rna-binding

Ro 08-2750 is a non-peptide, reversible nerve growth factor (NGF) inhibitor that binds to NGF with an IC50 of approximately 1 µM. It is also a selective MSI RNA-binding activity inhibitor, exhibiting an IC50 of 2.7 μM. Additionally, Ro 08-2750 selectively inhibits NGF binding to p75NTR over TRKA.

PTBP1-RNA-binding inhibitor P6 TFA (PTBP1 α3-helix derived peptide P6 TFA) is a specific stapled peptide inhibitor of the splicing factor PTBP1, which is used to inhibit RNA alternative splicing events regulated by PTBP1. PTBP1-RNA-binding inhibitor P6 TFA exerts its effects by binding to the RNA recognition motif of PTBP1.

Suramin Sodium Salt (BAY-205) is a sodium salt form of suramin, a polysulphonated naphthylurea with potential antineoplastic activity. Suramin blocks the binding of various growth factors, including insulin-like growth factor I (IGF-I), epidermal growth factor (EGF), platelet-derived growth factor (PDGF), and tumor growth factor-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cell proliferation and migration. This agent also inhibits vascular endothelial growth factor (VEGF)- and basic fibroblast growth factor (bFGF)-induced angiogenesis; retroviral reverse transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cellular folate transport; and steroidogenesis.

Puromycin dihydrochloride (CL13900 dihydrochloride) is a cinnamamide adenosine antibiotic and an inhibitor of protein synthesis. Puromycin dihydrochloride inhibits protein synthesis by binding to RNA and has antitumor and antitrypanosomal activity.

Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50 = 650 nM). It inhibits multiple cancer cell lines via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome, displaying low-nM to sub-nM IC50s. Thailanstatin A, as a payload for ADCs, is conjugated to the lysines on trastuzumab, yielding linker-less ADC.

AOH1996 is an orally active ligand for the replicasome component PCNA (proliferating cell nuclear antigen), targeting the transcription-replication conflict (TRC). It interferes with the interaction of PCNA with its binding proteins, leading to DNA replication stress and apoptosis. AOH1996 causes proteasome-dependent rpb1 degradation and lethal DNA damage by stabilizing the interaction between PCNA and RNA polymerase II, and acts synergistically with DNA damaging agents to inhibit tumor cell growth.

Galidesivir hydrochloride is an inhibitor of viral RNA-dependent RNA polymerase (RdRp). It inhibits SARS-CoV-2 by tightly binding to its RdRp.

Setrobuvir (ANA-598) is an orally active non-nucleoside HCV NS5B polymerase inhibitor with inhibitory effects on de novo RNA synthesis and primer extension with IC50s between 4 and 5 nM. setrobuvir shows good binding affinity for SARS-CoV-2 RdRp and induces inhibition of RdRp.

SMN-C2 is a selective regulator of SMN2 gene splicing, a risdiplam analogue, a selective RNA-binding ligand that regulates pre-mRNA splicing and acts by binding to SMN2 pre-mRNA.SMN-C2 has the potential to be used in the study of spinal muscular atrophy (SMA).

Tedizolid (DA-7157)is a novel oxazolidinone-class antibiotic that inhibits bacterial protein synthesis by binding to the 23S ribosomal RNA of the 50S subunit of the ribosome.

EDC hydrochloride (EDC-HCl Crosslinker) is a water-soluble carbodiimide compound. EDC hydrochloride, as a condensing agent, forms peptide bonds through the condensation reaction of carboxyl and amino groups and can be used to synthesize peptides with specific sequences and functions. EDC hydrochloride can covalently bind haptens to carrier proteins to form immune antigens, which are used in vaccine research. EDC hydrochloride can react with the 5 'phosphate group of nucleic acids and is used for the labeling of DNA and RNA. EDC hydrochloride can cross-link proteins with nucleic acids and is used to prepare immune cross-links. EDC hydrochloride, as a crosslinking agent, connects the amine-reactive NHS ester of biomolecules with the carboxyl group, which can be used for protein coupling to create hybrid molecules with new properties and functions.

Lin28 1632 is an inhibitor of RNA binding protein Lin28. It promotes mESC differentiation. Lin281632 is also bromodomain inhibitor.

L-Histidine benzyl ester bistosylate may serve as an activator for HutP, an RNA-binding protein.

