## 1-Deazatubercidin: A Promising Research Tool
1-Deazatubercidin is a synthetic nucleoside analog with a fascinating history and promising applications in research. Here's a breakdown of its key features and significance:
**What is it?**
* **Structure:** 1-Deazatubercidin is a modified version of the naturally occurring nucleoside tubercidin. It differs by having a nitrogen atom replaced with a carbon atom at position 1 of the purine base.
* **Chemical Formula:** C12H14N4O4
* **Properties:** It exists as a white solid, soluble in water and various organic solvents.
**Importance in Research:**
1-Deazatubercidin has emerged as a valuable tool for various research areas, primarily due to its:
* **Inhibition of Inosine Monophosphate Dehydrogenase (IMPDH):** This enzyme plays a crucial role in purine biosynthesis. 1-Deazatubercidin acts as a potent inhibitor, preventing the conversion of inosine monophosphate (IMP) to xanthine monophosphate (XMP). This disruption in purine synthesis has implications for various cellular processes.
* **Antiviral Activity:** This inhibition of IMPDH contributes to its antiviral properties. It has shown efficacy against different viruses, including:
* **HIV:** 1-Deazatubercidin has been investigated for its potential in treating HIV infection.
* **Hepatitis C Virus (HCV):** Its antiviral activity against HCV has been explored in research.
* **Anti-Cancer Activity:** 1-Deazatubercidin has shown potential anti-cancer properties in various studies. It has been investigated for its effects on leukemia, lymphoma, and solid tumors. Its mechanism of action in cancer cells is likely linked to its ability to inhibit IMPDH and disrupt purine metabolism.
* **Probing Cellular Processes:** Researchers utilize 1-Deazatubercidin as a tool to understand the roles of purine metabolism and IMPDH in various cellular processes, including:
* **Immune responses:** Its effects on immune cell proliferation and function are being studied.
* **Inflammation:** The role of IMPDH in inflammatory processes is being investigated using 1-Deazatubercidin.
**Current Research:**
While 1-Deazatubercidin holds promise, it is still in the preclinical and research stages. Currently, efforts are focused on:
* **Developing new derivatives:** Researchers are working on synthesizing modified versions of 1-Deazatubercidin with improved properties, such as increased potency or better pharmacokinetic profiles.
* **Exploring its therapeutic potential:** Ongoing research aims to determine its potential as a therapeutic agent for various diseases, including cancer and viral infections.
* **Understanding its cellular mechanisms:** Research efforts are ongoing to elucidate the intricate cellular pathways affected by 1-Deazatubercidin and to identify its precise mechanisms of action.
**Future Prospects:**
1-Deazatubercidin remains a promising candidate for developing novel therapies for various diseases. Its ability to target IMPDH, a crucial enzyme involved in purine metabolism, opens up opportunities for the development of effective antiviral, anti-cancer, and other therapeutic agents. However, further research is needed to fully understand its therapeutic potential and to optimize its use in clinical settings.
1-deazatubercidin: structure given in first source
ID Source | ID |
---|---|
PubMed CID | 128557 |
CHEMBL ID | 4436060 |
SCHEMBL ID | 1473241 |
MeSH ID | M0110360 |
Synonym |
---|
1-deazatubercidin |
83683-90-3 |
(2r,3r,4s,5r)-2-(4-aminopyrrolo[2,3-b]pyridin-1-yl)-5-(hydroxymethyl)oxolane-3,4-diol |
SCHEMBL1473241 |
4-amino-1-beta-d-ribofuranosyl-1h-pyrrolo(2,3-b)pyridine |
1h-pyrrolo(2,3-b)pyridin-4-amine, 1-beta-d-ribofuranosyl- |
DTXSID701003690 |
1-pentofuranosyl-1h-pyrrolo[2,3-b]pyridin-4-amine |
CHEMBL4436060 |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1879379 | Antileishmanial activity against intracellular Leishmania infantum MHOM/MA(BE)/67 amastigotes infected in Swiss mouse peritoneal macrophages assessed as parasite growth inhibition incubated for 5 days by giemsa staining based microscopic analysis | 2022 | European journal of medicinal chemistry, Mar-05, Volume: 231 | N |
AID1616129 | Selectivity index, ratio for EC50 for human MRC5 SV2 cells to EC50 for Trypanosoma cruzi Tulahuen CL2 amastigotes infected in human MRC5 SV2 cells | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19 | Discovery of Pyrrolo[2,3- |
AID1879377 | Antitrypanosomal activity against intracellular Trypanosoma cruzi Tulahuen amastigotes expressing CL2 beta-galactosidase in human MRC5 cells assessed as parasite growth inhibition using chlorophenol red beta-D-galactopyranoside as substrate treated for 7 | 2022 | European journal of medicinal chemistry, Mar-05, Volume: 231 | N |
AID1879381 | Selectivity index, ratio of CC50 for Swiss mouse peritoneal macrophages to EC50 for antileishmanial activity against intracellular Leishmania infantum MHOM/MA(BE)/67 amastigotes infected in Swiss mouse peritoneal macrophages | 2022 | European journal of medicinal chemistry, Mar-05, Volume: 231 | N |
AID1616128 | Antitrypanosomal activity against Trypanosoma cruzi Tulahuen CL2 amastigotes infected in human MRC5 SV2 cells incubated for 7 days by chlorophenol red beta-D-galactopyranoside substrate based spectrophotometric assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19 | Discovery of Pyrrolo[2,3- |
AID1616127 | Cytotoxicity against human MRC5 SV2 cells assessed as reduction in cell viability incubated for 3 days by resazurin dye based assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19 | Discovery of Pyrrolo[2,3- |
AID1879380 | Cytotoxicity against Swiss mouse peritoneal macrophages assessed as reduction in cell viability measured after 5 days by microscopic analysis | 2022 | European journal of medicinal chemistry, Mar-05, Volume: 231 | N |
AID1879378 | Selectivity index, ratio of CC50 for human MRC-5 cells to EC50 for antitrypanosomal activity against intracellular Trypanosoma cruzi Tulahuen amastigotes expressing CL2 beta-galactosidase in human MRC5 cells | 2022 | European journal of medicinal chemistry, Mar-05, Volume: 231 | N |
AID1879375 | Cytotoxicity against human MRC5 fibroblast cells assessed as reduction in cell viability measured after 3 days by fluorometry | 2022 | European journal of medicinal chemistry, Mar-05, Volume: 231 | N |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 2 (50.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 0 (0.00) | 29.6817 |
2010's | 1 (25.00) | 24.3611 |
2020's | 1 (25.00) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 0 (0.00%) | 5.53% |
Reviews | 0 (0.00%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 5 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |