Table 1.
No | PDB ID |
Year | GEF | SmallG | GEF | Reso | Ligand *1 | Disorder *2 (p,sw1,sw2) | HVR *3 |
---|---|---|---|---|---|---|---|---|---|
1 | 1LFD | 1998 | RALGDS | H-Ras | RasGEF | 2.1 | GNP | no, no, no | no |
2 | 1BKD | 1998 | SOS1 | H-Ras | RasGEF | 2.8 | no, no, no | no | |
3 | 1NVU | 2000 | SOS1 | H-Ras | RasGEF | 2.2 | no, no, no | no | |
4 | 1NVV | 2003 | SOS1 | H-Ras | RasGEF | 2.2 | GNP | no, no, no | no |
5 | 1NVW | 2003 | SOS1 | H-Ras | RasGEF | 2.7 | GNP | no, no, no | no |
6 | 1NVX | 2003 | SOS1 | H-Ras | RasGEF | 3.2 | GTP | no, no, no | no |
7 | 1XD2 | 2004 | SOS1 | H-Ras | RasGEF | 2.7 | GDP | no, no, no | no |
8 | 3CF6 | 2008 | Epac2 | Rap1B | RapGEF | 2.2 | SO4 | no, no, no | no |
9 | 4NYJ | 2014 | SOS1 | H-Ras | RasGEF | 2.9 | GNP | no, no, no | no |
10 | 4NYM | 2014 | SOS1 | H-Ras | RasGEF | 3.6 | no, no, no | no | |
11 | 4MGI | 2014 | Epac | Rap1b | RapGEF | 2.8 | SO4 | no, no, no | no |
12 | 4MGK | 2014 | Epac | Rap1b | RapGEF | 2.7 | SO4 | no, no, no | no |
13 | 4MGY | 2014 | Epac | Rap1b | RapGEF | 2.6 | SO4 | no, no, no | no |
14 | 4MGZ | 2014 | Epac | Rap1b | RapGEF | 3.0 | SO4 | no, no, no | no |
15 | 4MH0 | 2014 | Epac | Rap1b | RapGEF | 2.4 | SO4 | no, no, no | no |
16 | 4URU | 2015 | SOS1 | H-Ras | RasGEF | 2.8 | no, no, no | no | |
17 | 4URV | 2015 | SOS1 | H-Ras | RasGEF | 2.6 | no, no, no | no | |
18 | 4URW | 2015 | SOS1 | H-Ras | RasGEF | 2.8 | no, no, no | no | |
19 | 4URX | 2015 | SOS1 | H-Ras | RasGEF | 2.5 | no, no, no | no | |
20 | 4URY | 2015 | SOS1 | H-Ras | RasGEF | 2.5 | no, no, no | no | |
21 | 4URZ | 2015 | SOS1 | H-Ras | RasGEF | 2.2 | no, no, no | no | |
22 | 4US0 | 2015 | SOS1 | H-Ras | RasGEF | 2.2 | no, no, no | no | |
23 | 4US1 | 2015 | SOS1 | H-Ras | RasGEF | 2.7 | L71 | no, no, no | no |
24 | 4US2 | 2015 | SOS1 | H-Ras | RasGEF | 2.5 | L71 | no, no, no | no |
25 | 5CM8 | 2015 | Rlf (Rgl2) | RalA | RalGEF | 2.6 | no, no, no | no | |
26 | 6AXG | 2017 | RasGRP4 | H-Ras | RasGEF | 3.3 | no, yes, no | no | |
27 | 6AXF | 2017 | RasGRP | Rap1b | RapGEF | 3.1 | no, no, no | no | |
28 | 6D55 | 2018 | SOS1 | H-Ras | RasGEF | 1.7 | Na, FMT, GOL, Mg, GNP, FWA | no, no, no | no |
29 | 6D5W | 2018 | SOS1 | H-Ras | RasGEF | 2.5 | FVV, Mg, GNP | no, no, no | no |
