Rare & Orphan Lab · DeCure for X

DeCure for Pitt-Hopkins-like syndrome 2

DeCure's autonomous Rare AI scientist is researching a drug-repurposing hypothesis for Pitt-Hopkins-like syndrome 2 — 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 modulePitt-Hopkins-like syndrome 2 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 pitt-hopkins-like syndrome 2 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

neurexin 1 (NRXN1)NRXN1 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 apo structuredrag to rotate · scroll to zoom

RCSB Protein Data Bank · entry 3B3Q · 2.4 Å · ligand none (apo structure). Experimental structure, not a prediction.

What the evidence adds up to

Pitt-Hopkins syndrome (PTHS) is caused by haploinsufficiency of the TCF4 gene on chromosome 18q21. Most cases are sporadic, but somatic mosaicism has been reported infrequently. In one family, a proband with typical PTHS and his younger brother with a less striking phenotype both carried a heterozygous frameshift mutation (c.1901_1909delinsA, p.Ala634AspfsX67) in exon 19 of TCF4; the same mutation was found at low levels in DNA from the mother's blood, urine and saliva, despite her being healthy. In another family, a phenotypically normal father carried a mosaic 263.4 kb deletion removing exons 4–9 of TCF4 at approximately 20% mosaicism in blood, and his affected son inherited the full deletion. A separate report describes a girl with a PTHS phenotype who carried a de novo mosaic 10.17 Mb deletion on 18q21.2q21.33 at approximately 12% mosaicism in blood; her parents were normal. A total of 11 individuals carrying various mosaic TCF4 aberrations have been reported, with phenotypes ranging from severe PTHS to completely normal. The degree of mosaicism in blood does not reliably predict clinical severity: the girl with 12% mosaicism had severe PTHS, while the father with 20% mosaicism was unaffected, likely due to tissue-specific differences in the brain.

A 2001 report described two sibs with severe intellectual disability, coarse facial features, short stature, seizures, hypertrichosis, short great toes, and overbreathing, and suggested they could represent the first familial cases of Pitt-Hopkins syndrome, supporting autosomal recessive inheritance. However, subsequent molecular work has established that PTHS is caused by TCF4 haploinsufficiency, and the majority of cases are de novo. A 2023 study identified a heterozygous c.607delT (p.S203Pfs*31) variant in exon 9 of TCF4 in a child with facial dysmorphism, single palmar crease, motor and language delay, and hypoplasia of the corpus callosum; both parents were wild-type, and the variant was classified as pathogenic.

Current approaches to PTHS have limited impact, and the phenotypic variation among patients is not fully understood. Genotype-phenotype correlations remain unclear: some studies suggest larger deletions including contiguous genes add to severity, while others show no significant phenotypic differences between various deletion sizes and point mutations, confirming TCF4 haploinsufficiency as the main pathogenic mechanism. What is still missing is a systematic collection of clinical and genetic data on mosaic cases to understand tissue-specific mosaicism, particularly in brain tissue, which cannot be directly sampled. Better detection of parental mosaicism is needed for accurate genetic counselling and recurrence risk assessment, but this requires routine use of sensitive techniques such as deep sequencing or FISH in parents of apparently sporadic cases. No targeted therapies exist, and no clinical trials for PTHS are described in these abstracts.

Evidence

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

Clinical Genetics · 2012 · 70 citations

Somatic mosaicism in a mother of two children with Pitt–Hopkins syndrome

AbstractSteinbusch CVM, van Roozendaal KEP, Tserpelis D, Smeets EEJ, Kranenburg‐de Koning TJ, de Waal KH, Zweier C, Rauch A, Hennekam RCM, Blok MJ, Schrander‐Stumpel CTRM. Somatic mosaicism in a mother of two children with Pitt–Hopkins syndrome. Pitt–Hopkins syndrome (PTHS) is a neurodevelopmental disorder characterized by intellectual disability, unusual face and breathing abnormalities and can be caused by haploinsufficiency of TCF4 . The majority of cases are sporadic. Somatic mosaicism was reported infrequently. We report on a proband with typical manifestations of PTHS and his younger brother with a less striking phenotype. In both, a heterozygous frameshift mutation (c.1901_1909delinsA, p.Ala634AspfsX67) was found in exon 19 of TCF4 . The same mutation was found at low levels in DNA extracted from the mother's blood, urine and saliva. This report of familial recurrence with somatic mosaicism in a healthy mother has important consequences for genetic counseling. We suggest careful studies in parents of other patients with PTHS to determine the frequency of germline and somatic mosaicism for TCF4 mutations.

