Neuro Lab · DeCure for X

DeCure for Hypomyelinating leukodystrophy 11

DeCure's autonomous Neuro AI scientist is researching a drug-repurposing hypothesis for hypomyelinating leukodystrophy 11 — screening already-approved drugs against its 1-gene Open Targets disease module to publish open-access research. Research is fast; the path to publication is funded in milestone stages.

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The disease map

Disease moduleHypomyelinating leukodystrophy 11 maps to a 1-gene Open Targets module — the target space DeCure's AI scientist screens approved drugs against.
DeCure.ai methodSignature reversal (LINCS) plus network proximity (STRING) rank already-approved drugs likely to perturb this module — the same engine that produces DeCure.ai's repurposing hypotheses.
Repurposing thesisScreening approved medicines against this disease module, then publishing the evidence for the strongest candidate. Known pharmacology and human exposure data make the first question sharper — they do not establish safety or efficacy in a new indication.

Research record

01
ResearchComing soon
Candidate research + dossier — target rationale, drug-repurposing thesis and evidence pack.proof: Published dossier + on-chain hash
02
ValidationComing soon
In-vitro biological validation at a contract research org (CRO).proof: CRO contract + in-vitro report
03
Peer review & paperComing soon
Peer-reviewed paper published open-access (preprint + journal).proof: DOI + open-access link + on-chain hash

Current lead

No approved-drug candidate for hypomyelinating leukodystrophy 11 is corroborated in the literature DeepSearch retrieved. Some conditions are managed with non-pharmacological care — a device, surgery or physical therapy — rather than a medicine; that may be the case here, or the literature we found may simply be too sparse yet to support a drug-repurposing angle.

Molecular view

RNA polymerase I and III subunit C (POLR1C)POLR1C is one of the genes genetically linked to this disease in Open Targets — shown as context, not as a drug target we're pursuing: no approved-drug candidate for this disease is yet corroborated in the literature we found.

Loading structure…
helix sheet sf4drag to rotate · scroll to zoom

RCSB Protein Data Bank · entry 7AE1 · 2.8 Å · ligand IRON/SULFUR CLUSTER (SF4). Experimental structure, not a prediction.

What the evidence adds up to

Hypomyelinating leukodystrophies are a genetically heterogeneous group of heritable disorders with no curative treatment or disease-modifying therapy currently available. Current management relies on serial MRI to establish and monitor hypomyelination, molecular diagnostics, and careful attention to neurologic complications. Significant gaps remain in disease classification, characterisation, and outcome measures needed for clinical trials.

POLR3-related leukodystrophy, one of the most common hypomyelinating leukodystrophies, has no disease-modifying therapy. A 2021 review discusses stem cell transplantation, gene replacement therapy, and gene editing as potential approaches that have shown promise in other leukodystrophies, but these remain at the stage of pre-clinical consideration for POLR3-related disease.

In 2017, a recurrent de novo mutation c.754G>A (p.Asp252Asn) in TMEM106B was identified in four unrelated patients with hypomyelinating leukodystrophy. All four had early-onset nystagmus, hypotonia, delayed motor development, and variable intellectual disability and epilepsy. In one family, the father carried the mutation in mosaic form (approximately 25% mutant TMEM106B in leucocytes) and, though he had nystagmus and developmental delay in infancy, at age 65 he had normal cognition and no obvious neurological abnormalities. The effect of the p.Asp252Asn mutation on TMEM106B expression or function was not studied in vitro or in patient material, so the disease mechanism remains speculative. TMEM106B levels appear to be tightly regulated; available data suggest that either too much or too little may have devastating consequences.

What is still missing: validated outcome measures for clinical trials, funding for pre-clinical studies of the specific mutations involved, and patient stratification by genetic subtype. No therapy has been tested in a controlled trial for any hypomyelinating leukodystrophy.

