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DRUG CLASS:

DNA minor groove binder

4ms
FIH Study to Evaluate Safety, Tolerability, PK, PD & Preliminary Efficacy of AT03-65 With Advanced Solid Tumors (clinicaltrials.gov)
P1, N=83, Not yet recruiting, Axcynsis Therapeutics Pte Ltd | Initiation date: Aug 2025 --> Nov 2025
Trial initiation date
4ms
[18F]FDG PET metabolic correlates of cerebrospinal fluid TAR DNA-binding protein 43 in prodromal Alzheimer's disease. (PubMed, Neurobiol Dis)
TDP-43 pathology in prodromal AD, as indicated by elevated CSF TDP-43 levels, contributes to metabolic disruptions in posterior parietal regions, particularly the precuneus. These changes diverge from typical amyloid- and tau-related alterations, offering indirect in vivo insights into TDP-43 co-pathology in prodromal AD.
Journal
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TARDBP (TAR DNA Binding Protein)
7ms
A novel DNA binding protein encoded by circZNF131 inhibits the growth of gastric cancer by suppressing CTBP2 transcription. (PubMed, Int J Biol Macromol)
Moreover, ZNF131-354aa was found to promote E-cadherin and phosphatase and tensin homolog (PTEN) expression by interacting with the intron of the C-terminal binding protein 2 (CTBP2) gene and repressing its expression. In conclusion, ZNF131-354aa acts as a tumor suppressor in GC by inhibiting CTBP2 transcription.
Journal
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PTEN (Phosphatase and tensin homolog) • CDH1 (Cadherin 1) • CTBP2 (C-Terminal Binding Protein 2) • TRIM28 (Tripartite Motif Containing 28)
10ms
New P1 trial
1year
DNA-Binding Protein A Is Actively Secreted in a Calcium-and Inflammasome-Dependent Manner and Negatively Influences Tubular Cell Survival. (PubMed, Cells)
Given that CSD proteins YB-1 and DbpA fulfill the criteria of alarmins, we propose that their release signals an inherent danger to the host. Some data hint at an extracellular complex formation at a ratio of 10:1 (DbpA:YB-1) of both proteins.
Journal
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TNFA (Tumor Necrosis Factor-Alpha) • TNFRSF1A (TNF Receptor Superfamily Member 1A) • YBX1 (Y-Box Binding Protein 1) • NLRP3 (NLR Family Pyrin Domain Containing 3)
1year
Detection of SEZ6, a therapeutic target, in medullary thyroid carcinoma. (PubMed, J Clin Endocrinol Metab)
SEZ6 may serve as a novel biomarker for MTCs. Although SEZ6 lacks any prognostic values in MTC, its positivity in 91% to 93% of MTCs, including MTCs without RET and RAS mutations, renders SEZ6-targetted antibody-drug conjugate therapy a promising targeted therapy for MTCs.
Journal
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SEZ6 (Seizure Related 6 Homolog)
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RAS mutation • RET mutation • SEZ6 expression
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ABBV-011
1year
A Phase I First-in-Human Study of ABBV-011, a Seizure-Related Homolog Protein 6-Targeting Antibody-Drug Conjugate, in Patients With Small Cell Lung Cancer. (PubMed, Clin Cancer Res)
ABBV-011 1.0 mg/kg Q3W monotherapy was well tolerated and demonstrated encouraging antitumor activity in heavily pretreated patients with relapsed/refractory SCLC. SEZ6 is a promising novel SCLC target and warrants further investigation.
P1 data • Journal
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SEZ6 (Seizure Related 6 Homolog)
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ABBV-011
over1year
Anti-Skin Aging Potential, Antibacterial Activity, Inhibition of Single-Stranded DNA-Binding Protein, and Cytotoxic Effects of Acetone-Extracted Passiflora edulis (Tainung No. 1) Rind Extract on Oral Carcinoma Cells. (PubMed, Plants (Basel))
These results underscore the potential of P. edulis (Tainung No. 1) rind as a promising candidate for anti-skin aging, antibacterial, and anticancer applications, meriting further therapeutic investigation.
Journal
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CA9 (Carbonic anhydrase 9) • RPA1 (Replication Protein A1)
over1year
Regulation of DNA Damage Response by RNA/DNA-Binding Proteins: Implications for Neurological Disorders and Aging. (PubMed, Ageing Res Rev)
In this review, we discuss the emerging roles of common RDBPs from the heterogeneous nuclear ribonucleoprotein (hnRNP) family, such as TAR DNA binding protein-43 (TDP43) and fused in sarcoma (FUS) in controlling DNA damage response (DDR). We also explore the implications of RDBP pathology in aging and neurodegenerative diseases and provide a prospective on the therapeutic potential of targeting RDBP pathology mediated DDR defects for motor neuron diseases and aging.
Review • Journal
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TARDBP (TAR DNA Binding Protein) • FUS (FUS RNA Binding Protein)
over1year
Serum transactive response DNA binding protein 43 associates with poor short-term neurologic outcome after return of spontaneous circulation following cardiac arrest. (PubMed, Shock)
Elevated serum TDP-43 level was associated with and could be used together with Witnessed CA, IL-6, and NSE to predict poor 28-day neurologic outcome in patients after ROSC following cardiac arrest.
Journal
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IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • TARDBP (TAR DNA Binding Protein) • CRP (C-reactive protein)
over1year
Comprehensive Analysis of the Expression, Prognosis, and Immune Infiltrates for Chromodomain-Helicase-DNA-Binding Proteins in Breast Tumor. (PubMed, Asian Pac J Cancer Prev)
The altered expression of some CHD members was significantly related to clinical cancer outcomes, and CHD1/2/8/9 could serve as potential prognostic biomarkers to improve the survival of BrCa patients. However, to evaluate the studied CHD members in detail are needed further investigations including experimental validation.
Journal • BRCA Biomarker • Epigenetic controller
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CHD1 (Chromodomain Helicase DNA Binding Protein 1) • CHD8 (Chromodomain Helicase DNA Binding Protein 8) • CHD2 (Chromodomain Helicase DNA Binding Protein 2) • MIR615 (MicroRNA 615) • MIRLET7B (MicroRNA Let-7b)
over1year
Z-DNA binding protein 1 orchestrates innate immunity and inflammatory cell death. (PubMed, Cytokine Growth Factor Rev)
In response to damaged mitochondrial DNA, ZBP1 can interact with cyclic GMP-AMP synthase to augment IFN-I responses but inhibits toll like receptor 9-mediated inflammatory responses. This review summarizes the structure and expression pattern of ZBP1, discusses its roles in human diseases through immune-dependent (e.g., the production of IFN-I and pro-inflammatory cytokines) and -independent (e.g., the activation of cell death) functions, and highlights the attractive prospect of manipulating ZBP1 as a promising therapeutic target in diseases.
Review • Journal • IO biomarker • Inflammatory cell
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CASP3 (Caspase 3) • TLR9 (Toll Like Receptor 9) • AIM2 (Absent In Melanoma 2) • CDK7 (Cyclin Dependent Kinase 7) • IGF2BP1 (Insulin Like Growth Factor 2 MRNA Binding Protein 1) • CGAS (Cyclic GMP-AMP Synthase) • RIPK1 (Receptor Interacting Serine/Threonine Kinase 1)