Page last updated: 2024-11-12
tubulysin a
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
tubulysin A: has both antiangiogenic and antineoplastic activities; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 12134544 |
| CHEMBL ID | 256922 |
| CHEBI ID | 80034 |
| SCHEMBL ID | 12219629 |
| MeSH ID | M0498637 |
Synonyms (20)
| Synonym |
|---|
| tubulysin a |
| tubulysin-a |
| CHEMBL256922 |
| chebi:80034 , |
| 205304-86-5 |
| tuba |
| HY-15995 |
| SCHEMBL12219629 |
| DTXSID90478254 |
| tubulysin a, >=95% (hplc), from streptomyces sp., film |
| J-013387 |
| NCGC00485650-01 |
| benzenepentanoic acid, .gamma.-(((2-((1r,3r)-1-(acetyloxy)-4-methyl-3-(((2s,3s)-3-methyl-2-((((2r)-1-methyl-2-piperidinyl)carbonyl)amino)-1-oxopentyl)((3-methyl-1-oxobutoxy)methyl)amino)pentyl)-4-thiazolyl)carbonyl)amino)-4-hydroxy-.alpha.-methyl-, (.alph |
| Q27149181 |
| unii-x9rp3ade9z |
| x9rp3ade9z , |
| benzenepentanoic acid, gamma-(((2-((1r,3r)-1-(acetyloxy)-4-methyl-3-(((2s,3s)-3-methyl-2-((((2r)-1-methyl-2-piperidinyl)carbonyl)amino)-1-oxopentyl)((3-methyl-1-oxobutoxy)methyl)amino)pentyl)-4-thiazolyl)carbonyl)amino)-4-hydroxy-alpha-methyl-, (.alp |
| (2s,4r)-4-[[2-[(1r,3r)-1-acetyloxy-4-methyl-3-[3-methylbutanoyloxymethyl-[(2s,3s)-3-methyl-2-[[(2r)-1-methylpiperidine-2-carbonyl]amino]pentanoyl]amino]pentyl]-1,3-thiazole-4-carbonyl]amino]-5-(4-hydroxyphenyl)-2-methylpentanoic acid |
| tubulysin a,tuba |
| EX-A5466B |
Research Excerpts
Overview
Tubulysin A (tubA) is a natural product isolated from a strain of myxobacteria. It has been shown to depolymerize microtubules and induce mitotic arrest.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Tubulysin A (tubA) is a natural product isolated from a strain of myxobacteria that has been shown to depolymerize microtubules and induce mitotic arrest. " | ( Biological evaluation of tubulysin A: a potential anticancer and antiangiogenic natural product. Agarwal, S; Camalier, RF; Dömling, A; Holbeck, S; Hollingshead, M; Kaur, G; Schauer-Vukasinović, V, 2006) | 2.08 |
| "Tubulysin A is a highly cytotoxic peptide with antimitotic activity that induces depletion of cell microtubules and triggers the apoptotic process. " | ( Mechanism of action of tubulysin, an antimitotic peptide from myxobacteria. Elnakady, YA; Khalil, MW; Lünsdorf, H; Reichenbach, H; Sasse, F, 2006) | 1.78 |
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Drug Classes (2)
| Class | Description |
|---|---|
| diester | A diester is a compound containing two ester groups. |
| carboxylic acid | A carbon oxoacid acid carrying at least one -C(=O)OH group and having the structure RC(=O)OH, where R is any any monovalent functional group. Carboxylic acids are the most common type of organic acid. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
Bioassays (6)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID331686 | Inhibition of rat brain tubulin polymerization | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9 | Tubulysin analogs incorporating desmethyl and dimethyl tubuphenylalanine derivatives. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (18)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 7 (38.89) | 29.6817 |
| 2010's | 8 (44.44) | 24.3611 |
| 2020's | 3 (16.67) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 19.28
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (19.28) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (5.26%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 18 (94.74%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||