Gunning Group

Multidisciplinary team of molecular architects using #medicinalchemistry & #molecularrecognition to design better medicines. 🧵 gunninggroup 🐘 gunninglabuoft

[Gunning Group @GunningLabUofT]

Thrilled to share our #OpenAccess online resource "An Introduction to Medicinal Chemistry & Molecular Recognition" on @OpenLibraryON! We designed this resource to provide budding medicinal chemists with the knowledge & tools to navigate small molecule drug discovery! #OER

[Eric Topol @EricTopol]

Today "a milestone in the evolution of personalized therapies for rare & ultra-rare inborn errors of metabolism"
—the 1st human to undergo custom genome editing
—outgrowth of decades of NIH funded research
https://t.co/HmJxYWDCV7
https://t.co/4DsNELnBut @NEJM
https://t.co/y7NMGPpXnE

[Brain Cancer Canada @braincancercan]

NEW SITE LAUNCH! https://t.co/aJ9BgdKfVn

NEW! Researchers & Scientists: https://t.co/DOvaQq3FHH

NEW! Patient & Caregiver Resources
https://t.co/159YcwPM18

NEW! Projects Funded
https://t.co/CpyaXUbkch

NEW! Community
https://t.co/ssmRrYQE6Y

#braincancer

[Chemical Communications @ChemCommun]

In case you missed it:

'Microwave-assisted synthesis of pomalidomide building blocks for rapid PROTAC and molecular glue development'

Fom Patrick Gunning and colleagues at @GunningLabUofT

https://t.co/URQzvQhoNo

[Guillaume Laconde @Glaconde34]

Monoselective Histone Deacetylase 6 PROTAC Degrader Shows In Vivo Tractability | Journal of Medicinal Chemistry https://t.co/Qdo3NgkP9K

[Gunning Group @GunningLabUofT]

@HartungIngo @Glaconde34 @ProtDegraders As Tobi mentioned, one explanation could be the relatively short PEG1-triazole linker which may cause the pyridyl arm of the HDAC6 ligand to sterically preclude neosubstrate recruitment.

[Gunning Group @GunningLabUofT]

@HartungIngo @Glaconde34 @ProtDegraders It surprised us too, since most of the 4-alkylamino-substituted CRBN recruiters we've seen show some degree of neosubstrate degradation, but the proteomic data was quite convincing and corroborated by Western blots. (1/2)

[Gunning Group @GunningLabUofT]

Congratulations to first authors Harsimran Garcha and @OlutobiOlaoye, co-authors @Taleb_Sedighi, Daniel Pölöske, Pearla Hariri, Wenlong Yu, @d_abdallah98, & our longtime friend and collaborator @richard_moriggl for this work! @Patrick_Gunning @e_dearaujo https://t.co/1VUCyZu5g6

[Gunning Group @GunningLabUofT]

Excited to share our latest work on an exquisitely selective #PROTAC of #HDAC6 in #JMedChem @ACSBioMed @ACSPublications!! TO-1187 is a highly potent HDAC6 degrader with complete proteome selectivity, sparing all #CRBN neosubstrates and other #HDAC isoforms.

[Gunning Group @GunningLabUofT]

Congratulations to first authors @d_abdallah98 and @brohannes10, co-authors Lina Hasan, Naman Patel, Timothy Wright, @bilalsaqib_, and many thanks to our collaborator @theKeillors for this excellent work! @Patrick_Gunning @e_dearaujo

[Gunning Group @GunningLabUofT]

Do you find multi-step #PROTAC synthesis to be laborious and time-consuming? We present our latest work in @ChemCommun on a microwave-assisted #SNAr methodology for rapid preparation of #pomalidomide-based #PROTACs!
#targetedproteindegradation #molecularglues

[Chemical Communications @ChemCommun]

Take a look at 'Microwave-assisted synthesis of pomalidomide building blocks for rapid PROTAC and molecular glue development'

New from Patrick Gunning and colleagues at @GunningLabUofT

https://t.co/URQzvQhoNo

[Gunning Group @GunningLabUofT]

We optimized conventional conditions for fluorothalidomide SNAr (overnight, oil bath heating) to achieve improved yields on gram-scale in only 15 minutes under microwave irradiation, exemplifying the method by preparing the clinically explored PROTAC #bavdegalutamide (ARV-110)!

