trna

Aminoacyl tRNA synthetase-IN-1 is an inhibitor of bacterial aminoacyl tRNA synthetase (aaRS).

Isoleucyl tRNA synthetase-IN-1 is a selective and potent inhibitor (Ki: 88 nM) that targets isoleucyl tRNA synthetase (IleRS).

Isoleucyl tRNA synthetase-IN-2 is a selective and potent inhibitor (Ki: 114 nM) that targets isoleucyl tRNA synthetase (IleRS).

Aminoacyl tRNA Synthetase-IN-2 (Compound 14) serves as an inhibitor of aminoacyl-tRNA synthetase (aaRS), presenting potential for the formulation of a novel class of antibiotics [1].

N4-Acetylcytidine (N-Acetylcytidine) is a modified nucleoside. N4-acetylcytidine is an endogenous urinary nucleoside product of the degradation of transfer ribonucleic acid (tRNA); urinary nucleosides are biological markers for patients with colorectal cancer.

Kasugamycin hydrochloride hydrate (Ksg (hydrochloride hydrate))(Ksg) specifically inhibits translation initiation of canonical but not of leaderless messenger RNAs. Ksg inhibition is thought to occur by direct competition with initiator transfer RNA

Tetracycline (Tetracyclin) is a naphthacene antibiotic that inhibits AMINO ACYL TRNA binding during protein synthesis.

N-BENZYL-2-PHENYLETHYLAMINE is an inhibitor of rel+ Escherichia coli B Phe-tRNA.

Oxytetracycline (OTC) is a broad-spectrum antibiotic that acts by inhibiting protein synthesis in bacteria. Oxytetracycline prevents the binding from aminoacil-tRNA to the complex m-ribosomal RNA. Oxytetracycline also possesses anti-HSV-1 activity[1][2][3

eukaryotic translation elongation factor 1 alpha 1 (EEF1A1) (387-394) [Multiple species](TFA) is Elongation factor 1 subunit.eukaryotic translation elongation factor 1 alpha 1 (EEF1A1) encodes an isoform of the alpha subunit of the elongation factor-1 complex, which is responsible for the enzymatic delivery of aminoacyl tRNAs to the ribosome. This isoform (alpha 1) is expressed in the brain, placenta, lung, liver, kidney, and pancreas, and the other isoform (alpha 2) is expressed in the brain, heart, and skeletal muscle. This isoform is identified as an autoantigen in 66% of patients with Felty syndrome. This gene has been found to have multiple copies on many chromosomes, some of which, if not all, represent different pseudogenes1.

2'-O-Methyl-2-thiouridine is a purine nucleoside analogue present in synthetic thermophilic bacterial tRNAs. 2'-O-Methyl-2-thiouridine is more selective for A than unmodified U.

HALOFUGINONE LACTATE is a halogenated derivative of febrifugine, a natural quinazolinone-containing compound found in the Chinese herb D. febrifuga.Halofuginone inhibits prolyl-tRNA synthetase in an ATP-dependent manner with a Ki of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity

GJ071 oxalate is a Nonsense suppressor. Nonsense suppressors (NonSups) induce “readthrough”, i.e., the selection of near cognate tRNAs at premature termination codons and insertion of the corresponding amino acid into nascent polypeptide.

LysRs-IN-1 is an inhibitor of Lysyl-tRNA synthetase (LysRs).

Halofuginone specifically inhibits collagen type I gene expression and matrix metalloproteinase 2 (MMP-2) gene expression, which may result in the suppression of angiogenesis, tumor stromal cell development, and tumor cell growth. Halofuginone Hydrobromide is the hydrobromide salt of halofuginone, a semisynthetic quinazolinone alkaloid anticoccidial derived from the plant Dichroa febrifuga, with antifibrotic and potential antineoplastic activities. These effects appear to be due to halofuginone-mediated inhibition of the collagen type I and MMP-2 promoters. Collagen type I and MMP-2 play important roles in fibroproliferative diseases.

N2-methylguanosine is a modified nucleoside of tRNA that occurs at several specific locations in many tRNA's

Oxytetracycline (Terramycin) is a TETRACYCLINE analog isolated from the actinomycete STREPTOMYCES rimosus and used in a wide variety of clinical conditions.

Tigecycline hydrate (GAR-936 hydrate) is a broad spectrum glycylcycline antibiotic. Tigecycline hydrate is bacteriostatic, that inhibits protein synthesis by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation. Tigecycline hydrate is active against resistant strains of Gram-positive and Gram-negative bacteria .