Evidence

Retrieved by DeepSearch across 234,678,978 indexed works and resolved on OpenAlex — ranked by citations, including the results that did not work.

Annals of Neurology · 2014 · 152 citations · open access

Hypomyelinating leukodystrophies: Translational research progress and prospects

AbstractHypomyelinating leukodystrophies represent a genetically heterogeneous but clinically overlapping group of heritable disorders. Current management approaches in the care of the patient with a hypomyelinating leukodystrophy include use of serial magnetic resonance imaging (MRI) to establish and monitor hypomyelination, molecular diagnostics to determine a specific etiology, and equally importantly, careful attention to neurologic complications over time. Emerging research in oligodendrocyte biology and neuroradiology with bedside applications may result in the possibility of clinical trials in the near term, yet there are significant gaps in knowledge in disease classification, characterization, and outcome measures in this group of disorders. Here we review the biological background of myelination, the clinical and genetic variability in hypomyelinating leukodystrophies, and the insights that can be obtained from current MRI techniques. In addition, we discuss ongoing research approaches to define potential outcome markers for future clinical trials.

https://doi.org/10.1002/ana.24194
Neurology · 2014 · 64 citations · open access

<i>TUBB4A</i> de novo mutations cause isolated hypomyelination

AbstractOBJECTIVE: We present a series of unrelated patients with isolated hypomyelination, with or without mild cerebellar atrophy, and de novo TUBB4A mutations. METHODS: Patients in 2 large institutional review board-approved leukodystrophy bioregistries at Children's National Medical Center and Montreal Children's Hospital with similar MRI features had whole-exome sequencing performed. MRIs and clinical information were reviewed. RESULTS: Five patients who presented with hypomyelination without the classic basal ganglia abnormalities were found to have novel TUBB4A mutations through whole-exome sequencing. Clinical and imaging characteristics were reviewed suggesting a spectrum of clinical manifestations. CONCLUSION: Hypomyelinating leukodystrophies remain a diagnostic challenge with a large percentage of unresolved cases. This finding expands the phenotype of TUBB4A-related hypomyelinating conditions beyond hypomyelination with atrophy of the basal ganglia and cerebellum. TUBB4A mutation screening should be considered in cases of isolated hypomyelination or hypomyelination with nonspecific cerebellar atrophy.

https://doi.org/10.1212/wnl.0000000000000754
Frontiers in Cellular Neuroscience · 2021 · 19 citations · open access

POLR3-Related Leukodystrophy: Exploring Potential Therapeutic Approaches

AbstractLeukodystrophies are a class of rare inherited central nervous system (CNS) disorders that affect the white matter of the brain, typically leading to progressive neurodegeneration and early death. Hypomyelinating leukodystrophies are characterized by the abnormal formation of the myelin sheath during development. POLR3-related or 4H (hypomyelination, hypodontia, and hypogonadotropic hypogonadism) leukodystrophy is one of the most common types of hypomyelinating leukodystrophy for which no curative treatment or disease-modifying therapy is available. This review aims to describe potential therapies that could be further studied for effectiveness in pre-clinical studies, for an eventual translation to the clinic to treat the neurological manifestations associated with POLR3-related leukodystrophy. Here, we discuss the therapeutic approaches that have shown promise in other leukodystrophies, as well as other genetic diseases, and consider their use in treating POLR3-related leukodystrophy. More specifically, we explore the approaches of using stem cell transplantation, gene replacement therapy, and gene editing as potential treatment options, and discuss their possible benefits and limitations as future therapeutic directions.

https://doi.org/10.3389/fncel.2020.631802
CONTINUUM Lifelong Learning in Neurology · 2018 · 15 citations

