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. 2019 Sep 11;24(18):3308. doi: 10.3390/molecules24183308

Table 1.

GEF:Small GTPase structures.

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”.