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Last update 08 May 2025

CDK5RAP2

Last update 08 May 2025

Basic Info

Synonyms

C48, CDK5 activator-binding protein C48, CDK5 regulatory subunit associated protein 2

+ [7]

Introduction

Potential regulator of CDK5 activity via its interaction with CDK5R1. Negative regulator of centriole disengagement (licensing) which maintains centriole engagement and cohesion. Involved in regulation of mitotic spindle orientation (By similarity). Plays a role in the spindle checkpoint activation by acting as a transcriptional regulator of both BUBR1 and MAD2 promoter. Together with EB1/MAPRE1, may promote microtubule polymerization, bundle formation, growth and dynamics at the plus ends. Regulates centrosomal maturation by recruitment of the gamma-tubulin ring complex (gamma-TuRC) onto centrosomes (PubMed:26485573). In complex with PDE4DIP isoform 13/MMG8/SMYLE, MAPRE1 and AKAP9, contributes to microtubules nucleation and extension from the centrosome to the cell periphery (PubMed:29162697). Required for the recruitment of AKAP9 to centrosomes (PubMed:29162697). Plays a role in neurogenesis (By similarity).

Drugs associated with CDK5RAP2

CN118165049

Patent Mining

Target

CDK5RAP2 x HHEX

Mechanism

CDK5RAP2 inhibitors [+1]

Active Org.

Henan University of Traditional Chinese Medicine

Originator Org.

Henan University of Traditional Chinese Medicine

Active Indication

Allergic asthma

Inactive Indication-

Drug Highest PhaseDiscovery

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with CDK5RAP2

100 Translational Medicine associated with CDK5RAP2

0 Patents (Medical) associated with CDK5RAP2

228

Literatures (Medical) associated with CDK5RAP2

01 Jun 2025·Journal of Molecular Biology

Cryo-EM of AKAP350/AKAP9 Reveals Fibrillar Clusters and an Association With DNA

Article

Author: Raught, Brian ; Liu, Alex C H ; Keszei, Alexander F A ; Goldenring, James R ; Dai, David L ; Zhang, Xu ; Kolobova, Elena ; St-Germain, Jonathan ; Mazhab-Jafari, Mohammad T ; Hasan, S M Naimul

AKAP350 is a massive human scaffolding protein, encoded by AKAP9, that anchors protein kinase A (PKA) to the Golgi apparatus and the centrosome. AKAP9 is among the most frequently mutated genes in various human cancers, and dysregulation of AKAP350 function is strongly linked to metastasis. However, the molecular mechanisms underlying these disease processes remain poorly understood due to the challenges of studying its large and unstructured protein sequence. To learn more about AKAP350 basic function and architecture, we successfully expressed and purified full-length AKAP350 from human cells. Its functional state was validated based on the scaffolding protein's ability to pulldown endogenous CEP170 and CDK5RAP2, and to co-purify with endogenous PKA. Cryo-electron microscopy (cryo-EM) revealed that AKAP350 appears as polydisperse clusters ∼50 nm in diameter, characterized by fibrous outgrowths. Surprisingly, these fibers reconstructed into double-stranded DNA. DNA sequencing and mass spectrometry confirmed that AKAP350 co-purified with human DNA and endogenous DNA-binding proteins, including nuclear factor 1B (NFIB) and nucleolin (NCL). Interestingly, the pull-down of NFIB and NCL, but not the centrosomal proteins CEP290, CDK5RAP2, or CEP170, was reduced in the presence of DNase-I, suggesting that AKAP350's interaction with these DNA-binding proteins is mediated by DNA. Furthermore, cryo-electron tomography (cryo-ET) revealed that AKAP350 fibrillar clusters form a three-dimensional network of entangled filaments, a structure significantly altered by DNase-I treatment. Overall, our findings suggest AKAP350 forms fibrillar clusters that serve as nucleoprotein scaffolding complexes in human cells.