Leukodystrophies

AbstractPURPOSE OF REVIEW: The leukodystrophies, typically considered incurable neurodegenerative disorders, are often diagnosed after irreversible central and peripheral nervous system injury has occurred. Early recognition of these disorders is imperative to enable potential therapeutic interventions. This article provides a summary of the symptoms of and diagnostic evaluation for leukodystrophies, along with the currently available therapies and recent advances in management. RECENT FINDINGS: The leukodystrophies are a rapidly expanding field because of advances in neuroimaging and genetics; however, recognition of the clinical and biochemical features of a leukodystrophy is essential to accurately interpret an abnormal MRI or genetic result. Moreover, the initial symptoms of leukodystrophies may mimic other common pediatric disorders, leading to a delay in the recognition of a degenerative disorder. SUMMARY: This article will aid the clinician in recognizing the clinical features of leukodystrophies and providing accurate diagnosis and management.

https://doi.org/10.1212/con.0000000000000560
Brain · 2017 · 3 citations · open access

TMEM106B and myelination: rare leukodystrophy families reveal unexpected connections

AbstractThis scientific commentary refers to ‘A recurrent de novo mutation in TMEM106B causes hypomyelinating leukodystrophy’, by Simons et al. (doi:10.1093/brain/awx314). Leukodystrophies are a group of rare genetic disorders that affect the CNS by disrupting the growth or maintenance of the myelin sheath that insulates nerve cells. A classification system based on the pathological mechanisms responsible for the white matter pathology was recently proposed, reserving the term hypomyelinating leukodystrophies (HLDs) for those diseases with a primary or predominant involvement of oligodendrocytes and/or myelin and a permanent deficiency in the formation or deposition of myelin (in contrast to demyelinating leukodystrophies in which the integrity of myelin is disrupted after its formation) (van der Knaap and Bugiani, 2017). HLDs are genetically and clinically diverse; however, most patients present in the neonatal or infantile period with a combination of hypotonia and nystagmus and a range of possible additional symptoms including developmental delay, ataxia, spasticity intellectual disability. Pelizaeus-Merzbacher disease (PMD) is the archetypical HLD caused by mutations in the gene encoding proteolipid protein 1 (PLP1), a primary constituent of myelin. However, more than a dozen additional HLD genes have been identified with a wide range of functions involved in different cellular processes: from RNA and protein synthesis to endolysosomal trafficking (Fig. 1) (Baskin et al., 2016; Charzewska et al., 2016; Edvardson et al., 2016). In this issue of Brain, Simons and co-workers reveal an intriguing connection between TMEM106B, a relatively unknown transmembrane protein localized to the lysosomal membrane, and HLD through the identification of a recurrent de novo TMEM106B mutation in four families (Simons et al., 2017). Overview of known disease genes for classical hypomyelinating leukodystrophies (HLDs). For each HLD-associated protein, the primary subcellular localization is reported as well as its primary known function(s) (Baskin et al., 2016; Charzewska et al., 2016; Edvardson et al., 2016). Nomenclature and numbering of HLD1 through HLD13 is in accordance with the OMIM database (https://www.omim.org/), while the newly identified HLD gene, TMEM106B, was temporarily assigned the acronym HLD14. PM = plasma membrane. Two unrelated patients recruited and studied on different continents by independent research groups formed the basis for the discovery. Researchers from the Care4Rare Canada Consortium and the Amsterdam Database of Unclassified Leukoencephalopathies in The Netherlands each diagnosed a patient with PMD-like disease based on the presence of nystagmus and hypotonia shortly after birth, delayed motor development, and prominent hypomyelination on brain MRI; however, genetic testing excluded mutations in PLP1. As a result of the childhood onset of disease and absence of family history, trio exome sequencing was performed in both families and, remarkably, the same de novo mutation c.754G>A (p.Asp252Asn) in TMEM106B was identified in both patients. Through effective use of the GeneMatcher website, which enables connections between researchers dealing with ‘unsolved exomes’, the researchers noted the strong overlap in clinical presentation and identical gene mutation, suggesting a potential causal role for this mutation in their patients. The study of exome data from 10 additional trios from The Netherlands and one unrelated patient from Canada, identified another two unrelated patients carrying the same c.754G>A mutation. Each of the four unrelated patients had the classical clinical presentation of hypomyelination with early-onset nystagmus, hypotonia and delayed motor development with variable degrees of intellectual disability and epilepsy. In one family the mutation was found to be transmitted from the father, who is a mosaic for the p.Asp252Asn mutation, to the affected child. The father expresses approximately 25% mutant TMEM106B, according to quantification of expression in leucocytes. While this presumably led to nystagmus and developmental delay in infancy, the currently 65-year-old male has normal cognition and no obvious neurological abnormalities. TMEM106B was first reported in 2010 as a genetic risk factor for frontotemporal lobar degeneration with pathologically confirmed TDP-43 pathology (FTLD-TDP), a neurodegenerative disease characterized by the preferential atrophy of the frontal and temporal lobes (Nicholson and Rademakers, 2016). Subsequent studies provided strong support for TMEM106B as a disease modifier, especially in patients with FTLD-TDP with loss-of-function