1,1-Diheterocyclic Ethylenes Derived from Quinaldine and Carbazole as New Tubulin Polymerization Inhibitors: Synthesis, Metabolism, and Biological Evaluation. Determined by X-ray diffraction at 2.75 Å resolution. Released 19 Dec 2018.
Explore 6H9B in 3D Show helices and sheets RCSB PDB PDBe
6H9B contains 116 α-helices and 71 β-strands across 5 chains. Residue ranges use author residue numbering, as in the PDB file, from PDBe. To see them in 3D, choose the Cartoon representation with Secondary structure coloring: helices, sheets and coils get different colors.
| Element | Residues | Length | Sheet |
|---|---|---|---|
| β-strand | 4-9 | 6 | 1 |
| α-helix | 10-28 | 19 | |
| α-helix | 48-51 | 4 | |
| β-strand | 53-55 | 3 | 2 |
| β-strand | 61-63 | 3 | 2 |
| β-strand | 65-69 | 5 | 1 |
| α-helix | 73-80 | 8 | |
| α-helix | 89-91 | 3 | |
| β-strand | 92-94 | 3 | 1 |
| α-helix | 103-104 | 2 | |
| α-helix | 105-109 | 5 | |
| α-helix | 111-127 | 17 | |
| β-strand | 134-140 | 7 | 1 |
| α-helix | 144 | 1 | |
| α-helix | 145-149 | 5 | |
| α-helix | 150-161 | 12 | |
| β-strand | 165-172 | 8 | 1 |
| α-helix | 175-177 | 3 | |
| α-helix | 183-194 | 12 | |
| α-helix | 195-197 | 3 | |
| β-strand | 200-205 | 6 | 1 |
| α-helix | 206-217 | 12 | |
| α-helix | 224-243 | 20 | |
| α-helix | 252-259 | 8 | |
| α-helix | 268 | 1 | |
| β-strand | 269-273 | 5 | 3 |
| β-strand | 277 | 1 | 4 |
| α-helix | 284-287 | 4 | |
| α-helix | 288-294 | 7 | |
| α-helix | 298-300 | 3 | |
| β-strand | 301 | 1 | 3 |
| α-helix | 307-309 | 3 | |
| β-strand | 312-321 | 10 | 3 |
| α-helix | 325-338 | 14 | |
| α-helix | 342 | 1 | |
| β-strand | 343 | 1 | 3 |
| α-helix | 344 | 1 | |
| β-strand | 349-356 | 8 | 3 |
| α-helix | 359-361 | 3 | |
| β-strand | 368 | 1 | 4 |
| α-helix | 369-370 | 2 | |
| β-strand | 373-381 | 9 | 3 |
| α-helix | 382-384 | 3 | |
| α-helix | 385-399 | 15 | |
| α-helix | 405-409 | 5 | |
| α-helix | 415-435 | 21 |
| Element | Residues | Length | Sheet |
|---|---|---|---|
| β-strand | 3-9 | 7 | 5 |
| α-helix | 10-28 | 19 | |
| β-strand | 30 | 1 | 6 |
| β-strand | 35 | 1 | 7 |
| β-strand | 36 | 1 | 6 |
| α-helix | 42-47 | 4 | |
| α-helix | 49-51 | 3 | |
| β-strand | 53-56 | 4 | 7 |
| β-strand | 60-63 | 4 | 7 |
| β-strand | 65-69 | 5 | 5 |
| α-helix | 73-80 | 8 | |
| α-helix | 84-86 | 3 | |
| α-helix | 89-91 | 3 | |
| β-strand | 92-94 | 3 | 5 |
| α-helix | 103-108 | 6 | |
| α-helix | 110-127 | 18 | |
| β-strand | 132-140 | 9 | 5 |
| α-helix | 145-149 | 5 | |
| α-helix | 150-160 | 11 | |
| β-strand | 165-172 | 8 | 5 |
| α-helix | 173 | 1 | |
| α-helix | 175-177 | 3 | |
| α-helix | 183-197 | 15 | |
| β-strand | 200-205 | 6 | 5 |
| α-helix | 206-211 | 6 | |
| α-helix | 212-216 | 5 | |
| α-helix | 224-243 | 20 | |
| α-helix | 252-259 | 8 | |
| β-strand | 267-268 | 2 | 5 |
| β-strand | 269-273 | 5 | 8 |