Lysidine (2-Methyl-2-iMidazoline) is a nucleoside rarely seen outside of tRNA. Lysidine has better translation fidelity.

ms2i6A is a mitochondrial tRNA-specific modification, which regulates efficient mitochondrial translation and energy metabolism in mammals.

Pulvomycin is a protein biosynthesis inhibitor preventing ternary complex formation between elongation factor Tu, GTP, and aminoacyl-tRNA.

LeuRS-IN-1 hydrochloride is a potent and orally active inhibitor of M. tuberculosis leucyl-tRNA synthetase (M.tb LeuRS). It has IC 50 and Kd values of 0.06 μM and 0.075 μM, respectively, for M.tb LeuRS. Additionally, LeuRS-IN-1 hydrochloride inhibits human cytoplasmic LeuRS with an IC 50 of 38.8 μM and HepG2 protein synthesis with an EC 50 of 19.6 μM.

Virginiamycin S1 is a cyclic hexadepsipeptide antibiotic, inhibits bacterial protein synthesis at the level of aminoacyl-tRNA binding and peptide bond formation.

UAA crosslinker 1 hydrochloride is an amber codon used to incorporate non-canonical amino acids (ncAAs) into proteins in vivo. This is achieved by leveraging the promiscuous activity of specific wildtype and engineered aminoacyl-tRNA synthetases[1].

SB-217452 is a potent seryl tRNA synthetase inhibitor isolated from Streptomyces.

N-Formyl-L-histidine demonstrates a binding affinity for histidyl-tRNA synthetase, featuring a K i value of 4.6 μM. Additionally, it acts as a competitive inhibitor against L-histidine ammonia-lyase, suppressing urocanic acid formation from L-histidine with a K i value of 4.26 mM [1] [2].

2′-O-Methyluridine is a natural product that found in RNA such as rRNA, snRNA, snoRNA and tRNA in Archaea, Bacteria, and Eukaryota.

LeuRS-IN-1 is a highly potent and orally active inhibitor of the leucyl-tRNA synthetase enzyme derived from Mycobacterium tuberculosis (M.tb LeuRS). It exhibits significant inhibitory activity against M.tb LeuRS with IC 50 and Kd values of 0.06 μM and 0.075 μM, respectively. Additionally, LeuRS-IN-1 effectively inhibits human cytoplasmic LeuRS with an IC 50 value of 38.8 μM and suppresses protein synthesis in HepG2 cells with an EC 50 value of 19.6 μM.

L-Methioninamide hydrochloride is a potent inhibitor of methionyl-tRNA synthetase that reduces the toxicity of CDDP.

Borrelidin (Treponemycin) is a bacterial and eukaryal threonyl-tRNA synthetase inhibitor. It is a macrolide antibiotic isolated from Streptomyces rochei.

Spectinomycin dihydrochloride pentahydrate (Spectogard) is an antibiotic produced by Streptomyces spectabilis. It is active against gram-negative bacteria and used for the treatment of gonorrhea.

CRS3123 (REP-3123) dihydrochloride is an orally active, fully synthetic antimicrobial agent that effectively inhibits Clostridioides difficile methionyl-tRNA synthetase (MetRS). CRS3123 dihydrochloride can be used in the study of Clostridioides difficile infection (CDI).

Asp-AMS is a strong competitive inhibitor of the mitochondrial enzyme and also an aspartyl-tRNA synthetase inhibitor.

Chlortetracycline Hydrochloride is a tetracycline with broad-spectrum antibacterial and antiprotozoal activity. Chlortetracycline hydrochloride (Isphamycin) is bacteriostatic and inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit, thereby preventing the addition of amino acids to the growing peptide chain. This tetracycline is active against a wide range of gram-positive and gram-negative organisms, spirochetes, rickettsial species, certain protozoa and Mycoplasma and Chlamydia organisms.

Tetracycline hydrochloride (NCI-c55561) is the hydrochloride salt of the tetracycline, a broad-spectrum naphthacene antibiotic produced semisynthetically from chlortetracycline, an antibiotic isolated from the bacterium Streptomyces aureofaciens. In bacteria, tetracycline blocks binding of aminoacyl-tRNA to the mRNA-ribosome complex, thereby inhibiting protein synthesis and bacterial cell growth. Because naturally, fluorescing tetracycline binds to a newly formed bone at the bone/osteoid interface, tetracycline-labeling of bone and fluorescence microscopy may be used to perform bone histomorphometry.

ThrRS-IN-1 (Compound 30d) is a potent inhibitor of threonyl-tRNA synthetase (ThrRS) from Salmonella enterica (Se ThrRS), exhibiting an IC50 of 1.4 μM and a Kd of 1.36 μM. It uniquely targets both the tRNA Thr and L-threonine binding sites of ThrRS, demonstrating significant antibacterial activities [1].