mutations in progranulin (GRN), a neurotrophic growth factor that is processed into possibly functionally active granulin peptides within lysosomes. While the basis for the risk/protective effect of TMEM106B is still being studied, available data suggest that an increase in TMEM106B levels is cytotoxic and is associated with increases in lysosomal size and reduced lysosomal acidification, leading to the disruption of endolysosomal- and autophagic-lysosomal degradation (Nicholson and Rademakers, 2016). Lowering TMEM106B levels has therefore been suggested as a potential therapeutic avenue in patients with GRN mutations, and it was recently reported that Tmem106b deletion can normalize lysosomal protein levels in Grn−/− mice and rescue FTLD-related behavioural abnormalities and retinal degeneration in this model (Klein et al., 2017). However, TMEM106B knockdown may not be completely without consequences. Studies in neuronal cultures suggested mild effects on lysosomal trafficking, and the activity of several lysosomal enzymes was reduced in Tmem106b−/− mice, arguing for a tight regulation of TMEM106B in vivo (Nicholson and Rademakers, 2016; Klein et al., 2017). In line with these observations, relatively mild effects on the expression levels of TMEM106B were observed in individuals carrying the TMEM106B risk (increased expression) or TMEM106B protective (decreased expression) alleles (Nicholson and Rademakers, 2016). Intriguingly, the same TMEM106B variant(s) implicated in FTLD-TDP were recently identified in an unbiased screen for genetic modifiers of healthy brain ageing, with increased inflammation, neuronal loss, and cognitive deficits in brain specimens of TMEM106B risk allele carriers (Rhinn and Abeliovich, 2017). This study suggested an inappropriate polarization of microglia and other innate immune myeloid cells toward a pro-inflammatory state in TMEM106B risk allele carriers, yet the authors did not rule out a function for TMEM106B in neurons. The current study by Simons and colleagues in this issue of Brain (Simons et al., 2017) is the first to link TMEM106B to oligodendrocytes and myelination, unveiling an unexplored area of research into TMEM106B function and disease mechanisms. Unfortunately, the effect of the specific p.Asp252Asn mutation on TMEM106B expression and/or function was not studied in vitro or in patient material, and discussion of the potential disease mechanism is consequently speculative at this time. The close vicinity of the p.Asp252Asn mutation to one of the sites requiring complex glycosylation for proper TMEM106B transport, sorting and probably function (Nicholson and Rademakers, 2016), combined with the fact that all patients carried the exact same de novo mutation supports the hypothesis of a loss-of-function disease mechanism, although a gain of toxic function associated with the specific mutation cannot yet be excluded. Since all patients were heterozygous for the mutation, a dominant-negative disease mechanism may in fact be at play. The majority of HLD genes are transmitted as autosomal recessive disorders or are x-linked (PLP1) with the notable exception of TUBB4A, in which the heterozygous p.Asp249Asn mutation was shown to cause HLD with atrophy of the basal ganglia and cerebellum. In the latter case, a dominant-negative effect of the mutation presumably led to the loss or inefficient dimerization of microtubules (Simons et al., 2013; Charzewska et al., 2016). Given that PLP1 is one of the main structural components of the myelin sheath, and that PLP1 mutations are known to cause PMD with overlapping disease phenotypes to those described in association with the new TMEM106B mutation, it is tempting to speculate that mutant TMEM106B could potentially interfere with the highly regulated endocytosis and/or exocytosis of PLP1, thereby affecting its spatial and temporal expression (Saher and Stumpf, 2015). PLP1 is synthesized in oligodendrocytes in the rough endoplasmic reticulum (ER) and then transported to the Golgi and plasma membrane in lipid raft-like membrane domains, where it is integrated into the developing myelin sheet. In the absence of neuronal signals, PLP1 is internalized and stored in late endosomes and lysosomes from where it can be rapidly recruited to the sites of membrane growth when needed (Feldmann et al., 2011). In PMD, point mutations in PLP1 interfere with its trafficking, resulting in accumulation of PLP1 within the ER/Golgi. By contrast, overexpression of PLP1 due to duplications leads to excessive Glossary Hypomyelinating leukodystrophies (HLD): Genetically determined white matter diseases caused by a primary deficit in myelin deposition. Multiple HLD genes have been identified (Fig. 1). TMEM106B: Type I transmembrane protein mainly localized to late endosomes and lysosomes. Common variants at the TMEM106B locus have been implicated in frontotemporal dementia with TDP-43 pathology. Regardless of the specific mechanism associated with the recurrent TMEM106B mutation, the addition of TMEM106B to the list of known HLD genes reinforces the connection between lysosomes and myelination. Currently available data further suggest that TMEM106B levels are tightly regulated and that either too much or too little TMEM106B may have devastating consequences. Future mechanistic studies of this newly discovered p.Asp252Asn mutation will undoubtedly provide much-needed insights into the normal function of TMEM106B within lysosomes. This would appear to be the critical next step towards the development of therapies or disease-modifying treatments not only for HLDs but also for patients with FTLD-TDP with and without GRN mutations. X.Z. is supported by a postdoctoral fellowship from The Bluefield Project to Cure Frontotemporal Dementia. R.R. is funded by NIH grants R35 NS097261, UG3/UH3 NS0103870 P50 AG016574 and P01 NS084974 and the Consortium for Frontotemporal Dementia (CFR).

