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PDBsum entry 6zwc
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Contents |
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436 a.a.
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431 a.a.
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155 a.a.
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References listed in PDB file
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Key reference
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Title
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A robust, Gfp-Orthogonal photoswitchable inhibitor scaffold extends optical control over the microtubule cytoskeleton.
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Authors
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L.Gao,
J.C.M.Meiring,
Y.Kraus,
M.Wranik,
T.Weinert,
S.D.Pritzl,
R.Bingham,
E.Ntouliou,
K.I.Jansen,
N.Olieric,
J.Standfuss,
L.C.Kapitein,
T.Lohmüller,
J.Ahlfeld,
A.Akhmanova,
M.O.Steinmetz,
O.Thorn-Seshold.
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Ref.
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Cell Chem Biol, 2021,
28,
228.
[DOI no: ]
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PubMed id
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Abstract
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Optically controlled chemical reagents, termed "photopharmaceuticals,"
are powerful tools for precise spatiotemporal control of proteins particularly
when genetic methods, such as knockouts or optogenetics are not viable options.
However, current photopharmaceutical scaffolds, such as azobenzenes are
intolerant of GFP/YFP imaging and are metabolically labile, posing severe
limitations for biological use. We rationally designed a photoswitchable
"SBT" scaffold to overcome these problems, then derivatized it to
create exceptionally metabolically robust and fully GFP/YFP-orthogonal
"SBTub" photopharmaceutical tubulin inhibitors. Lead compound SBTub3
allows temporally reversible, cell-precise, and even subcellularly precise
photomodulation of microtubule dynamics, organization, and microtubule-dependent
processes. By overcoming the previous limitations of microtubule
photopharmaceuticals, SBTubs offer powerful applications in cell biology, and
their robustness and druglikeness are favorable for intracellular biological
control in in vivo applications. We furthermore expect that the robustness and
imaging orthogonality of the SBT scaffold will inspire other derivatizations
directed at extending the photocontrol of a range of other biological targets.
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