Proteins > Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha

Page last updated: 2024-08-07 16:45:32

Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha

A protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha that is encoded in the genome of human. [PRO:DNx, UniProtKB:P49354]

Synonyms

EC 2.5.1.58;
EC 2.5.1.59;
CAAX farnesyltransferase subunit alpha;
FTase-alpha;
Ras proteins prenyltransferase subunit alpha;
Type I protein geranyl-geranyltransferase subunit alpha;
GGTase-I-alpha

Research

Bioassay Publications (54)

Timeframe	Studies on this Protein(%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	12 (22.22)	18.2507
2000's	28 (51.85)	29.6817
2010's	14 (25.93)	24.3611
2020's	0 (0.00)	2.80

Compounds (30)

Drugs with Inhibition Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
1,10-phenanthroline	Homo sapiens (human)	IC50	4,000.0000	1	1
2,2'-dipyridyl	Homo sapiens (human)	IC50	100,000.0000	1	1
ethylenediamine	Homo sapiens (human)	IC50	15,500.0000	1	1
cortisone acetate	Homo sapiens (human)	IC50	14.0000	1	1
gliotoxin	Homo sapiens (human)	IC50	32.7000	3	3
sch 37370	Homo sapiens (human)	IC50	27.0000	1	1
desloratadine	Homo sapiens (human)	IC50	65.0000	1	1
b 581	Homo sapiens (human)	IC50	50.0000	1	1
r115777	Homo sapiens (human)	IC50	0.0044	1	2
lonafarnib	Homo sapiens (human)	IC50	36.7965	15	15
tipifarnib	Homo sapiens (human)	IC50	6.4557	11	11
l 778,123	Homo sapiens (human)	IC50	7.3082	14	14
halenaquinone	Homo sapiens (human)	IC50	0.9300	2	2
fti 276	Homo sapiens (human)	IC50	0.0067	14	14
lb42908	Homo sapiens (human)	IC50	5.3344	3	3
a 228839	Homo sapiens (human)	IC50	0.0011	2	2
bms 214662	Homo sapiens (human)	IC50	0.3617	10	10
fti 277	Homo sapiens (human)	IC50	0.0202	2	2
ggti 286	Homo sapiens (human)	IC50	8.0061	4	4
chaetomellic acid a	Homo sapiens (human)	IC50	15.4417	6	6
kurasoin a	Homo sapiens (human)	IC50	59.0000	1	1
kurasoin b	Homo sapiens (human)	IC50	59.0000	1	1
manumycin	Homo sapiens (human)	IC50	11.9000	1	1
clavaric acid	Homo sapiens (human)	IC50	0.8250	2	2
ggti 298	Homo sapiens (human)	IC50	0.0540	1	1
sch 44342	Homo sapiens (human)	IC50	19.5208	12	12
lb42708	Homo sapiens (human)	IC50	0.0008	1	1
actinoplanic acid a	Homo sapiens (human)	IC50	0.2300	1	1
moverastin a	Homo sapiens (human)	IC50	14.7000	1	1

Drugs with Activation Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
l 778,123	Homo sapiens (human)	EC50	3.4460	2	2
farnesyl pyrophosphate	Homo sapiens (human)	Kd	0.0020	1	1
a 228839	Homo sapiens (human)	EC50	0.0160	1	1

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
farnesyl pyrophosphate	Homo sapiens (human)	Km	0.0735	2	2

Enables

This protein enables 8 target(s):

Target	Category	Definition
protein farnesyltransferase activity	molecular function	Catalysis of the reaction: farnesyl diphosphate + protein-cysteine = S-farnesyl protein + diphosphate. [EC:2.5.1.58, PMID:8621375]
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]
Rab geranylgeranyltransferase activity	molecular function	Catalysis of the reaction: 2 geranylgeranyl diphosphate + protein-cysteine = 2 S-geranylgeranyl-protein + 2 diphosphate. This reaction is the formation of two thioether linkages between the C-1 atom of the geranylgeranyl groups and two cysteine residues within the terminal sequence motifs XXCC, XCXC or CCXX. Known substrates include Ras-related GTPases of a single family and the Rab family. [EC:2.5.1.60, GOC:mah, PMID:8621375]
protein binding	molecular function	Binding to a protein. [GOC:go_curators]
microtubule binding	molecular function	Binding to a microtubule, a filament composed of tubulin monomers. [GOC:krc]
receptor tyrosine kinase binding	molecular function	Binding to a receptor that possesses protein tyrosine kinase activity. [GOC:mah]
alpha-tubulin binding	molecular function	Binding to the microtubule constituent protein alpha-tubulin. [GOC:jl]
molecular adaptor activity	molecular function	The binding activity of a molecule that brings together two or more molecules through a selective, non-covalent, often stoichiometric interaction, permitting those molecules to function in a coordinated way. [GOC:mtg_MIT_16mar07, GOC:vw]

Located In

This protein is located in 2 target(s):

Target	Category	Definition
cytosol	cellular component	The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl]
plasma membrane	cellular component	The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]

Active In

This protein is active in 1 target(s):

Target	Category	Definition
cytoplasm	cellular component	The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684]

Part Of

This protein is part of 3 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]
microtubule associated complex	cellular component	Any multimeric complex connected to a microtubule. [GOC:jl]
protein farnesyltransferase complex	cellular component	A protein complex that possesses protein farnesyltransferase activity. [GOC:mah]

Involved In

This protein is involved in 8 target(s):

Target	Category	Definition
transforming growth factor beta receptor signaling pathway	biological process	The series of molecular signals initiated by an extracellular ligand binding to a transforming growth factor beta receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:BHF, GOC:mah, GOC:signaling]
protein farnesylation	biological process	The covalent attachment of a farnesyl group to a protein. [GOC:jl]
protein geranylgeranylation	biological process	The covalent attachment of a geranylgeranyl group to a protein. [GOC:jl]
positive regulation of Rac protein signal transduction	biological process	Any process that activates or increases the frequency, rate or extent of Rac protein signal transduction. [GOC:bf]
skeletal muscle acetylcholine-gated channel clustering	biological process	The accumulation of acetylcholine-gated cation channels in a narrow, central region of muscle fibers, in apposition to nerve terminals. [GOC:bf, GOC:dsf, PMID:19285469]
positive regulation of tubulin deacetylation	biological process	Any process that increases the frequency, rate or extent of tubulin deacetylation. Tubulin deacetylation is the removal of an acetyl group from a protein amino acid. [GOC:BHF, GOC:dph, GOC:tb]
positive regulation of deacetylase activity	biological process	Any process that activates or increases the frequency, rate or extent of deacetylase activity, the catalysis of the hydrolysis of an acetyl group or groups from a substrate molecule. [GOC:BHF, GOC:dph, GOC:tb]
positive regulation of skeletal muscle acetylcholine-gated channel clustering	biological process	Any process that activates or increases the frequency, rate or extent of skeletal muscle acetylcholine-gated channel clustering. [GO_REF:0000058, GOC:TermGenie, PMID:7722643]