30 | 6D56 | 2018 | SOS1 | H-Ras | RasGEF | 1.7 | Na, FMT, GOL, Mg, GNP, FVN | no, no, no | no |
31 | 6D59 | 2018 | SOS1 | H-Ras | RasGEF | 1.7 | Na, FMT, GOL, Mg, GNP, FVJ | no, no, no | no |
32 | 6D5E | 2018 | SOS1 | H-Ras | RasGEF | 1.8 | Na, FMT, GOL, Mg, GNP, FVG, CL | no, no, no | no |
33 | 6D5G | 2018 | SOS1 | H-Ras | RasGEF | 1.9 | FMT, GOL, Mg, GNP, FVD, Cl, BME | no, no, no | no |
34 | 6D5H | 2018 | SOS1 | H-Ras | RasGEF | 1.8 | FMT, GOL, MG, GNP, FV7, Cl | no, no, no | no |
35 | 6D5J | 2018 | SOS1 | H-Ras | RasGEF | 1.8 | Na, FMT, GOL, MG, GNP, FV4 | no, no, no | no |
36 | 6D5L | 2018 | SOS1 | H-Ras | RasGEF | 1.7 | Na, FMT, GOL, MG, GNP, FW7 | no, no, no | no |
37 | 6D5V | 2018 | SOS1 | H-Ras | RasGEF | 2.0 | Mg, GNP, FVY | no, no, no | no |
38 | 6D5M | 2018 | SOS1 | H-Ras | RasGEF | 2.1 | Mg, GNP, FW4 | no, no, no | no |
39 | 5WFO | 2018 | SOS1 | H-Ras | RasGEF | 2.0 | Mg, GNP, 5UU | no, no, no | no |
40 | 5WFP | 2018 | SOS1 | H-Ras | RasGEF | 2.1 | Mg, GNP, 5UX | no, no, no | no |
41 | 5WFQ | 2018 | SOS1 | H-Ras | RasGEF | 2.3 | Mg, GNP, 5UV | no, no, no | no |
42 | 5WFR | 2018 | SOS1 | H-Ras | RasGEF | 2.5 | Mg, GNP, 5UW | no, no, no | no |
43 | 6BVI | 2018 | SOS1 | H-Ras | RasGEF | 1.8 | NA, FMT, EC4, GOL, Mg, GNP | no, no, no | no |
44 | 6BVJ | 2018 | SOS1 | H-Ras | RasGEF | 1.7 | NA, FMT, EAS, GOL, Mg, GNP | no, no, no | no |
45 | 6BVK | 2018 | SOS1 | H-Ras | RasGEF | 1.8 | NA, FMT, EAV, GOL, Mg, GNP | no, no, no | no |
46 | 6BVL | 2018 | SOS1 | H-Ras | RasGEF | 1.7 | NA, FBY, EAV, GOL, Mg, GNP | no, no, no | no |
47 | 6BVM | 2018 | SOS1 | H-Ras | RasGEF | 1.8 | NA, FBY, EBV, GOL, Mg, GNP | no, no, no | no |
48 | 6EPL | 2019 | SOS1 | K-Ras | RasGEF | 2.6 | GOL | no, no, no | no |
49 | 6EPM | 2019 | SOS1 | K-Ras | RasGEF | 2.5 | BQ5, GOL | no, no, no | no |
50 | 6EPN | 2019 | SOS1 | K-Ras | RasGEF | 2.5 | BQ2, DMS, GOL | no, no, no | no |
51 | 6EPO | 2019 | SOS1 | K-Ras | RasGEF | 2.4 | GOL, BPW | no, no, no | no |
52 | 6EPP | 2019 | SOS1 | K-Ras | RasGEF | 2.4 | GOL, BOQ | no, no, no | no |
53 | 1LB1 | 2002 | Dbs (Mcf21) | RhoA | RhoGEF | 2.8 | no, no, no | no | |
54 | 1 × 86 | 2004 | ARHGEF12 | RhoA | RhoGEF | 3.2 | PO4 | no, no, no | no |
55 | 1XCG | 2004 | ARHGEF11 (PDZ-rhoGEF) | RhoA | RhoGEF | 2.5 | no, no, no | no | |