https://doi.org/10.1093/brain/awx318
Neurology · 2020 · 1 citations · open access

Reader response: Teaching NeuroImages: A rare case of Jacobsen syndrome with global diffuse hypomyelination of brain

AbstractWith interest we read the report by Patel et al.1 concerning a patient with Jacobsen syndrome due to an 11q23–11q24 deletion and MRI evidence for leukodystrophy with improvement at a follow-up, substantiated by FLAIR images. The authors claimed that these abnormalities represent hypomyelination. Hypomyelination is defined as a significant and permanent myelin deficit.2 Its MRI appearance is characterized by a diffusely hyperintense T2 white matter (WM) signal, which is less high than the signal in other leukodystrophies2,3 and certainly less high than the WM signal in the patient discussed here,1 who has strongly T2-hyperintense WM signal abnormalities.

https://doi.org/10.1212/wnl.0000000000009070

Disease module: DeepOracle (Open Targets). Structures: RDKit from PubChem SMILES. Literature: retrieved by DeepSearch across 234,678,978 indexed works (targeted per-candidate search), resolved on OpenAlex.

DeCure is a research and publication project, not medical advice and not a treatment. "DeCure for X" describes a research goal, not a claim that a cure exists. Backing a cure is a contribution to fund the research — it is not an investment, and confers no yield, royalty, equity or IP ownership. Papers are published open-access by the DeCure.ai DAO.