Novel photoswitches with {features|attributes|functions|characteristics|capabilities|options} complementary {to the|towards the|for the} well-established azobenzenes are increasingly driving high-precision {research|study|analysis|investigation} in photopharmacology in cells and in vivo. Styrylthiazolium (StyTz) and styrylbenzothiazolium (StyBtz) are cellularly untested E/Z-isomerisation photoswitches {which are|that are} {nearly|almost|practically} isosteric to azobenzenes, but have distinct photophysical and physicochemical properties: {including|such as|which includes|like} ca. 60 nm red-shifted π→π* absorption, self-reporting fluorescence, Z→E relaxation that matches {typical|common|standard} biological timescales, and {good|great|excellent|very good|fantastic|superior} solubility {due to|because of|as a result of|on account of|resulting from|as a consequence of} their permanent {positive|good|optimistic|constructive} charge. We {here|right here} tested StyTz and StyBtz for their {potential|possible|prospective} as photopharmaceutical scaffolds, by applying them to photocontrol the dynamics {of the|from the|in the|on the|with the|of your} microtubule cytoskeleton. We observed light-specific disruption of microtubule network architecture and antiproliferative activity, {with a|having a|using a} structure-activity {relationship|partnership|connection} matching expectations for tubulin inhibitors. {However|Nevertheless|Nonetheless|Even so|On the other hand|Having said that}, {while|whilst|although|even though|when|though} testing the lead StyBtz2 for its molecular mechanism of action, we {found|discovered|identified|located} that it {did not|didn’t} inhibit microtubule dynamics. We tracked its localisation in {live|reside} cells by relying on its self-reporting fluorescence, observing accumulation of E-StyBtz2 into mitochondria; {after|following|right after|soon after|immediately after|just after} {several|a number of|numerous|many|various|quite a few} minutes of illumination it was then released {into the|in to the} cytosol concomitant with blebbing and cell death. We interpret this as light-dependent catastrophic rupturing of mitochondria on acute timescales. We conclude that StyTz/StyBtz {can be|may be|could be|might be|is often|is usually} {interesting|fascinating|intriguing|exciting} photopharmaceutical scaffolds for addressing mitochondrial, {rather than|instead of|as opposed to|as an alternative to|in lieu of} cytosolic, targets. Price of 309964-23-6 (1R,2R)-2-(1-Piperidinyl)cyclohexylamine web PMID:35954127
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