56 | 2RGN | 2007 | ARHGEF25 (p63RhoGEF) |
RhoA | RhoGEF | 3.5 | no, no, no | no | |
57 | 3KZ1 | 2010 | ARHGEF11 (PDZ-rhoGEF) | RhoA | RhoGEF | 2.7 | GSP | no, no, no | no |
58 | 3LW8 | 2010 | IpgB2 | RhoA | RhoGEF | 1.9 | GDP | no, no, no | no |
59 | 3LWN | 2010 | IpgB2 | RhoA | RhoGEF | 2.3 | GDP | no, no, no | no |
60 | 3LXR | 2010 | IpgB2 | RhoA | RhoGEF | 1.7 | GDP | no, no, no | no |
61 | 3T06 | 2011 | ARHGEF11 (PDZ-rhoGEF) | RhoA | RhoGEF | 2.8 | no, no, no | no | |
62 | 4D0N | 2014 | AKAP13 | RhoA | RhoGEF | 2.1 | GDP | no, no, no | no |
63 | 4XH9 | 2015 | NET1 (ARHGEF8) | RhoA | RhoGEF | 2.0 | no, yes, no | no | |
64 | 6BC0 | 2017 | ARHGEF28 (p190RhoGEF) |
RhoA | RhoGEF | 2.2 | GSP | no, no, no | no |
65 | 5JHG | 2017 | ARHGEF11 | RhoA | RhoGEF | 2.5 | GOL | no, no, no | no |
66 | 6BCA | 2017 | ARHGEF18 (LbcRhoGEF) |
RhoA | RhoGEF | 2.0 | GSP | no, no, no | no |
67 | 6BCB | 2017 | ARHGEF18 (p114RhoGEF) |
RhoA | RhoGEF | 1.4 | GSP | no, no, no | no |
68 | 5JHH | 2017 | ARHGEF11 | RhoA | RhoGEF | 2.3 | RAO | no, no, no | no |
69 | 5ZHX | 2018 | SmgGDS | RhoA | RhoGEF | 3.5 | yes, yes, yes | yes | |
70 | 1FOE | 2000 | Tiam | Rac1 | RhoGEF | 2.8 | SO4 | no, no, no | no |
71 | 2NZ8 | 2007 | Trio | Rac1 | RhoGEF | 2.0 | no, no, no | no | |
72 | 2VRW | 2008 | Vav1 | Rac1 | RhoGEF | 1.9 | no, no, no | no | |
73 | 2YIN | 2011 | DOCK2 | Rac1 | RhoGEF | 2.7 | no, no, no | no | |
74 | 3B13 | 2012 | DOCK2 | Rac1 | RhoGEF | 3.0 | no, no, no | no | |
75 | 3BJI | 2007 | Vav1 | Rac1 | RhoGEF | 2.6 | no, no, no | no | |
76 | 4YON | 2015 | P-Rex1 | Rac1 | RhoGEF | 2.0 | no, no, no | no | |
77 | 5FI0 | 2016 | P-Rex1 | Rac1 | RhoGEF | 3.3 | no, no, no | yes | |
78 | 5O33 | 2017 | Kalirin | Rac1 | RhoGEF | 1.6 | GDP | no, no, no | no |
79 | 6BC1 | 2018 | ARHGEF28 (p190RhoGEF) |
Rac1 | RhoGEF | 2.9 | GSP | no, no, no | no |
80 | 1KZ7 | 2002 | Dbs (Mcf2l) | Cdc42 | RhoGEF | 2.4 | no, no, no | no | |
81 | 1GZS | 2002 | SOPE | Cdc42 | RhoGEF | 2.3 | PO4 | no, no, no | no |
82 | 1KI1 | 2002 | ITSN1 | Cdc42 | RhoGEF | 2.3 | PO4 | no, no, no | no |
83 | 1KZG | 2002 | Mcf2l (Dbs) | Cdc42 | RhoGEF | 2.6 | no, no, no | no | |
84 | 2DFK | 2006 | ARHGEF9 (Collybistin II) |
Cdc42 | RhoGEF | 2.2 | PO4 | no, no, no | yes |