https://doi.org/10.1111/j.1399-0004.2012.01857.x
American Journal of Medical Genetics · 2001 · 26 citations

Possible case of Pitt-Hopkins syndrome in sibs

AbstractIn this article, we describe two sibs, a brother and sister, with severe mental retardation and multiple congenital anomalies including "coarse" facial features, short stature, seizures, hypertrichosis, short great toes, and overbreathing. Comparison of these patients with previous reports suggests that they could represent the first familial cases of the Pitt-Hopkins syndrome. The recurrence in sibs within the same family supports autosomal recessive inheritance for the condition. Variable expression of the respiratory symptoms, which has not been reported earlier, is underlined.

https://doi.org/10.1002/ajmg.1523
American Journal of Medical Genetics Part A · 2018 · 4 citations · open access

Two unrelated individuals carrying rare mosaic deletions in <i>TCF4</i> gene

AbstractPitt–Hopkins syndrome (PTHS; MIM #610954) is a rare neurodevelopmental disorder first described in 1978 (Pitt & Hopkins, 1978), with a distinctive phenotype including facial dysmorphias, global developmental delay, severe intellectual disability, and hyperventilation episodes (Marangi & Zollino, 2015; Sweatt, 2013; Whalen et al., 2012). PTHS has a relatively short history of clinical and genetic investigation: its rarity and similarity to other well recognized syndromes has hampered the efforts for a deeper understanding of the underlying pathological mechanisms. It is only in the last decade that PTHS has emerged as a clinically and genetically defined entity (Whalen et al., 2012; Zweier et al., 2007). On the molecular level, PTHS is caused by mutations or variable size deletions involving the gene encoding basic helix–loop–helix transcription factor 4 (TCF4, OMIM 602272) located on 18q21 (Amiel et al., 2007; Brockschmidt et al., 2007; Hasi et al., 2011; Zweier et al., 2007). The involvement of TCF4 was first demonstrated in 2006 (Peippo et al., 2006) and to this day more than 200 PTHS patients with TCF4 point mutations or deletions have been reported (Marangi & Zollino, 2015) with the sizes of deletions ranging from 63 kb (Brockschmidt et al., 2007) to 13 Mb (Gustavsson, Kimber, Wahlstrom, & Anneren, 1999). Literature on mosaic TCF4 deletions is limited because of their rarity and interpretation challenges (Giurgea et al., 2008; Rossi et al., 2012; Stavropoulos, MacGregor, & Yoon, 2010). In this research letter we describe a unique mosaic TCF4 deletion in a girl with phenotype highly suggestive of PTHS (Family 1). This new finding is discussed in the light of a previous publication by our group (Family 2), where the phenotypically normal father of a PTHS patient carries a mosaic TCF4 deletion which is inherited in full by his affected son (Kousoulidou et al., 2013). Family 1 consists of a female with PTHS phenotype and her nonaffected parents. The patient was 13 months old at the time of assessment and was referred for array-comparative genomic hybridization (array-CGH). Clinical features included global developmental delay, happy predisposition, flapping hand movements, prominent forehead, deep-set eyes, thin eyebrows, up-slanting palpebral fissures, wide mouth, full lips, prominent nose, and cup-shaped ears. Microcephaly noted at birth at the fifth percentile, progressed to below second percentile by the time of referral. The patient also displayed fleshy hands and bilateral single palmar creases. At the age of 6 years the patient managed to walk unaided in an unstable manner, whereas cyanotic episodes with possible sleep apnea were reported. Array-CGH analysis of the patient using Cytochip ISCA array (BlueGnome-version 1.0) revealed a mosaic deletion of 10.17 Mb in size on chromosomal region18q21.2q21.33 spanning from 50,150,502 bp to 60,317,102 bp (GRCh38/hg19) harbouring TCF4 gene (Figure 1). Fluorescence in situ hybridization (FISH) analysis using locus specific probes confirmed this finding and determined the mosaicism level to be approximately 12%, with 6 abnormal out of 53 studied cells (Figure 2). FISH analysis of the parents was normal for all cells (n = 20), thus defining the patient's mosaic deletion as de novo. Family 2 consists of a male with PTHS spectrum phenotype and his nonaffected parents who were referred to our laboratory for genetic testing. A detailed clinical description of the patient as well as the results of genetic investigation, are included in a previous publication by our group (Kousoulidou et al., 2013). Briefly, array-CGH of the affected child revealed a 263.4 kb deletion of chromosomal region 18q21.2 spanning from 51,095,520 bp to 51,358,929 bp (hg18) and removing exons 4–9 of TCF4 gene. The exact same region exhibited a slight ratio shift towards lower values on the array-CGH profile of the patient's father, suggesting a possible mosaic deletion. Quantitative real-time PCR and FISH confirmed the deletion in the patient and estimated a ~20% mosaicism in the phenotypically normal father. The rarity of mosaicism for TCF4 deletions or mutations in PTHS patients adds a significant scientific and diagnostic value to any new findings of this type. A total of 11 individuals are currently found to carry various mosaic aberrations affecting TCF4 and exhibit various phenotypes (de Pontual et al., 2009; Essaoui et al., 2013; Giurgea et al., 2008; Jehee et al., 2017; Rossi et al., 