Target intelligence / Profile preview

Microtubule-associated protein tau (cis-pT231 conformation) (None)

Target
None
Molecular classification
Microtubule-associated protein, Intrinsically disordered protein
01

Overview

Microtubule-associated protein tau (MAPT) is a neuronal protein that stabilizes microtubules. The cis-pT231 conformation, specifically tau phosphorylated at threonine 231 adopting a *cis* conformation at the peptide bond preceding proline, is implicated as an early driver of neurodegeneration and a potential therapeutic target for Alzheimer's disease and other tauopathies. This conformation impairs normal dephosphorylation processes, leading to its accumulation and subsequent pathological effects.

Other names
MAPT (cis-pT231)cis-pT231-tauPhosphorylated tau at T231 (cis conformation)
02

Mechanism of action

Inhibition of tau phosphorylation or aggregation, promotion of tau dephosphorylation, or clearance of pathological tau species.

03

Biological functions

Microtubule stabilizationRegulation of cytoskeletal dynamicsAxonal transportmRNA translation regulation
04

Disease associations

Alzheimer's diseaseTauopathiesFrontotemporal dementiaProgressive supranuclear palsyNeurodegenerative disease
05

Safety considerations

Off-target effects of kinase inhibitorsPotential for exacerbating other tau isoforms or phosphorylation sites if not selectiveBlood-brain barrier penetration for therapeutic antibodies or large molecules
06

Biomarkers

cis-pT231-tau levels in cerebrospinal fluid (CSF)cis-pT231-tau levels in plasmaPET imaging ligands targeting cis-pT231 tau conformation

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