#303 - A breakthrough in Alzheimer's disease: the promising potential of klotho for brain health, cognitive decline, and as a therapeutic tool for Alzheimer's disease | Dena Dubal, M.D., Ph.D.

May 27, 2024 Episode Page ↗
Overview

Dr. Dena Dubal, a UCSF neurologist and neuroscientist, discusses klotho, a longevity factor linked to brain resilience. She details its decline with age, its increase with exercise, and its profound impact on cognitive function in animal models, including potential for Alzheimer's and Parkinson's treatment.

At a Glance
7 Insights
2h 5m Duration
16 Topics
6 Concepts

Deep Dive Analysis

Introduction to Dr. Dina Dubal and Klotho

Dr. Dubal's Path to Studying Brain Aging and Klotho

Serendipitous Discovery and Early Findings of Klotho

Biological Structure and Forms of Klotho Protein

Factors Influencing Klotho Levels and Their Daily/Lifespan Variation

Klotho's Unexpected Cognitive Benefits in Healthy and Alzheimer's Mouse Models

Investigating How Peripheral Klotho Impacts Brain Function

The Role of Platelet Factor 4 (PF4) as a Klotho Messenger

PF4's Sufficiency but Not Necessity for Klotho's Cognitive Effects

Klotho's Impact on Cognitive Deficits in Parkinson's Mouse Models

Cognitive Enhancement in Aging Non-Human Primates with Klotho

Human Genetic Variant KL-VS and Its Impact on Klotho Levels and Cognition

KL-VS Interaction with APOE4 and Broader Health Implications

Association of Low Klotho Levels with Increased Mortality and Organ Health

Challenges and Future of Measuring Klotho Levels

Future Therapeutic Potential and Funding for Klotho Research

Klotho (protein/gene)

Klotho is a longevity factor accidentally discovered in 1997. Its disruption in mice causes premature aging and a shortened lifespan, while its overexpression can extend lifespan by about 30%. It is a large transmembrane protein predominantly made in the kidney and choroid plexus.

Soluble Klotho (Klotho hormone)

This is the majority of the Klotho protein that is cleaved from the cell membrane by enzymes (ADAM10, ADAM17) and released into the blood or cerebrospinal fluid (CSF). It acts as a hormonal factor, circulating throughout the body and influencing various organs, including the brain.

BDNF (Brain-Derived Neurotrophic Factor)

BDNF is a trophic factor in the brain that is strongly associated with positive brain health. It is known to improve neuronal function and is increased by interventions like exercise and intermittent fasting.

Brain Resilience

Brain resilience refers to the ability of the brain to maintain normal cognitive function despite the presence of age-related or disease-related pathologies, such as amyloid beta and tau in Alzheimer's disease. Klotho appears to confer this resilience by preserving synaptic connections.

Platelet Factor 4 (PF4)

PF4 is a chemokine released by activated platelets, which can cross the blood-brain barrier and enhance cognition by acting on GluN2B subunits of NMDA receptors. It is increased by Klotho, exercise, and factors found in young blood, suggesting it acts as a messenger for brain health.

KL-VS (Klotho genetic variant)

KL-VS is a genetic variant (two single nucleotide polymorphisms) in the Klotho gene. Carrying one copy (heterozygous) leads to approximately 15-20% higher circulating Klotho levels and is associated with better cognition and protection against Alzheimer's disease risk, especially in APOE4 carriers. Homozygosity for KL-VS is rare and associated with lower Klotho levels and shorter lifespans.

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What is Klotho and how was it discovered?

Klotho is a longevity factor accidentally discovered in 1997 by Makoto Kuroo while studying hypertension in mice. He found that disrupting the Klotho gene led to premature aging, while overexpressing it extended lifespan.

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How does Klotho circulate in the body and what influences its levels?

Klotho is primarily produced in the kidney and choroid plexus, and its extracellular portion is cleaved to form a soluble, hormonal version that circulates in the blood and CSF. Levels are highest at birth, decline with age, show a diurnal rhythm (highest in the morning), and are influenced by factors like chronic stress (decreasing levels) and exercise (increasing levels).