01 Jan 2025·Combinatorial Chemistry & High Throughput Screening

Acupuncture Increased the Number of Retrieved Oocytes in a Mouse Model of POR: The Involvement of DNA Methylation in the Oocytes

Article

Author: Zhu, Xinyun ; Yuan, Rongli ; Li, Zimeng ; Wu, Jie ; Xiong, Yueheng ; Wang, Mengjing ; Wang, Tianyu ; Chen, Xin ; Li, Zhi

Background:Poor ovarian response (POR) reduces the success rate of in vitro fertilization mainly because of fewer oocytes retrieved. Acupuncture (Ac) therapy can improve the number of retrieved oocytes in the controlled ovarian stimulation program. The role of Ac in the corresponding epigenetic mechanism of POR has not been studied.Objective:This study was conducted to determine the effect of Ac on the number of retrieved oocytes and its role in DNA methylation in a mouse model of POR.Methods::Forty C57BL/6N female mice with normal estrous cycles were randomly classified into 4 groups of 10 each: control (Con) group, Ac-Con group, POR group, and Ac-POR group. Mice in POR and Ac-POR groups received a gastric gavage of Tripterygium wilfordii polyglycoside suspension of 50 mg/kg-1 once a day for 14 consecutive days. Ac was applied at “Shenting” (DU 24), “Guanyuan” (CV 4), “Zusanli” (ST 36), and “Shenshu” (BL 23) in the Ac-POR group for 10 min per session, once a day for 14 consecutive days. All four groups were stimulated with pregnant mare serum gonadotropin and human chorionic gonadotropin, and the number of retrieved oocytes and proportion of mature oocytes were recorded. The DNA methylation level in a single mouse oocyte in each group was analyzed using single-cell genome-wide bisulfite sequencing (scBSseq), and key pathways were identified using GO and KEGG enrichment analyses.Results:A dissecting microscope revealed that the Ac therapy improved the number of retrieved oocytes compared with the POR group (p < 0.05). ScBS-seq showed that there was no significant change in global DNA methylation levels between the POR model and control group mice. However, differences were primarily observed in the differentially methylated regions (DMRs) of each chromosome, and Ac decreased global DNA methylation. DMR analysis identified 13 genes that may be associated with Ac treatment. Cdk5rap2 and Igf1r, which mediate germ cell apoptosis, growth, and development, maybe most closely related to the Ac treatment of POR. KEGG analysis revealed that differentially expressed genes were mainly enriched in Wnt, GnRH, and calcium signaling pathways. The genes were closely related to the regulation of POR via Ac.Conclusion:The results suggest that DNA methylation in oocytes is related to the development of POR and that the role of Ac in affecting DNA methylation in oocytes is associated with the Wnt, GnRH, and calcium signaling pathways as well as Cdk5rap2 and Igf1r in POR mice.

01 Jan 2025·Clinical Biochemistry

Serological proteomic profiling uncovered CDK5RAP2 as a novel marker in benign prostatic hyperplasia

Article

Author: Fan, Junli ; Wang, Jiajun ; Chen, Lili ; Pan, Yunbao ; Xie, Huan ; Li, Yirong ; Liu, Tao ; Li, Xinran

BACKGROUNDBenign prostatic hyperplasia (BPH) affects approximately half of men over the age of 50. Early detection and timely treatment facilitate disease intervention and achieve a better clinical outcome. However, current clinical methods, such as prostate specific antigen (PSA), lack the sensitivity to accurately distinguish between BPH and prostate cancer (PCa). Thus, optimal serum markers are warranted to complement existing diagnostic tests.METHODSIn this study, we recruited 1987 BPH patients and characterized their clinical features. To explore BPH proteomic alterations, a data independent acquisition-based mass spectrometry proteomics approach was adopted for 66 serum samples from healthy males (n = 22), patients with BPH (n = 22) and prostate cancer (n = 22). Bioinformatic evaluations were performed for proteomic profiling and candidate selection. In addition, a promising candidate was further validated with ELISA assay.RESULTSOur findings revealed that the level of free PSA correlated with prostate volume. 7.95 % of BPH patients had a PSA value greater than 10 ng/mL, with elevated free PSA, prostate volume, PSA density, and decreased free to total PSA ratio. Mass spectrometry-based serum profiling demonstrated distinct differences between BPH and PCa. CDK5RAP2 was weighted most important in BPH patients' serum and achieved an area under the receiver operating characteristic curve of 0.900 in distinguishing BPH and PCa, which was further validated by publicly-available mRNA microarray analysis and cellular phenotype evaluation.CONCLUSIONOur comprehensive analysis systematically explored BPH serum characteristics, proteomic profiles, and identified novel serum markers that may contribute to the understanding of BPH and facilitate early diagnosis and intervention.

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