Apramycin(Nebramycin II) is an aminoglycoside antibiotic used in veterinary medicine. IC50 value:Target: Apramycin stands out among aminoglycosides for its mechanism of action which is based on blocking translocation and its ability to bind also to the eukaryotic decoding site despite differences in key residues required for apramycin recognition by the bacterial target. The drug binds in the deep groove of the RNA which forms a continuously stacked helix comprising non-canonical C.A and G.A base pairs and a bulged-out adenine. The binding mode of apramycin at the human decoding-site RNA is distinct from aminoglycoside recognition of the bacterial target, suggesting a molecular basis for the actions of apramycin in eukaryotes and bacteria. [1]. Apramycin, From Wikipedia

Erythromycin thiocyanate acts by binding to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid .Erythromycin thiocyanate

Lefamulin acetate (BC-3781 acetate) (formally BC-3781 acetate) is a novel pleuromutilin antibiotic and is the first to be used for the systemic treatment of bacterial infections in humans. Lefamulin acetate (BC-3781 acetate) inhibits protein synthesis by binding to the peptidyl transferase center of the 50S bacterial ribosome, preventing the binding of transfer RNA for peptide transfer. Lefamulin acetate (BC-3781 acetate) is an orally active antibiotic for community-acquired bacterial pneumonia (CABP) treatment.

Hycanthone (Etrenol(mesylate)) is a potent drug of antischistosomal. Hycanthone is a DNA intercalator that inhibits RNA synthesis and DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits APE1 via direct protein binding(KD: 10 nM).

Streptolydigin inhibits RNA synthesis by binding to RNA polymerase and does not inhibit eukaryotic RNA polymerases. Streptolydigin is a 3-acetyltetramic acid antibiotic and a potent bacterial RNA polymerase inhibitor (Ki: 18 μM and a Kd: 15 μM).

Clemizole, an H1 histamine receptor antagonist, inhibits NS4B's RNA binding and hepatitis C virus (HCV) replication.

Clemizole hydrochloride is an antagonist for H1 histamine receptor. According to the research, Clemizole hydrochloride can inhibit hepatitis C virus (HCV) replication and NS4B's RNA binding.

Puromycin (NSC-3055) is an antibiotic protein synthesis inhibitor. It inhibits protein synthesis by binding to RNA. It also serves as an anticancer drug by suppressing the growth and metastasis in esophagus cancer cells by Akt phosphorylation. It is an antineoplastic and antitrypanosomal agent and is used in research as an inhibitor of protein synthesis.

DMDA-PatA is a small-molecule inhibitor of eIF4A, a DEAD-box RNA-binding protein. It functions by clamping eIF4A onto the GNG motif in an mRNA-selective and ATP-independent manner, thereby inhibiting translation. DMDA-PatA holds potential for applications in cancer and viral infection research.

Guanosine triphosphate tritris (GTP tritris) serves as a crucial enhancer in myocyte differentiation, playing an essential role in regulating miRNA-muscle regulatory factors. It promotes the release of exosomes rich in guanine and guanine-derived molecules, and is considered an activation precursor for RNA synthesis. In mitochondrial functionality, GTP is involved in the entry of proteins into the matrix, which is vital for various regulatory pathways. It initiates peptide synthesis by facilitating the binding of formylmethionine-tRNA to the ribosome, and aids in polypeptide chain elongation. Additionally, GTP acts as a carrier for phosphates and pyrophosphates, channeling chemical energy into specific biosynthetic pathways. It activates signal transduction G proteins, regulates cellular processes such as proliferation and differentiation, and its hydrolysis by small GTPases (including Ras and Rho) is indispensable for both proliferation and apoptosis. Furthermore, the small GTPase Rab assists in vesicle docking, fusion, and formation. Beyond signal transduction, GTP is also an energy-rich precursor in the biosynthesis of DNA and RNA enzymes.

Tuberactinomycin compounds are essential components in the current combination of drugs used to combat Mycobacterium tuberculosis infections. These compounds target bacterial ribosomes and function by binding RNA and disrupting bacterial protein biosynthesis. Tuberactinomycin is produced by the actinomycete [Streptomyces puniceus], which binds RNA and inhibits protein synthesis in prokaryotes as well as certain forms of RNA splicing.