2012; Stavropoulos et al., 2010). A list of all patients with phenotypic data is presented on Table 1. The only mosaic TCF4 aberrations with no clinical consequences are carried by the father of Family 2 (Kousoulidou et al., 2013) and the unaffected mother of twins with PTHS (Steinbusch et al., 2013). Most PTHS occurrences so far are caused by de novo events; only in three cases the causative mutations/deletions were inherited from a mosaic parent, namely the father of Family 2, the unaffected mosaic female mentioned above (Steinbusch et al., 2013) and the mosaic female with depression presented on Table 1 (de Pontual et al., 2009). In these rare instances the detection of parental germline mosaicism is crucial for genetic counseling, as it defines the exact origin of the aberration and indicates a significantly increased recurrence risk requiring targeted prenatal diagnosis in future pregnancies. Novel genetic testing techniques, in combination with traditional cytogenetic approaches such as karyotype and FISH will enable accurate identification of mosaicism within the frame of routine genetic investigation. Mosaicism detection is vital not only for assessment of PTHS inheritance, but also for prediction of possible phenotypic outcomes in affected mosaic individuals or foetuses with prenatal ultrasound abnormalities, the latter being far more challenging for genetic counseling. The accumulation of clinical and genetic data on mosaic cases would enable deeper understanding of TCF4––PTHS correlation, which is currently unclear: because TCF4 gene has important functions (Peippo & Ignatius, 2012), aberrations in the gene can affect several organs; consequently, some patients carrying TCF4 abnormalities may not be classified as PTHS because of atypical phenotype, not resembling those described in original publications (Peippo et al., 2006; Pitt & Hopkins, 1978). Genotype–phenotype correlations are expected to create the background for predictions that are valuable to the families involved. The degree of mosaicism in the patient from Family 1 is lower than in the nonaffected father from Family 2 (~12% vs. ~20%), although the clinical consequences are more severe, probably because of tissue specificity: the nonaffected father of Family 2 may have a lower rate of mosaicism in the brain than in peripheral blood; in contrast it could be assumed that the patient from Family 1 exhibits a higher percentage of abnormal cells in the brain, causing PTHS phenotype. Brain tissue mosaicism can indirectly be estimated by buccal swab analysis, where gene expression correlates with brain tissue (de Hoon, Monkhorst, Riegman, Laven, & Gribnau, 2015; Smith et al., 2015); however neither Family 1 nor Family 2 were available for further testing therefore a buccal sample could not be obtained. The size of deletions differs significantly between the two investigated families −10 Mb in Family 1 versus 263.4 kb in Family 2. The phenotype of the patient from Family 1 was consistent with PTHS, given the wide variability found in different patients (Marangi & Zollino, 2015; Whalen et al., 2012). Despite the small size of the deletion in Family 2, it removes some of the critical exons (Kalscheuer et al., 2008) and affects all 47 transcripts of TCF4 (Sepp, Kannike, Eesmaa, Urb, & Timmusk, 2011), hence the affected child carries the key clinical features of PTHS. When comparing the affected individuals from the two families, it is difficult to determine whether or not the size of deletion is an important factor in the phenotype severity, since one of the patients carries a larger deletion but in a mosaic state. Some studies suggest that larger deletions including contiguous genes add to the phenotype severity (Kato, Morimoto, Kimura, Matsushima, & Kondo, 2010; Marangi & Zollino, 2015), whereas other studies show no significant phenotypic differences between various size deletions and even point mutations, confirming TCF4 haploinsufficiency as the main pathogenic mechanism of PTHS (Giurgea et al., 2008). Currently the phenotypic variation among PTHS patients is not fully understood and not always correlates with the size of deletions detected in different patients. For this reason, epigenetic modifications, variable expressivity and genetic background are among the factors that should be taken into account. In our research letter we have once again highlighted that accurate diagnosis can only be achieved by combining clinical evaluation with detailed genetic profiling, especially for syndromes with phenotypic and genetic variability such as PTHS. Current and future developments in genetic testing will lead to more PTHS patients being diagnosed, thereby increasing the variability of PTHS phenotype, further defining the boundaries of PTHS spectrum. In addition, we have demonstrated the wide range of possible phenotypic outcomes in individuals carrying mosaic TCF4 mutations––from severe PTHS to a completely normal phenotype. For these rare and challenging cases, tissue specificity would be an exciting new focus for further studies. This information is vital for a more accurate diagnosis, prognosis and management. Clinical and molecular characterization of carriers of TCF4 mosaic deletions and/or mutations contributes to our understanding of the pathogenic mechanisms leading to PTHS. The authors would like to thank the patients and their families for participating in the study. None.

