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The anti-aging membrane protein αKlotho is highly expressed in the kidney, and deletion of the Klotho gene creates a phenotype of chronic kidney disease in mice. Klotho functions as a co-receptor for fibroblast growth factor 23 signaling, whereas its shed extracellular domain, sKlotho, carries glycosidase activity and regulates renal health. In the present study, the structure-function relationships and posttranslational modifications (PTMs) of sKlotho expressed in stable Chinese Hamster ovary (CHO) cells and transient human embryonic kidney (HEK) 293 cells were explored to guide future design and understanding of Klotho-based therapeutics [1]. A combination of mass spectrometry (MS)-based methods, including intact protein analysis, released 2-AB labeled N-linked oligosaccharide analysis with glycosidase treatments, and glycopeptide-mapping by LC-MS/MS, were carried out to characterize and localize the PTMs in CHO and HEK expressed sKlotho. ESI MS analysis of intact sKlotho indicated the presence of core-1 O-glycosylation with partial sialylation in both CHO and HEK materials. The combination of released N-glycan analysis with beta-N-acetylhexosaminidase treatment and tryptic glycopeptide mapping via LC-MS/MS revealed that HEK-sKlotho is uniquely modified with a rare N-glycan antennal structure consisting of GalNAc-beta1-4GlcNAc (LacdiNAc) at multiple N-linked sites, with some structures being additionally sulfated and fucosylated. The observed diagnostic oxonium ions generated by higher-energy dissociation (HCD) clearly distinguished N-glycans with and without LacdiNAc structural determinants. CHO cells cannot produce LacdiNAc structures; thus, CHO-derived sKlotho contained normal sialylated complex-type N-glycans, which resulted in slow clearance in vivo. However, HEK-derived sKlotho had an unusually short half-life in rats presumably due to abundant terminal LacdiNAc moieties. [1] Zhong et al. J. Biol. Chem. (2020) 295(10) 3115-3133.

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Mellisa Ly

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Team Members

Mellisa Ly profile image

Mellisa Ly

Pfizer, Inc.

Presenter
Mellisa Ly
Pfizer, Inc.
Email: mellisa.ly@pfizer.com
Eric Sousa profile image

Eric Sousa

Pfizer, Inc.

Co-Author
Eric Sousa
Pfizer, Inc.
Email: Eric.Sousa@pfizer.com
Jason Rouse profile image

Jason Rouse

Pfizer, Inc.

Co-Author
Jason Rouse
Pfizer, Inc.
Email: jason.rouse@pfizer.com
Justin Cohen profile image

Justin Cohen

Pfizer, Inc.

Co-Author
Justin Cohen
Pfizer, Inc.
Email: Justin.Cohen@pfizer.com
Kaffa Cote profile image

Kaffa Cote

Pfizer, Inc.

Co-Author
Kaffa Cote
Pfizer, Inc.
Email: Kaffa.Cote@pfizer.com
Xiaotian Zhong profile image

Xiaotian Zhong

Pfizer, Inc.

Co-Author
Xiaotian Zhong
Pfizer, Inc.
Email: xiaotian.zhong@pfizer.com
Yan Zhang profile image

Yan Zhang

Pfizer, Inc.

Co-Author
Yan Zhang
Pfizer, Inc.
Email: Yan.Zhang4@pfizer.com