| α-helix | 288-293 | 6 | |
| α-helix | 298-300 | 3 | |
| β-strand | 301 | 1 | 8 |
| α-helix | 307-309 | 3 | |
| β-strand | 312-320 | 9 | 8 |
| α-helix | 325-338 | 14 | |
| α-helix | 340-342 | 3 | |
| β-strand | 343 | 1 | 8 |
| β-strand | 351-356 | 6 | 8 |
| α-helix | 359-360 | 2 | |
| β-strand | 374-381 | 8 | 8 |
| α-helix | 382-384 | 3 | |
| α-helix | 385-400 | 16 | |
| α-helix | 405-409 | 5 | |
| α-helix | 415-437 | 23 |
| Element | Residues | Length | Sheet |
|---|---|---|---|
| β-strand | 4-9 | 6 | 9 |
| α-helix | 10-28 | 19 | |
| α-helix | 48-51 | 4 | |
| β-strand | 53-55 | 3 | 10 |
| β-strand | 61-63 | 3 | 10 |
| β-strand | 65-69 | 5 | 9 |
| α-helix | 73-80 | 8 | |
| α-helix | 89-91 | 3 | |
| β-strand | 92-94 | 3 | 9 |
| α-helix | 103-104 | 2 | |
| α-helix | 105-109 | 5 | |
| α-helix | 111-113 | 3 | |
| α-helix | 115-126 | 12 | |
| β-strand | 134-140 | 7 | 9 |
| α-helix | 144 | 1 | |
| α-helix | 145-149 | 5 | |
| α-helix | 150-161 | 12 | |
| β-strand | 165-172 | 8 | 9 |
| α-helix | 175-177 | 3 | |
| α-helix | 183-194 | 12 | |
| α-helix | 195-197 | 3 | |
| β-strand | 200-205 | 6 | 9 |
| α-helix | 206-215 | 10 | |
| α-helix | 224-243 | 20 | |
| β-strand | 247 | 1 | 11 |
| α-helix | 252-259 | 8 | |
| α-helix | 268 | 1 | |
| β-strand | 269-273 | 5 | 11 |
| β-strand | 277 | 1 | 12 |
| α-helix | 288-293 | 6 | |
| α-helix | 294-296 | 3 | |
| α-helix | 298-300 | 3 | |
| β-strand | 301 | 1 | 11 |
| α-helix | 307-309 | 3 | |
| β-strand | 312-321 | 10 | 11 |
| α-helix | 325-336 | 12 | |
| α-helix | 342 | 1 | |
| β-strand | 343 | 1 | 11 |
| α-helix | 344 | 1 | |
| β-strand | 351-356 | 6 | 11 |
| α-helix | 359-361 | 3 | |
| β-strand | 368 | 1 | 12 |
| α-helix | 369-370 | 2 | |
| β-strand | 373-381 | 9 | 11 |
| α-helix | 382-384 | 3 | |
| α-helix | 385-399 | 15 | |
| α-helix | 405-409 | 5 | |
| α-helix | 415-435 | 21 |
| Element | Residues | Length | Sheet |
|---|---|---|---|
| β-strand | 3-9 | 7 | 13 |
| α-helix | 10-28 | 19 | |
| β-strand | 30 | 1 | 14 |
| β-strand | 35 | 1 | 15 |
| β-strand | 36 | 1 | 14 |
| α-helix | 42-47 | 4 | |
| α-helix | 49-51 | 3 | |
| β-strand | 53-56 | 4 | 15 |
| β-strand | 60-63 | 4 | 15 |
| β-strand | 65-69 | 5 | 13 |
| α-helix | 73-80 | 8 | |
| α-helix | 84-86 | 3 | |
| α-helix | 89-91 | 3 | |
| β-strand | 92-94 | 3 | 13 |
| α-helix | 103-108 | 6 | |
| α-helix | 110-127 | 18 | |
| β-strand | 132-140 | 9 | 13 |
| α-helix | 145-149 | 5 | |
| α-helix | 150-160 | 11 | |
| β-strand | 165-172 | 8 | 13 |
| α-helix | 173 | 1 | |
| α-helix | 175-177 | 3 | |
| α-helix | 183-197 | 15 | |
| β-strand | 200-205 | 6 | 13 |
| α-helix | 206-211 | 6 | |
| α-helix | 212-216 | 5 | |
| α-helix | 224-243 | 20 | |
| α-helix | 252-259 | 8 | |
| β-strand | 267-268 | 2 | 13 |
| β-strand | 269-273 | 5 | 16 |
| α-helix | 288-293 | 6 | |
| α-helix | 298-300 | 3 | |