https://doi.org/10.1002/ajmg.a.60692
Pediatru ro · 2020 · 0 citations · open access

Pediatric neuropsychiatry at a glance. A rare condemnatory disease: Pitt-Hopkins syndrome

AbstractPitt-Hopkins syndrome is a genetic condition less de­bated in the literature in our country and even abroad. How­ever, in daily practice, the clinical pediatrician may en­coun­ter this syndrome, which may mask or overlap other psychiatric conditions, such as autism spectrum dis­order, or various aspects of certain neuromuscular dis­orders. The fact that not all children present the symptoms of this syndrome makes the differential diagnosis ex­treme­ly difficult. Moreover, current approaches to this neuro­pa­tho­lo­gical syndrome have a limited impact.

https://doi.org/10.26416/pedi.58.2.2020.3578
PubMed · 2023 · 0 citations

[Analysis of genetic variant in a child with Pitt-Hopkins syndrome].

AbstractOBJECTIVE: To explore the genetic basis for a child featuring facial dysmorphism, single palmar crease, motor and language delay, and hypoplasia of corpus callosum. METHODS: A child who had visited the Affiliated Hospital of Binzhou Medical College on March 16, 2021 was selected as the study subject. Peripheral blood samples of the child and his parents were collected, and the genomic DNA was extracted for whole exome sequencing (WES). Candidate variant was verified by Sanger sequencing and bioinformatic analysis. RESULTS: WES revealed that the child has harbored a heterozygous c.607delT (p.S203Pfs*31) variant in exon 9 of the TCF4 gene, for which both of his parents were of the wild-type. Based on guidelines from the American College of Medical Genetics and Genomics, the variant was classified as pathogenic (PVS1+PM2_Supporting+PM6). CONCLUSION: The heterozygous c.607delT (p.S203Pfs*31) variant of the TCF4 gene probably underlay the Pitt-Hopkins syndrome in this child. Genetic testing has enabled the definite diagnosis.

https://doi.org/10.3760/cma.j.cn511374-20220425-00278
Zurich Open Repository and Archive (University of Zurich) · 2013 · 0 citations · open access

Somatic mosaicism in a mother of two children with Pitt-Hopkins syndrome

AbstractSteinbusch CVM, van Roozendaal KEP, Tserpelis D, Smeets EEJ, Kranenburg-de Koning TJ, de Waal KH, Zweier C, Rauch A, Hennekam RCM, Blok MJ, Schrander-Stumpel CTRM. Somatic mosaicism in a mother of two children with Pitt-Hopkins syndrome. Pitt-Hopkins syndrome (PTHS) is a neurodevelopmental disorder characterized by intellectual disability, unusual face and breathing abnormalities and can be caused by haploinsufficiency of TCF4. The majority of cases are sporadic. Somatic mosaicism was reported infrequently. We report on a proband with typical manifestations of PTHS and his younger brother with a less striking phenotype. In both, a heterozygous frameshift mutation (c.1901_1909delinsA, p.Ala634AspfsX67) was found in exon 19 of TCF4. The same mutation was found at low levels in DNA extracted from the mother's blood, urine and saliva. This report of familial recurrence with somatic mosaicism in a healthy mother has important consequences for genetic counseling. We suggest careful studies in parents of other patients with PTHS to determine the frequency of germline and somatic mosaicism for TCF4 mutations.

https://doi.org/10.5167/uzh-72456

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.