Target type: cellularcomponent
A protein complex which is capable of GTPase activity. [GO_REF:0000088, GOC:bhm, GOC:TermGenie, PMID:9178006]
The GTPase complex is a molecular machine found in various cellular processes, including signal transduction, vesicle trafficking, and cytoskeletal organization. It typically consists of a GTPase protein, which binds and hydrolyzes GTP, and various regulatory proteins that control its activity. The GTPase protein is characterized by a conserved GTP-binding domain that binds to GTP and hydrolyzes it to GDP. This hydrolysis event triggers a conformational change in the GTPase protein, often leading to the recruitment of other proteins and the initiation of downstream signaling cascades. The regulatory proteins associated with the GTPase complex can be: \\n\\n1. **Guanine nucleotide exchange factors (GEFs):** These proteins promote the exchange of GDP for GTP, thus activating the GTPase. \\n\\n2. **GTPase-activating proteins (GAPs):** These proteins accelerate the hydrolysis of GTP to GDP, effectively inactivating the GTPase. \\n\\n3. **Guanine nucleotide dissociation inhibitors (GDIs):** These proteins prevent the dissociation of GDP from the GTPase, thereby keeping it in an inactive state. \\n\\nThe specific composition and function of the GTPase complex vary depending on the cell type and the specific process it is involved in. For example, the Ras GTPase complex, a key player in cell growth and proliferation, typically includes Ras protein, GEF proteins such as Sos, and GAP proteins such as p120GAP. The Rho GTPase complex, involved in cytoskeletal reorganization and cell migration, can include RhoA, RhoB, RhoC, and their respective GEFs and GAPs. In general, the GTPase complex serves as a molecular switch, cycling between an active (GTP-bound) and inactive (GDP-bound) state, allowing for precise regulation of cellular processes. This dynamic interplay of proteins within the complex ensures efficient signal transduction and cellular function.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| GTPase HRas | A GTPase HRas that is encoded in the genome of human. [PRO:DNx, UniProtKB:P01112] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| stallimycin | |||
| lonafarnib | lonafarnib : A 4-{2-[4-(3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidin-1-yl]-2-oxoethyl}piperidine-1-carboxamide that has R configuration. It is used as oral farnesyltransferase inhibitor. lonafarnib: inhibitor of farnesyl protein transferase | 4-{2-[4-(3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidin-1-yl]-2-oxoethyl}piperidine-1-carboxamide | antineoplastic agent; EC 2.5.1.58 (protein farnesyltransferase) inhibitor |
| l 778,123 | L-778,123 (free base) : A member of the class of imidazoles that is 1H-imidazole substituted by (4-cyanophenyl)methyl and [4-(3-chlorophenyl)-3-oxopiperazin-1-yl]methyl groups at positions 1 and 5, respectively. It is a dual inhibitor of FPTase and GGPTase-I. | imidazoles; monochlorobenzenes; nitrile; piperazinone; tertiary amino compound | antineoplastic agent; EC 2.5.1.58 (protein farnesyltransferase) inhibitor; EC 2.5.1.59 (protein geranylgeranyltransferase type I) inhibitor |
| bms 214662 | 7-cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine: a farnesyltransferase inhibitor; structure in first source BMS-214662 : A member of the class of benzodiazepines that is 2,3,4,5-tetrahydro-1H-1,4-benzodiazepine substituted by (1H-imidazol-5-yl)methyl, benzyl, (thiophen-2-yl)sulfonyl, and cyano groups at positions 1, 3R, 4 and 7, respectively. It is a potent inhibitor of farnesyltransferase (IC50 = 1.35nM) which was under clinical development for the treatment of solid tumors. | benzenes; benzodiazepine; imidazoles; nitrile; sulfonamide; thiophenes | antineoplastic agent; apoptosis inducer; EC 2.5.1.58 (protein farnesyltransferase) inhibitor |