| β-strand | 301 | 1 | 16 |
| α-helix | 307-309 | 3 | |
| β-strand | 312-321 | 10 | 16 |
| α-helix | 325-338 | 14 | |
| α-helix | 340-342 | 3 | |
| β-strand | 343 | 1 | 16 |
| β-strand | 351-356 | 6 | 16 |
| α-helix | 359-360 | 2 | |
| β-strand | 373-381 | 9 | 16 |
| α-helix | 382-384 | 3 | |
| α-helix | 385-400 | 16 | |
| α-helix | 406-409 | 4 | |
| α-helix | 415-437 | 23 |
| Element | Residues | Length | Sheet |
|---|---|---|---|
| β-strand | 7-14 | 8 | 3 |
| β-strand | 17-25 | 9 | 3 |
| α-helix | 47-138 | 92 |
| Molecule | Chains | Type | Length | Organism | UniProt |
|---|---|---|---|---|---|
| Tubulin alpha chain | A, C | protein | 433 | Ovis aries | D0VWZ0 (AlphaFold model) |
| Tubulin beta chain | B, D | protein | 431 | Ovis aries | D0VWY9 (AlphaFold model) |
| Stathmin-4 | E | protein | 142 | Rattus norvegicus | P63043 (AlphaFold model) |
>6H9B_1 Tubulin alpha chain (chains A, C) MRECISIHVGQAGVQIGNACWELYCLEHGIQPDGQMPSDDSFNTFFSETGAGKHVPRAVF VDLEPTVIDEVRTGTYRQLFHPEQLITGKEDAANNYARGHYTIGKEIIDLVLDRIRKLAD QCTGLQGFLVFHSFGGGTGSGFTSLLMERLSVDYGKKSKLEFSIYPAPQVSTAVVEPYNS ILTTHTTLEHSDCAFMVDNEAIYDICRRNLDIERPTYTNLNRLISQIVSSITASLRFDGA LNVDLTEFQTNLVPYPRIHFPLATYAPVISAEKAYHEQLSVAEITNACFEPANQMVKCDP RHGKYMACCLLYRGDVVPKDVNAAIATIKTKRSIQFVDWCPTGFKVGINYQPPTVVPGGD LAKVQRAVCMLSNTTAIAEAWARLDHKFDLMYAKRAFVHWYVGEGMEEGEFSEAREDMAA LEKDYEEVGVDSV
>6H9B_2 Tubulin beta chain (chains B, D) MREIVHIQAGQCGNQIGAKFWEVISDEHGIDPTGSYHGDSDLQLERINVYYNEATGNKYV PRAILVDLEPGTMDSVRSGPFGQIFRPDNFVFGQSGAGNNWAKGHYTEGAELVDSVLDVV RKESESCDCLQGFQLTHSLGGGTGSGMGTLLISKIREEYPDRIMNTFSVMPSPKVSDTVV EPYNATLSVHQLVENTDETYCIDNEALYDICFRTLKLTTPTYGDLNHLVSATMSGVTTCL RFPGQLNADLRKLAVNMVPFPRLHFFMPGFAPLTSRGSQQYRALTVPELTQQMFDSKNMM AACDPRHGRYLTVATIFRGRMSMKEVDEQMLNIQNKNSSYFVEWIPNNVKTAVCDIPPRG LKMSSTFIGNSTAIQELFKRISEQFTAMFRRKAFLHWYTGEGMDEMEFTEAESNMNDLVS EYQQYQDATAD
>6H9B_3 Stathmin-4 (chains E) ADMEVIELNKATSGQSWEVILKPPSFDGVPEFNASLPRRRDPSLEEIQKKLEAAEERRKY QEAELLKHLAEKREHEREVIQKAIEENNNFIKMAKEKLAQKMESNKENREAHLAAMLERL QEKDKHAEEVRKNKELKEEASR
| ID | Name | Formula | Copies |
|---|---|---|---|
| FWH | 9-methyl-3-[1-(2-methylquinolin-4-yl)ethenyl]carbazole | C25 H20 N2 | 2 |
| GDP | Guanosine-5'-diphosphate | C10 H15 N5 O11 P2 | 2 |
| MG | Magnesium ion | Mg | 2 |
| GTP | Guanosine-5'-triphosphate | C10 H16 N5 O14 P3 | 2 |
Water and common crystallization additives (SO4) are not listed.
1,1-Diheterocyclic Ethylenes Derived from Quinaldine and Carbazole as New Tubulin-Polymerization Inhibitors: Synthesis, Metabolism, and Biological Evaluation. Naret, T., Khelifi, I., Provot, O. et al. J Med Chem (2019) 62:1902-1916. DOI 10.1021/acs.jmedchem.8b01386 · PubMed
Other PDB entries of the same protein (UniProt D0VWZ0 (AlphaFold model), which also has an AlphaFold model), best resolution first:
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