新生主要发生在生理性发育及成体创伤愈合,女性月经周期等过程,受到精密的促血管新生因子和抑制因子的平衡调控,一旦失衡则会导致多种疾病.由于在肿瘤生成,转移及很多疾病中的重要影响,血管新生在病理 ...

2022年1月7日 · G protein-coupled receptor kinase 5 (GRK5) is upregulated in failing human myocardium and promotes maladaptive cardiac hypertrophy in animal models. However, the role of GRK5 in ischemic heart disease is still unknown.

2024年2月12日 · Clinical resource with information about GRK5, A genome-wide association study identifies GRK5 and RASGRP1 as type 2 diabetes loci in Chinese Hans., Novel genetic loci identified for the pathophysiology of childhood obesity …