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MicroRNAs (miRNAs) are a naturally occurring class of small (approximately 22 nucleotides long) non-coding RNAs that regulate post-transcriptional gene expression to control cellular processes, development, cell differentiation, and homeostasis. MicroRNAs are essential for embryo, cell, and tissue development, regulating cell differentiation, proliferation, and apoptosis, hence their importance in human reproduction. Meanwhile, abnormal expression or function of miRNAs are found to be closely associated with the occurrence or development of various human diseases, including cancers. In light of their significant roles in physiology and pathology, miRNAs are emerging as novel biomolecular targets for chemical-biological studies, including regulation and detection.
Multiple steps are involved in the generation of miRNAs. Most miRNAs are produced by the canonical biogenesis pathway, which involves transcription by RNA polymerase II to make a primary transcript (pri-miRNA) and cleavage by the microprocessor complex to yield a hairpin precursor miRNA (pre-miRNA) in the nucleus. The pre-miRNA is then exported into the cytoplasm, where cleavage by the enzyme Dicer creates a double-stranded RNA duplex. Only a single strand from the double-stranded RNA duplex forms the mature miRNA and is incorporated into the RNA-induced silencing complex (RISC), which guides the binding of Argonaute (AGO) proteins in the RISC to the 3’untranslated region (UTR) to either repress protein translation or promote mRNA degradation. In addition to canonical miRNA biogenesis pathways, non-canonical microprocessor-independent or Dicer-independent miRNA biogenesis pathways also exist. Despite miRNAs being mostly involved in the down-regulation of gene expression, there are reports of miRNAs promoting gene expression.
In addition, relationships between miRNAs and their targets are not always one-to-one in a specific cell type. In fact, a single miRNA may regulate many mRNA targets, and conversely, a single mRNA target also can be regulated by many miRNAs.
Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells.
Cl-amidine hydrochloride is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine hydrochloride induces apoptosis in cancer cells. Cl-amidine hydrochloride induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine hydrochloride prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model.
Guanosine 5'-triphosphate (5'-GTP) trisodium salt is a G protein (G proteins) signaling activator and a high-energy precursor in the biosynthesis of nucleotide units in DNA and RNA. Guanosine 5'-triphosphate trisodium salt can promote myogenic cell differentiation by upregulating miRNA (miR133a, miR133b) and myogenic regulatory factor expression, and by inducing human myogenic precursor cells to release exosomes containing guanosine molecules. Guanosine-5'-triphosphate disodium salt holds promise for research in biosynthesis and skeletal muscle regeneration.
Diosgenin, a steroidal saponin, can inhibit STAT3 signaling pathway. Diosgenin is an exogenous activator of Pdia3/ERp57. Diosgenin inhibits aortic atherosclerosis progression by suppressing macrophage miR-19b expression.
Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway. Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM. Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC50 of 0.47 µM.
Miravirsen sodium is a potent miR-122 inhibitor and inhibits the biogenesis of miR-122. Miravirsen sodium is a 15-nucleotide locked nucleic acid-modified phosphorothioate antisense oligonucleotide. Miravirsen sodium inhibits HCV replication, and can be used in research of HCVinfection.
hsa-miR-24-3p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
RGLS4326 sodium is a first-in-class, short oligonucleotide inhibitor of microRNA-17 (miR-17). RGLS4326 sodium can be used for the research of autosomal dominant polycystic kidney disease (ADPKD). RGLS4326 sodium inhibits miR-17 function in HeLa cells with an EC50 value of 28.3 nM.
MicroRNA Mimic Negative Control is a miRNA mimic of 21-nucleotides, and can be used as a negative control. The sequence of MicroRNA Mimic Negative Control is derived from cel-mir-239b. It has minimal sequence identity with miRNAs in human, mouse, and rat.
RGLS4326 (RG4326) is a first-in-class, short oligonucleotide inhibitor of microRNA-17 (miR-17). RGLS4326 can be used for the research of autosomal dominant polycystic kidney disease (ADPKD). RGLS4326 inhibits miR-17 function in HeLa cells with an EC50 value of 28.3 nM.
PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor (API-1) with an IC50 of 72.3 nM. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase (PPIase) domain and potently inhibits Pin1cis-trans isomerizing activity. PIN1 inhibitor API-1 retains the active conformation of pXPO5 and restores the ability of pXPO5 to transport pre-miRNAs from nucleus to cytoplasm, thus up-regulating the anticancer miRNA biogenesis to suppress both in vitro and in vivo hepatocellular carcinoma development.
MicroRNA Inhibitor Negative Control is a full-length nucleotide 2'-methoxy modified oligonucleotide, and can be used as a negative control. The sequence of MicroRNA Inhibitor Negative Control is derived from cel-mir-239b. It has minimal sequence identity with miRNAs in human, mouse, and rat.
Enoxacin hydrate (Enoxacin sesquihydrate), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 μg/ml) and topoisomerase IV (IC50=26.5 μg/ml). Enoxacin hydrate is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin hydrate has potent activities against gram-positive and -negative bacteria. Enoxacin hydrate is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing.
MicroRNA Antagomir Negative Control is a chemically-modified oligonucleotide (2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification), and can be used as a negative control. The sequence of MicroRNA Antagomir Negative Control is derived from cel-mir-239b. It has minimal sequence identity with miRNAs in human, mouse, and rat.
LIN28 inhibitor LI71 is a potent and cell-permeable LIN28 inhibitor, which abolishes LIN28-mediated oligouridylation with an IC50 of 7 uM. LIN28 inhibitor LI71 directly binds the cold shock domain (CSD) to suppress LIN28’s activity against let-7 in leukemia cells and embryonic stem cells.
Pseudoprotodioscin, a furostanoside, inhibits SREBP1/2 and microRNA 33a/b levels and reduces the gene expression regarding the synthesis of cholesterol and triglycerides.
Targapremir-210 (TGP-210) is a potent and selective miR-210 (miRNA-210, microRNA-210) inhibitor. Targapremir-210 inhibits pre-miR-210 processing with high binding affinity (Kd~200 nM). Targapremir-210 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
hsa-miR-21-5p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
mmu-miR-155-5p mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
hsa-miR-21-5p mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