Antibacterial agent 92, a triple-site aminoacyl-tRNA synthetase (aaRS) inhibitor, demonstrates a potent antibacterial effect by inhibiting Salmonella enterica threonyl-tRNA synthetase (SeThrRS) with an IC50 of 0.58 μM.

T-3861174 is a prolyl tRNA synthetase (PRS) inhibitor, exhibiting significant in vitro anti-tumor activity with GCN2-ATF4 pathway activation.

T6A (N6-Threonylcarbamoyladenosine) is a ubiquitously conserved nucleoside, which is essential for modification. T6A is found in the tRNA responsible for transporting the ANN codon.

Bederocin (REP8839)is a novel inhibitor of methionyl tRNA synthase (METS) with potent antibacterial activity against clinical isolates of Staphylococcus aureus, Streptococcus pyogenes, and other clinically important Gram-positive bacteria.

Oxytetracycline Hydrochloride (Dalimycin) is a tetracycline derivative produced by Streptomyces rimosus with antimicrobial activity. It interferes with the binding of aminoacyl-tRNA to the mRNA-ribosome complex, resulting in preventing peptide elongation and inhibiting protein synthesis.

DS86760016 is a highly effective inhibitor of leucyl-tRNA synthetase (LeuRS), demonstrating potent activity against multidrug-resistant (MDR) Gram-negative bacteria including Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa. Notably, DS86760016 effectively inhibits LeuRS enzymes derived from Escherichia coli, Pseudomonas aeruginosa, and Acinetobacter baumannii, exhibiting IC50 values of 0.38 μM, 0.62 μM, and 0.16 μM, respectively.

N2,N2-Dimethylguanosine is an urinary nucleoside. The mean levels of urinary N2,N2-Dimethylguanosine in patients with colorectal cancer are significantly higher than those in patients with intestinal villous adenoma or healthy adults.

Clindamycin (Sobelin) dissociates peptidyl-tRNA from the bacterial ribosome, thereby disrupting bacterial protein synthesis. Clindamycin is a semisynthetic broad-spectrum antibiotic produced by chemical modification of the parent compound lincomycin.

Epetraborole is a potent and selective leucyl-tRNA synthetase inhibitor. Epetraborole was in development for the treatment of infections caused by multidrug-resistant Gram-negative pathogens.

Demeclocycline calcium is a semisynthetic tetracycline antibiotic which was derived from a strain of Streptomyces aureofaciens. Demeclocycline binds to bacterial 30S ribosomal subunit and prevents binding of aminoacyl-tRNA to the mRNA-ribosome complex, thereby inhibiting protein synthesis. Demeclocycline also inhibits the effect of vasopressin on the renal tubules, thereby causing diuresis.

Bersiporocin, a prolyl-tRNA synthetase inhibitor, demonstrates potent activity with an IC50 of ≤100 nM against phosphoribosylpyrophosphate synthetase (PRS). This compound proves valuable for antifibrotic research.

Halofuginone hydrobromide (RU-19110), a derivative of Febrifugine, functions as a competitive inhibitor of prolyl-tRNA synthetase, displaying a K_i value of 18.3 nM. This compound effectively inhibits type-I collagen synthesis, providing therapeutic benefits in osteoarthritis (OA) by impeding TGF-β signaling. Additionally, it serves as a potent pulmonary vasodilator, mainly through the activation of Kv channels and the inhibition of various calcium channels including voltage-gated, receptor-operated, and store-operated ones. Beyond its vascular effects, Halofuginone hydrobromide exhibits a broad spectrum of biological activities, including anti-malarial, anti-inflammatory, anti-cancer, and anti-fibrotic properties, supported by multiple studies [1] [2] [3] [4] [5].

Tigecycline (GAR-936) is a broad-spectrum glycylcycline antibiotic derived from tetracycline. Tigecycline binds to the 30S ribosomal subunit, thereby interfering with the binding of aminoacyl-tRNA to the mRNA-ribosome complex.

Antibacterial agent 111 (Compound 3) exhibits potent antibacterial activity against B. cereus and K. pneumonia, with MIC values of 3.90 μg/mL and 0.49 μg/mL, respectively. It achieves this antibacterial effect by strongly binding to specific residues of tyrosyl-tRNA synthetase [1].

eukaryotic translation elongation factor 1 alpha 1 (EEF1A1) encodes an isoform of the alpha subunit of the elongation factor-1 complex, which is responsible for the enzymatic delivery of aminoacyl tRNAs to the ribosome. This isoform (alpha 1) is expressed