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How does Klotho enhance cognition in the brain?

Klotho enhances cognition by increasing the presence of the GluN2B subunit at neuronal synapses, which is a key component of NMDA receptors. This leads to more efficient connections between neurons and improved memory formation, or synaptic plasticity.

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Does Klotho cross the blood-brain barrier?

No, Klotho does not cross the blood-brain barrier. Despite this, peripheral injections of Klotho still lead to cognitive enhancement, suggesting it acts through a messenger system in the blood that then enters the brain.

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What is Platelet Factor 4 (PF4) and how does it relate to Klotho?

Platelet Factor 4 (PF4) is a chemokine released by activated platelets. Research suggests Klotho modestly activates platelets to release PF4, which then travels to the brain and enhances cognition, acting as a messenger for Klotho's effects.

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Is PF4 necessary for Klotho's cognitive benefits?

While PF4 is sufficient to recapitulate Klotho-mediated cognitive enhancement, experiments in PF4 knockout mice showed that Klotho still enhanced cognition to the same extent in their absence, indicating that PF4 is not necessary and other messengers likely exist.

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Can Klotho help with neurodegenerative diseases like Parkinson's?

In mouse models of Parkinson's disease, Klotho treatment significantly improved cognitive abilities (nearly normalized them) but did not show any effect on motor dysfunctions. This suggests a potential role for Klotho in addressing the cognitive deficits associated with Parkinson's.

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What did the primate studies reveal about Klotho's effects?

Studies in aging Rhesus macaques showed that a single, low, physiologic dose of Klotho enhanced cognition within four hours, and this improvement lasted for at least three weeks. The effect was particularly pronounced in tasks requiring high memory load, while supraphysiologic doses did not provide additional benefit.

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What is the KL-VS genetic variant and how does it affect Klotho levels and cognition?

The KL-VS genetic variant involves two single nucleotide polymorphisms in the Klotho gene. Individuals carrying one copy (heterozygotes) have about 15-20% higher circulating Klotho levels and are associated with better cognitive performance in normal aging.

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How does KL-VS interact with APOE4 in Alzheimer's disease risk?

A large meta-analysis found that KL-VS heterozygosity appears to abrogate the toxicity of APOE4. APOE4 carriers who also carry the KL-VS variant have a decreased risk for developing Alzheimer's disease, reduced conversion from MCI to AD, and lower Alzheimer's biomarkers, regardless of whether they have one or two copies of APOE4.

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Are there any negative health consequences of the KL-VS variant?

While KL-VS heterozygosity is generally associated with protection against stroke, cardiovascular, and metabolic risks, it has been linked to a poorer prognosis in BRCA1 carriers with breast cancer, indicating it is not universally beneficial.

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What is the relationship between Klotho levels and overall mortality?

Large-scale human studies, such as the NHANES study, have shown a strong association between lower circulating Klotho levels and increased all-cause mortality. Individuals with Klotho levels below a certain threshold (e.g., <666 pg/mL) had a 30% higher mortality risk over five years, primarily due to cancer and cardiovascular disease.

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How should Klotho levels be measured in humans?

Due to Klotho's diurnal rhythm, it is recommended to measure levels in the morning, in a fasting state, similar to cholesterol tests, to obtain the most accurate and consistent results. A standardized clinical assay for Klotho is currently needed.

1. Engage in Chronic Exercise

Regularly engage in chronic exercise, as it is a robust intervention shown to increase clotho levels by about 30% after 12 weeks, potentially enhancing brain health and longevity.

2. Manage Chronic Stress

Actively manage chronic stress, as high levels of stress are associated with lower clotho levels and shorter telomeres, suggesting a negative impact on aging markers.

3. Consider Rapamycin

Consider rapamycin as a potential intervention, as studies in mice show it can increase clotho levels, contributing to the convergence of biology for longevity factors.

