Selectivity and Cooperativity of PROTAC^®s using HT-SPR

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Rizwan Chaudhrey: And joined by Rebecca Rich from Carterra at their poster from Carterra, so Rebecca first of all, how are you?

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Rebecca Rich: Doing lovely today thank you

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RC: it was lovely to see you so I can see you standing in front of your poster so tell me more about your poster and why you're doing it

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RR: Sure, this is to talk about some of the work we've done with the selectivity and cooperativity of protac using the carterra LSA platform the XT platform great so I'd like to walk through a little bit yeah sure the premise of this experiment was that we're able to put down a large number of proteins on the sensor surface and here we put down 96 bromodomain proteins over it we can flow either the binary the protac alone yeah or the protac in conjunction with the ligase right so we're able to screen L at one time these many different interactions right down below here this is a panel of the 96 binary interactions that's the Protac alone binding to 96 different bromodomain proteins and we can see there are some that are not binders and that we have ones of different shapes of different binding profiles.

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RC: what does that mean?

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RR: that means they have different affinities and different kinetics and we're able to identify those that bind and those that don't right these data along with this middle panel here of binary interactions for another compound and this third panel over here for yet a third compound were collected in one day right so pretty significant throughput in one day for these three compounds against 96 proteins right down here below is an example of the ternary interactions here again this is the protac in a mixture with the ligase injected across the same 96 bromodomains so we're able to pick up the ternary interaction again measured in one day and the binary measured the day before right we did that for all three compounds with that data we can therefore down here is a measure of the cooperity we can identify for this one particular compound mz1 those interactions that perform a positive cooperativity and those are no cooperativity and negative cooperativity by that example we can identify how this compound binds to both the ligase and the bromo domains so that's the highlights of this poster

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RC: brilliant and this is poster up for the rest of the show

RR: yes it is we're actually presenting today at noon but

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RR: I'll be here at the rest of the all of the sessions

RC: fantastic so there you go viewers if you'd like to know more about what Carterra are talking about here and also see the poster presentation then first will come and visit the Carterra booth and also come see the poster which is one three seven six eight so Rebecca thank you for taking time out thank you very much appreciate it so viewers as I said if you'd like to know more about criteria about the new product and about the other solutions they have as well as the poster check out the booth if you cannot do that then you can follow them on LinkedIn message them on LinkedIn and also go to their website and there are lots of other events throughout the year both in North America and in Europe so with that I want to say Rebecca thank you for your time have a great show thank you very much and viewers thank you for watching until next time stay well stay safe bye.