85 | 2WM9 | 2009 | DOCK9 | Cdc42 | RhoGEF | 2.2 | GOL | no, no, no | no |
86 | 2WMN | 2009 | DOCK9 | Cdc42 | RhoGEF | 2.4 | GDP | no, no, no | no |
87 | 2WMO | 2009 | DOCK9 | Cdc42 | RhoGEF | 2.2 | GDP | no, no, no | no |
88 | 3GCG | 2009 | map (L0028) | Cdc42 | RhoGEF | 2.3 | no, yes, no | no | |
89 | 3QBV | 2012 | ITSN1 | Cdc42 | RhoGEF | 2.7 | GDP | no, yes, no | no |
90 | 3VHL | 2012 | DOCK8 | Cdc42 | RhoGEF | 2.1 | PO4 | no, no, no | no |
91 | 6AJ4 | 2019 | DOCK7 | Cdc42 | RhoGEF | 3.2 | no, no, no | yes | |
92 | 6AJL | 2019 | DOCK7 | Cdc42 | RhoGEF | 3.2 | no, no, no | yes | |
93 | 3CX6 | 2008 | ARHGEF11 (PDZRhoGEF) |
Galpha-13 | RhoGEF | 2.5 | GDP | no, no, no | no |
94 | 3CX7 | 2008 | ARHGEF11 (PDZRhoGEF) |
Galpha-13 | RhoGEF | 2.3 | GSP | no, no, no | no |
95 | 3CX8 | 2008 | ARHGEF11 (PDZRhoGEF) |
Galpha-13 | RhoGEF | 2.5 | GDP | no, no, no | no |
96 | 1SHZ | 2005 | ARHGEF1 (p115RhoGEF) |
Gnai1,13 | RhoGEF | 2.9 | GDP+ALF | no, no, no | no |
97 | 2NTY | 2007 | ROPGEF8 | ROP4 | RopGEF | 3.1 | GDP | no, yes, no | no |
98 | 2WBL | 2009 | ROPGEF8 | ROP7 | RopGEF | 2.9 | no, yes, no | no | |
99 | 2WWX | 2009 | SidM/DrrA | Rab1 | RabGEF | 1.5 | no, no, no | no | |
100 | 3L0I | 2010 | SidM/DrrA | Rab1 | RabGEF | 2.9 | SO4 | no, no, no | no |
101 | 3JZA | 2010 | DrrA/SidM | Rab1b | RabGEF | 1.8 | PO4 | no, no, no | no |
102 | 5O74 | 2017 | DrrA/SidM | Rab1b | RabGEF | 2.5 | GDP | no, yes, yes | no |
103 | 2OT3 | 2007 | Rabex-5 (RabGEF1) |
Rab21 | RabGEF | 2.1 | no, yes, no | no | |
104 | 3TW8 | 2011 | DENND1B | Rab35 | RabGEF | 2.1 | no, yes, no | no | |
105 | 4Q9U | 2014 | Rabex-5 (RabGEF1) |
Rab5A | RabGEF | 4.6 | yes, yes, no | no | |
106 | 2FU5 | 2006 | MSS4 | Rab8A | RabGEF | 2.0 | no, yes, yes | no | |
107 | 4LHX | 2013 | RAB3IP (Rabin8) | Rab8A | RabGEF | 3.1 | SO4 | no, no, no | no |
108 | 4LHY | 2013 | RAB3IP (Rabin8) | Rab8A | RabGEF | 3.1 | GDP | no, no, no | no |
109 | 4LHZ | 2013 | RAB3IP (Rabin8) | Rab8A | RabGEF | 3.2 | GTP | no, no, no | no |
110 | 4LI0 | 2013 | RAB3IP (Rabin8) | Rab8A | RabGEF | 3.3 | GDP | no, no, no | no |
111 | 2EFD | 2010 | AtVps9a | Ara7 (RabF2B) |
RabGEF | 3.0 | no, yes, no | no | |
112 | 2EFE | 2010 | AtVps9a | Ara7 (RabF2B) |
RabGEF | 2.1 | GDP | no, no, no | no |
113 | 2EFH | 2010 | AtVps9a | Ara7 (RabF2B) |
