ArticleStructure (London, England : 1993)2007
Crystal Structures of the p21-activated kinases PAK4, PAK5, and PAK6 reveal catalytic domain plasticity of active group II PAKs.
Article in Structure (London, England : 1993), 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 54 papers.
What it found
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Who cites it
54 citing papers in PubMed, 114 citations in OpenAlex.
- Single-cell transcriptomics identifies a p21-activated kinase important for survival of the zoonotic parasiteiScience · 2026Article
- Structural basis for a p21-activated kinase 4 and nicotinamide phosphoribosyltransferase dual inhibitor.Acta crystallographica. Section D, Structural biology · 2026Article
- Facile Cobalt-supported Zeolite 4 A as ecofriendly catalyst to prepare 2-Furyl- hydrazine-1-carbothioamides and 1,2,4 Triazole-3-thiones with anticancer investigation.Scientific reports · 2026Article
- PAK4 in metabolic diseases: regulation by nutrient signals and therapeutic implications.Experimental & molecular medicine · 2026Review
- Identification of chrysin derivatives anticancer potential in MCF7 cells: biological insights and in silico evaluation.Future medicinal chemistry · 2025Article
- Biochemical Changes in Prostate Cancer: FMNL1 and PAK1 in Plasma and Urine.Current issues in molecular biology · 2025Article
- Review
- Review
- The Inhibitory Mechanism of 7Molecules (Basel, Switzerland) · 2023Article
- Identification of a Class of WNK Isoform-Specific Inhibitors Through High-Throughput Screening.Drug design, development and therapy · 2023Article
- The significance of PAK4 in signaling and clinicopathology: A review.Open life sciences · 2022Review
- Recent advances on development of p21-activated kinase 4 inhibitors as anti-tumor agents.Frontiers in pharmacology · 2022Review
- Over-expression of miR-193a-3p regulates the apoptosis of colorectal cancer cells by targeting PAK3.American journal of translational research · 2022Article
- An allosteric regulation mechanism of Arabidopsis Serine/Threonine kinase 1 (SIK1) through phosphorylation.Computational and structural biotechnology journal · 2022Article
- Osmosensing by WNK Kinases.Molecular biology of the cell · 2021Article
- Reprogramming an energetic AKT-PAK5 axis boosts axon energy supply and facilitates neuron survival and regeneration after injury and ischemia.Current biology : CB · 2021Article
- Activation of RSK by phosphomimetic substitution in the activation loop is prevented by structural constraints.Scientific reports · 2020Article
- Curcumin and Gastric Cancer: a Review on Mechanisms of Action.Journal of gastrointestinal cancer · 2019Review
- Solution structures and biophysical analysis of full-length group A PAKs reveal they are monomeric and auto-inhibited inThe Biochemical journal · 2019Article
- Cyclic AMP-dependent protein kinase A and EPAC mediate VIP and secretin stimulation of PAK4 and activation of NaAmerican journal of physiology. Gastrointestinal and liver physiology · 2019Article
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 2 countries.
Funding
Abstract
p21-activated kinases have been classified into two groups based on their domain architecture. Group II PAKs (PAK4-6) regulate a wide variety of cellular functions, and PAK deregulation has been linked to tumor development. Structural comparison of five high-resolution structures comprising all active, monophosphorylated group II catalytic domains revealed a surprising degree of domain plasticity, including a number of catalytically productive and nonproductive conformers. Rearrangements of helix alphaC, a key regulatory element of kinase function, resulted in an additional helical turn at the alphaC N terminus and a distortion of its C terminus, a movement hitherto unseen in protein kinases. The observed structural changes led to the formation of interactions between conserved residues that structurally link the glycine-rich loop, alphaC, and the activation segment and firmly anchor alphaC in an active conformation. Inhibitor screening identified six potent PAK inhibitors from which a tri-substituted purine inhibitor was cocrystallized with PAK4 and PAK5.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.