Proteins > Geranylgeranyl transferase type-1 subunit beta
Page last updated: 2024-08-07 16:49:54
Geranylgeranyl transferase type-1 subunit beta
A geranylgeranyl transferase type-1 subunit beta that is encoded in the genome of human. [PRO:DNx, UniProtKB:P53609]
Synonyms
EC 2.5.1.59;
Geranylgeranyl transferase type I subunit beta;
GGTase-I-beta;
Type I protein geranyl-geranyltransferase subunit beta
Research
Bioassay Publications (16)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 3 (18.75) | 18.2507 |
| 2000's | 11 (68.75) | 29.6817 |
| 2010's | 2 (12.50) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (11)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| gliotoxin | Homo sapiens (human) | IC50 | 17.0000 | 1 | 1 |
| lonafarnib | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| tipifarnib | Homo sapiens (human) | IC50 | 17.7500 | 4 | 4 |
| l 778,123 | Homo sapiens (human) | IC50 | 24.5738 | 4 | 4 |
| fti 276 | Homo sapiens (human) | IC50 | 0.0500 | 1 | 1 |
| lb42908 | Homo sapiens (human) | IC50 | 16.0000 | 1 | 1 |
| bms 214662 | Homo sapiens (human) | IC50 | 1.8000 | 2 | 2 |
| ggti 286 | Homo sapiens (human) | IC50 | 1.0036 | 2 | 2 |
| chaetomellic acid a | Homo sapiens (human) | IC50 | 92.0000 | 1 | 1 |
| ggti 298 | Homo sapiens (human) | IC50 | 0.0540 | 1 | 1 |
| sch 44342 | Homo sapiens (human) | IC50 | 114.0000 | 2 | 2 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| l 778,123 | Homo sapiens (human) | EC50 | 3.4460 | 2 | 2 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| l 778,123 | Homo sapiens (human) | Inhibition | 0.0980 | 1 | 1 |
| l 778,123 | Homo sapiens (human) | MIC | 1.0000 | 2 | 2 |
Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins.Journal of medicinal chemistry, , 04-26, Volume: 61, Issue:8, 2018
Prenyltransferase Inhibitors: Treating Human Ailments from Cancer to Parasitic Infections.MedChemComm, , Volume: 4, Issue:3, 2013
5-imidazolyl-quinolinones, -quinazolinones and -benzo-azepinones as farnesyltransferase inhibitors.Bioorganic & medicinal chemistry letters, , May-05, Volume: 13, Issue:9, 2003
Substituted azoloquinolines and -quinazolines as new potent farnesyl protein transferase inhibitors.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 13, Issue:24, 2003
Prenyltransferase Inhibitors: Treating Human Ailments from Cancer to Parasitic Infections.MedChemComm, , Volume: 4, Issue:3, 2013
Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.Bioorganic & medicinal chemistry letters, , Feb-09, Volume: 14, Issue:3, 2004
Design, synthesis, and biological activity of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles as potent and selective farnesyltransferase inhibitors.Journal of medicinal chemistry, , Jan-29, Volume: 47, Issue:3, 2004
Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy?Journal of medicinal chemistry, , Apr-08, Volume: 47, Issue:8, 2004
The synthesis and biological evaluation of a series of potent dual inhibitors of farnesyl and geranyl-Geranyl protein transferases.Bioorganic & medicinal chemistry letters, , Aug-05, Volume: 12, Issue:15, 2002
Aryloxy substituted N-arylpiperazinones as dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.Bioorganic & medicinal chemistry letters, , Jun-04, Volume: 11, Issue:11, 2001
Discovery of (R)-7-cyano-2,3,4, 5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent preclinical antitumor activity.Journal of medicinal chemistry, , Oct-05, Volume: 43, Issue:20, 2000
Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins.Journal of medicinal chemistry, , 04-26, Volume: 61, Issue:8, 2018
Potent, highly selective, and non-thiol inhibitors of protein geranylgeranyltransferase-I.Journal of medicinal chemistry, , Apr-22, Volume: 42, Issue:8, 1999
Structure-activity relationship of 3-substituted N-(pyridinylacetyl)-4- (8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene )- piperidine inhibitors of farnesyl-protein transferase: design and synthesis of in vivo active antitumor compJournal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Ras farnesyltransferase: a new therapeutic target.Journal of medicinal chemistry, , Sep-12, Volume: 40, Issue:19, 1997
Enables
This protein enables 4 target(s):
| Target | Category | Definition |
|---|
| protein geranylgeranyltransferase activity | molecular function | Catalysis of the covalent addition of a geranylgeranyl (20-carbon isoprenoid) group via thioether linkages to a cysteine residue at or near the C terminus of a protein. [PMID:8621375] |
| CAAX-protein geranylgeranyltransferase activity | molecular function | Catalysis of the reaction: geranylgeranyl diphosphate + protein-cysteine = S-geranylgeranyl-protein + diphosphate. This reaction is the formation of a thioether linkage between the C-1 atom of the geranylgeranyl group and a cysteine residue fourth from the C-terminus of the protein. The protein substrates have the C-terminal sequence CA1A2X, where the terminal residue, X, is preferably leucine and A2 should not be aromatic. Known substrates include most g-subunits of heterotrimeric G proteins and Ras-related GTPases such as members of the Ras and Rac/Rho families. [EC:2.5.1.59, PMID:8621375] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| zinc ion binding | molecular function | Binding to a zinc ion (Zn). [GOC:ai] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| CAAX-protein geranylgeranyltransferase complex | cellular component | A heterodimeric enzyme, composed of an alpha and a beta subunit. Participates in the post-translational C-terminal modification of several small GTPases, allowing their targeting to the membrane. [PMID:9781874] |
Involved In
This protein is involved in 1 target(s):
| Target | Category | Definition |
|---|
| protein geranylgeranylation | biological process | The covalent attachment of a geranylgeranyl group to a protein. [GOC:jl] |