RabGEF | 2.1 | GDP | no, yes, no | no |
114 | 2EFC | 2010 | AtVps9a | Ara7 (RabF2B) |
RabGEF | 2.1 | GDP | no, no, no | no |
115 | 4G01 | 2013 | Vps9a | Ara7 (RabF2B) |
RabGEF | 2.2 | GDP | no, no, no | no |
116 | 2OCY | 2007 | Sec2p | Sec4p | RabGEF | 3.3 | GDP | no, no, no | no |
117 | 2EQB | 2007 | Sec2p | Sec4p | RabGEF | 2.7 | no, no, no | no | |
118 | 4ZDW | 2015 | Sec2p | Sec4p | RabGEF | 2.9 | no, no, no | no | |
119 | 3CUE | 2008 | TRAPPI assembly | Ypt1p | RabGEF | 3.7 | no, yes, no | no | |
120 | 5LDD | 2017 | Mon1-Ccz1 | Ypt7 | RabGEF | 2.5 | SO4 | no, no, no | no |
121 | 6IXV | 2019 | SH3BP5 | Rab11 | RabGEF | 3.8 | PO4 | no, no, no | no |
122 | 6EKK | 2019 | DENND 1A | Rab35 | RabGEF | 1.8 | GDP, SO4, EDO | no, no, no | no |
123 | 6DJL | 2019 | SH3BP5 | Rab11 | RabGEF | 3.1 | no, no, no | no | |
124 | 1RE0 | 2003 | GEA1 | ARF1 | ArfGEF | 2.4 | GDP | no, no, no | no |
125 | 1R8Q | 2003 | CYTH2 (Arno) | ARF1 | ArfGEF | 1.9 | G3D | no, no, no | no |
126 | 1R8S | 2003 | CYTH2 (Arno) | ARF1 | ArfGEF | 1.5 | GDP | no, no, no | no |
127 | 1S9D | 2003 | CYTH2 (Arno) | ARF1 | ArfGEF | 1.8 | GDP | no, yes, no | no |
128 | 4C0A | 2013 | IQSEC1 | ARF1 | ArfGEF | 3.3 | G3D | no, no, no | no |
129 | 6FAE | 2018 | IQSEC2 | ARF1 | ArfGEF | 2.3 | no, yes, no | no | |
130 | 4KAX | 2013 | CYTH3 | ARF6 | ArfGEF | 1.9 | GTP | no, no, no | no |
131 | 5EE5 | 2016 | ARFGEF1 | ARL1 | ArfGEF | 2.3 | GTP | no, no, no | no |
132 | 5J5C | 2016 | ARFGEF1 | ARL1 | ArfGEF | 3.4 | GTP | no, no, no | no |
133 | 1I2M | 2001 | RCC1 | RAN | RanGEF | 1.8 | SO4 | no, yes, no | no |
*1 The names of the ligands are described below. GNP: phosphoaminophosphonic acid-guanylate ester; L71: (3S)-3-[3-(aminomethyl)phenyl]-1-ethylpyrrolidine-2,5-dione; FMT: formic acid; GOL: glycerol; FWA: 6-chloro-2-(2,6-diazaspiro [3.3]heptan-2-yl)-1-[(4-fluoro-3,5-dimethylphenyl)methyl]-4-(4-methylpiperazin-1-yl)-1H-benzimidazole; FVV: 10-[(4-fluorophenyl)methyl]-2,3,4,10-tetrahydropyrimido [1,2-a]benzimidazole; FVN: 6-chloro-2-(2,6-diazaspiro[3.3]heptan-2-yl)-4-(3,5-dimethyl-1H-pyrazol-4-yl)-1-[(4-fluoro-3,5-dimethylphenyl)methyl]-1H-benzimidazole; FVJ: 6-chloro-4-(3,5-dimethyl-1H-pyrazol-4-yl)-1-[(4-fluoro-3,5-dimethylphenyl)methyl]-2-(piperazin-1-yl)-1H-benzimidazole; FVG: 