4. Monitor Clotho Levels

Consider getting your clotho levels checked as a potential diagnostic biomarker, as lower levels are associated with increased mortality risk from diseases like cancer and cardiovascular disease.

5. Standardize Clotho Measurement

If getting clotho levels checked, ensure the blood draw is done in a morning fasting state to minimize diurnal variation and provide a more accurate and consistent measurement.

6. Pursue Big, Important Science

When conducting scientific research, aim for projects that are ‘big and important, and not incremental or mediocre,’ because both types of work will take the same amount of time.

7. Fund Risky, High-Upside Science

Philanthropists should fund scientific endeavors that are too risky for traditional funding but possess significant biologic plausibility and potential for transformative, game-changing impact.

Sometimes experiments will show you those differences. And then the next time you do it, they don't. Someone who runs the water maze is wearing a new cologne and the mice get stressed out. They don't always repeat and are not always replicable. This is a case that it was amazing, but was it going to replicate? Was it going to be true in different cognitive tasks? What would happen in an aging mouse? All of these questions opened up and we iterated and we did experiment after experiment and the data held strong in mice that clotho overexpression really enhanced their cognition in young mice, in aging mice, in mice that modeled Alzheimer's disease, and also in mice in a publication that's in peer review now, but also in mice that model Parkinson's disease, that overexpression of clotho enhanced cognition. It is really a remarkable finding. I think it's maybe one of the most important findings in my professional career.

Dina Dubal

I would go one step further. I feel like it's one of the most important findings in brain health, period. I mean, on some levels, it's a bit of a mystery to me why this isn't known by everyone.

Peter Attia

In other words, their brains are still riddled with the Alzheimer's toxins, but they've been able to really thwart the effects of those toxins because they show normal cognition.

Dina Dubal

If it doesn't work, it's going to kill your research program. And I would say, let it die then. I don't want to spend my career on something that's not important.

Dina Dubal
about three months
Mouse lifespan (Klotho knockout) Instead of 30 months, in mice without Klotho, due to premature aging.
30% longer
Mouse lifespan (Klotho overexpression) In mice engineered to overexpress Klotho.
about six times
Klotho levels at birth Higher than adult levels in cord blood.
by half
Klotho decline with age Decrease in Klotho levels from age 40 onwards.
40% or so
Klotho diurnal rhythm decrease Decrease in Klotho levels from morning high to midnight nadir.
about 30%
Klotho increase from chronic exercise Increase in Klotho levels after 12 weeks of chronic exercise in humans.
even double
Klotho increase from acute exercise (mice) Acute increase in Klotho levels after a 45-minute treadmill run in mice.
24 hours
Mouse fasting duration for Klotho/BDNF increase Duration of fasting in mice to increase Klotho and BDNF in the brain.
maybe 70% or so
Cognitive improvement in Parkinson's mouse model Improvement in cognitive abilities with Klotho treatment in alpha-synuclein overexpressing mice.
at least three weeks (14 to 21 days)
Duration of cognitive enhancement (primates) After a single subcutaneous injection of a low, physiologic dose of Klotho in Rhesus macaques, with some tested up to 28 days.
about one to four, one to five
Prevalence of KL-VS heterozygosity Fraction of individuals in the general population who carry one copy of the KL-VS genetic variant.
about 15%, maybe 20%
Klotho increase from KL-VS heterozygosity Increase in circulating Klotho levels due to carrying one copy of the KL-VS variant.
probably a 30% decrease
Klotho decrease from KL-VS homozygosity Compared to non-carriers, in individuals homozygous for the KL-VS variant.
over 10,000 people
NHANES study participants Number of participants in the study linking Klotho levels to mortality.
about 56 years
NHANES study mean age Mean age of participants in the NHANES study.
less than 666 picograms per mil
Klotho threshold for increased mortality Klotho serum level associated with increased mortality in the NHANES study.
30% mortality
Increased mortality with low Klotho Over five years, for individuals with Klotho levels below 666 pg/mL (NHANES study).