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G-quadruplex ligands bind four-stranded structures that form in guanine-rich DNA and RNA sequences. Four guanines pair through Hoogsteen hydrogen bonds into a planar G-quartet, and stacked quartets are stabilized by potassium ions. Parallel four-stranded complexes of guanine-rich DNA were described in 1988. In 2013 a structure-specific antibody visualized G-quadruplexes in human cell nuclei, with numbers that changed during the cell cycle. Such structures occur at telomeres, in gene promoters and in ribosomal DNA. Pyridostatin, reported in 2008, stabilizes telomeric G-quadruplexes and triggers a DNA damage response there. 360A and MTR-106 are further stabilizing ligands, and BMVC-8C3O is a carbazole-based G-quadruplex ligand. Quarfloxin targets G-quadruplexes in ribosomal DNA and inhibits ribosomal RNA (rRNA) biogenesis.
Synonyms: Pyridostatin; PDS
Pyridostatin stabilizes G-quadruplexes (G4s) in cells and elicits a DNA damage response by causing the formation of DNA double strand breaks (DSB).
Synonyms: RR82 hydrochloride; RR 82
Pyridostatin hydrochloride (RR82 hydrochloride) is a G-quadruplexe stabilizer, with a Kd of 490 nM.
BMVC-8C3O is a DNA G-quadruplexe (G4) ligand which can induce topological conversion of non-parallel to parallel forms in human telomeric DNA G4s.
L5-DA is a selective G-quadruplex stabilizer that preferentially interacts with G4 structures over double-stranded DNA. This compound exhibits notable cytotoxicity against HeLa cells, with an IC50 value of 4.3 μM. L5-DA effectively stabilizes G4s within HeLa cells, leading to the induction of apoptosis and cell cycle arrest. Its role in modulating G-quadruplexes makes it a valuable tool for research in cancer biology and therapeutic development.
MTR-106 is a potent G-quadruplex stabilizer that also functions as an RNA polymerase I inhibitor. This compound has demonstrated the ability to induce apoptosis and inhibit cell proliferation, making it a valuable tool in cancer research. Its unique mechanism of action provides insights into G-quadruplex dynamics and their implications in tumor biology.
Y502-2304 is a potent c-Myc G-quadruplex stabilizer that exhibits significant antiproliferative activity in multiple myeloma (MM) cells. It effectively downregulates both c-Myc mRNA and protein expression, leading to the induction of apoptosis characterized by increased γH2AX levels and elevated reactive oxygen species (ROS). Additionally, Y502-2304 disrupts mitochondrial function and demonstrates a marked inhibition of tumor growth in xenograft models of MM. This compound is suitable for various research applications focused on elucidating the molecular mechanisms underlying multiple myeloma.
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Telomeric G4s ligand 1 is a telomeric G-quadruplex ligand known for its ability to stabilize telomeric G4 structures and promote R-loop formation, resulting in DNA damage responses. This compound has been shown to induce apoptosis in tumor cells and trigger immunogenic cell death (ICD), making it a valuable tool for cancer research and therapeutic applications.
G-quadruplex ligand 1 targets G-quadruplex structures in DNA, disrupting their stability. This ligand significantly enhances gene expression by altering the conformation of G-quadruplexes, making it a valuable tool for studies involving gene regulation and potential therapeutic applications. Its unique properties facilitate investigations into the roles of G-quadruplexes in cellular processes and disease mechanisms.
PT-ttpy is a metallo-organic complex that acts as a potent ligand for G-quadruplex structures. It effectively induces telomere-related DNA damage in cancer cells by inhibiting telomerase activity and disrupting telomere functions. Additionally, PT-ttpy is associated with various chromatin abnormalities during mitosis, including the formation of chromatin bridges, ultrafine bridges (UFBs), and double-stranded breaks (DSBs). This reagent is valuable for research in cancer biology and the study of telomere dynamics.
Telomeric G4s Ligand 2 is a selective ligand that targets telomeric G-quadruplex (G4) structures, exhibiting an IC50 value of 0.4 μM. This compound binds to dimeric telomeric G4 and inhibits the functions of DHX36 and BLM helicases. It activates both cGAS-STING and TERRA-ZBP1 pathways, leading to induction of autophagy and G2/M cell cycle arrest, demonstrating significant antiproliferative effects across various cancer cell lines. This reagent is useful for investigating mechanisms underlying colorectal cancer.
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SYUIQ-5 is a G-quadruplex ligand that specifically stabilizes G-quadruplex structures, thereby inducing cellular senescence. This compound inhibits the activity of the c-myc gene promoter, which is critical in tumorigenesis. Additionally, SYUIQ-5 promotes autophagy in cancer cells by causing telomere damage through the delocalization of TRF2 from telomeric regions, making it a valuable tool for investigating pathways related to cancer and aging.
N-Methylmesoporphyrin IX (NMM) is a potent fluorescent binder that targets G-quadruplex DNA, making it an effective probe for studying Aβ fibrillation. It serves as both an in situ inhibitor and an ex situ monitor of Aβ amyloidogenesis in vitro and within cellular contexts. NMM exhibits high sensitivity to G-quadruplex structures while showing negligible response to duplexes, triplexes, and single-stranded DNA. Additionally, it remains nonfluorescent in monomeric Aβ environments, producing strong fluorescence upon interaction with Aβ aggregates.
Carboxy pyridostatin trifluoroacetate salt is a G-quadruplex ligand that selectively interacts with G-quadruplex structures in RNA and DNA. This compound has been shown to decrease levels of ATF-5 protein, thereby inhibiting cell proliferation and disrupting stress granule formation. It serves as a valuable tool in the study of G-quadruplex biology and its implications in cellular stress responses and cancer research.
Synonyms: o-BMVC
BMVC2 is a bisubstituted carbazole derivative that serves as a G-quadruplex (G4) stabilizer. This compound promotes the formation and stabilization of G-quadruplex structures, which are important in the regulation of gene expression and telomere maintenance. BMVC2 is utilized in research applications focusing on cancer biology, antiviral therapies, and the development of novel molecular therapeutics targeting G4 DNA structures.
Carboxypyridostatin is a selective ligand for G-quadruplex structures. It demonstrates significant affinity for RNA G-quadruplexes, leading to the downregulation of ATF-5 protein levels. This compound is known to inhibit cell proliferation and interfere with stress granule formation, making it valuable for studies on cellular stress responses and G-quadruplex-related mechanisms in cancer research.
Synonyms: RR82 trihydrochloride
Pyridostatin trihydrochloride is a potent G-quadruplex stabilizer with a binding affinity (Kd) of 490 nM, effectively targeting DNA and RNA G-quadruplex structures within cellular environments. This compound induces growth arrest in human cancer cells through mechanisms involving replication- and transcription-dependent DNA damage. Pyridostatin specifically impacts the proto-oncogene Src, leading to diminished SRC protein levels and reduced SRC-dependent cellular motility in human breast cancer cells. Its applications extend to cancer research, particularly in studying mechanisms of tumor progression and drug resistance.
Synonyms: Methoxymorpholinyl doxorubicin hydrochloride; FCE 23762 hydrochloride; PNU 152243A
Nemorubicin hydrochloride is a doxorubicin derivative that primarily targets G-quadruplex structures. It exhibits notable antitumor activity by intercalating into duplex DNA while also serving as a potent ligand for G-quadruplex DNA segments, effectively stabilizing their conformation. This compound is valuable for research applications focused on understanding G-quadruplex biology and developing therapeutic strategies targeting this unique DNA structure.