1-[(2S)-1-{6-chloro-1-[(4-fluoro-3,5-dimethylphenyl)methyl]-2-(piperazin-1-yl)-1H-benzimidazol-4-yl}pyrrolidin-2-yl]methanamine; FVD: 6-chloro-1-[(4-fluoro-3,5-dimethylphenyl)methyl]-2-(piperazin-1-yl)-4-(1,2,3,6-tetrahydropyridin-4-yl)-1H-benzimidazole; BME: beta-mercaptoethanol; FV7: 6-chloro-4-(2-chlorophenyl)-1-[(4-fluoro-3,5-dimethylphenyl)methyl]-2-(piperazin-1-yl)-1H-benzimidazole; FV4: 6-chloro-1-[(4-fluoro-3,5-dimethylphenyl)methyl]-2-(piperazin-1-yl)-1H-benzimidazole; FW7: 6-chloro-1-[(3-chloro-4-fluorophenyl)methyl]-2-(piperazin-1-yl)-1H-benzimidazole; FVY: 1-[(3-chloro-4-fluorophenyl)methyl]-5,6-dimethyl-1H-benzimidazol-2-amine; FW4: 1-[(3-chloro-4-fluorophenyl)methyl]-5,6-dimethyl-2-(piperazin-1-yl)-1H-benzimidazole; 5UU: 6-chloranyl-~{N}-(4-fluorophenyl)-1,2,3,4-tetrahydroacridin-9-amine; 5UX: 6-chloranyl-~{N}-(3-chloranyl-4-fluoranyl-phenyl)-1,2,3,4-tetrahydroacridin-9-amine; 5UV: 7-chloranyl-~{N}-(3-chloranyl-4-fluoranyl-phenyl)-1,2,3,4-tetrahydroacridin-9-amine; 5UW: ~{N}-(3,3-diphenylpropyl)piperidin-4-amine; EC4: 6-chloro-N-{1-[(5-chloro-1H-indol-3-yl)methyl]piperidin-4-yl}-L-tryptophanamide; EAS: 5-chloro-N-{1-[(5-chloro-1H-indol-3-yl)methyl]piperidin-4-yl}-L-tryptophanamide; EAV: N-{1-[(5-chloro-1H-indol-3-yl)methyl]piperidin-4-yl}-6-methyl-L-tryptophanamide; EBY: N-{1-[(5-chloro-1H-indol-3-yl)methyl]piperidin-4-yl}-5-methyl-L-tryptophanamide; EBV: (2S)-2-amino-1-[(3aR,6aS)-5-[(5-chloro-1H-indol-3-yl)methyl]hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl]-3-(1H-indol-3-yl)propan-1-one; BQ5: (1-phenyl-5,6-dihydro-4~{H}-cyclopenta[c]pyrazol-3-yl)methanamine; BQ2: 1-(3,4-dihydro-1~{H}-isoquinolin-2-yl)-2-oxidanyl-ethanone, DMS: dimethyl sulfoxide; BPW: 3-(4-chlorophenyl)propan-1-amine; BOQ: ethyl 2-(aminomethyl)-5-~{tert}-butyl-furan-3-carboxylate; GSP: 5′-guanosine-diphosphate-monothiophosphate; RA0: 3-{3-[ethyl(quinolin-2-yl)amino]phenyl}propanoic acid; ALF: tetrafluoroaluminate ion; EDO: 1,2-ethanediol; G3D: guanosine-3′-monophosphate-5′-diphosphate. *2 Disordered regions among P-loop (p), switch I (sw1), and switch II (sw2) are indicated. “yes” means that the region has a disordered structure. *3 The structure including the hyper variable region (HVR) is indicated as “yes”.