[Aubry K. Miller @DrugDiscov_DKFZ]

Check out our paper on proton pump inhibitor activation in cells in @NatureChemistry. Congrats to first author Teresa Marker who started this project in my group and finished it with Tobias Dick (@RedoxDKFZ). More collabs between our groups @DKFZ to come! https://t.co/oYt2rHEF0D

[NSERC / CRSNG @NSERC_CRSNG]

🗞️
"Characterization of conformational states of the homodimeric enzyme fluoroacetate dehalogenase by 19F–13C two-dimensional NMR" ⤵️
@UofT &+

With #NSERCsupport.

[Gunning Group @GunningLabUofT]

Congrats to Motasem in the #Prosserlab and our recent co-supervised alumnus @geordifrere for publishing a new story on tryptophan-based 2D 19F-13C NMR in @rsc_chembio!

[Geordi Frere @geordifrere]

Excited to share our new paper in @rsc_chembio on improving resolution in fluorotryptophan protein NMR by expanding into the 13C dimension! We prepared & used a 13C-labelled F-Trp precursor to achieve unprecedented spectral resolution of a F-Trp-bearing protein by 2D 19F-13C NMR!

[Gunning Group @GunningLabUofT]

We're hiring a #Postdoctoral Fellow in #medicinalchemistry in collaboration with @HDAXtx! Please repost and apply below if you're interested in advancing our novel small-molecule therapeutics!
#chemjobs #chempostdoc #postdoc #postdocjobs @ChemPostdocBot
https://t.co/PORxafv7to

[Communications Chemistry @CommsChem]

pharmacophore-optimized photoaffinity fragments-based hit discovery with improved hit rate and better sensitivity, and multiple binding sites, reported by @keserulab @GunningLabUofT
https://t.co/HbHZWUUyqY

[Gunning Group @GunningLabUofT]

Congratulations to our Sr. Researcher Associate @GeletuMulu for receiving the Rosemary Brown Outstanding Mentorship Award at @CanBlackSci's #BlackExcellenceInSTEMM conference!! Mulu's commitment to scientific mentorship in our community is nothing short of inspiring.
#BESTEMM2024

[Gunning Group @GunningLabUofT]

@NSERC_CRSNG @UTM_CPS @J_A_C_S @TheMediumUTM Geordi has been a pillar of our lab and the larger @UTM community in many capacities throughout his graduate studies. We wish him the absolute best as he heads to @harvardmed to pursue an exciting postdoc in the @GygiLab @HarvardCellBio! #gunningalumni

[Gunning Group @GunningLabUofT]

Delighted to congratulate Dr. @geordifrere for defending his PhD thesis on the design of #monovalent electrophilic protein degraders & novel probes for protein-observed 19F #NMR! Geordi is an expert synthetic chemist & our resident scientific lectiophile!
#PrOFNMR #covalent #TPD

[Gunning Group @GunningLabUofT]

@NSERC_CRSNG @UTM_CPS @J_A_C_S You can read more about Geordi's graduate journey by reading @TheMediumUTM's article featuring him! He discusses his path towards chemistry, describes the joy and wonder of creating new molecules, and shares some advice for prospective graduate students.
https://t.co/3XPlnBMrOC

[Gunning Group @GunningLabUofT]

Our PhD student @geordifrere was featured in the latest issue of @TheMediumUTM! Geordi is a talented medicinal chemist in our lab working on the development of covalent protein degraders as well as new ways to enable site-selective ligand discovery by NMR!
https://t.co/OIC8ZaILtL