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I am delighted to share that the main body of my postdoctoral work with #BenCravatt in collaboration with Bruno Melillo, #RamnikXavier and Stuart Schreiber is finally out which harnessed photoreactive stereoprobes to expand the ligandable proteome: tinyurl.com/f3uxbjj3.

Excited to share my postdoc work in Cravatt lab & Schreiber lab! We described photo-stereoprobes, DOS-inspired photo-reactive probes, for expanding the ligandable proteome. 🧵 doi.org/10.1101/2024.0…

Redirecting the pioneering function of FOXA1 with covalent small molecules biorxiv.org/cgi/content/sh… #bioRxiv

Together with the Cravatt group, we have a new manuscript out reporting the chemoproteomic discovery of covalent FOXA1 ligands that bind its DNA-binding domain, corrupt its motif preferences, and redistribute it on the genome. 1/11 biorxiv.org/content/10.110…

Excited to share my postdoctoral work in the Cravatt lab. We described a set of stereo- and regiochemically defined spirocycle acrylamides and their chemical proteomic analysis in human cancer cells, leading to the discovery of ERCC3 degraders and other novel ligands.

Beautiful talk by Benjamin Cravatt at #AACR24 about ABPP & targeting cysteines to extend druggable space. Featuring the recently disclosed FOXA1 stereospecific covalent ligand derived from marrying diversity-oriented chemistry Stuart Schreiber with the power of chemoproteomics.

Introducing CHARM: a new epigenome editor to methylate DNA at the promoter of a targeted gene. Our lab's collaboration with Jonathan Weissman's Lab's Edwin Neumann & Tessa Bertozzi shows deep silencing of brain PrP Paper: science.org/doi/10.1126/sc… Blog: cureffi.org/2024/06/27/int…

Prof. Keary Engle of the Engle Lab is the new Dean of Graduate and Postdoctoral Studies at Scripps Research, leading the Scripps Research Graduate Program. An alumnus, Engle brings personal experience and is committed to mentoring future researchers. More: ow.ly/FcHR50Su8l2

Excited to share a key part of my postdoctoral work in the Cravatt lab at @ScrippsResearch, published today in Nature Chemistry! Huge thanks to collaborators Bruno Melillo, Rachel Hayward, Vividion Therapeutics, and all coauthors.

The Cravatt Lab, with Bruno Melillo and Evert Njomen, identified novel proteins that could be targeted to delay or even prevent #cancer cell division. Published in Nature Chemistry, this study paves the way for developing innovative cancer therapies. More: ow.ly/jaWL50TeCWB

Ben Cravatt and Yuanjin Zhang | 张沅珒 report a paralog-hopping approach leveraging chemical proteomic data on covalently liganded cysteines, revealing an allosteric pocket shared by cysteine-containing CCNE2 and cysteine-less paralogous proteins. Read it here rdcu.be/dUlxn

Excited to share this CellChemicalBiology Review I wrote with Ben Cravatt highlighting recent applications of ABPP for ligand discovery. We highlight the expansion of ABPP beyond enzyme active sites with a special focus on covalent ligands. Enjoy! tinyurl.com/48cyaj6d

Simple, Enantiocontrolled Azetidine Library Synthesis via Strain Release Functionalization of 1-Azabicyclobutanes. A fantastic collaboration with the Cravatt lab. A simple, modular, programmable approach to access complex stereopure azetidines through strain-release

We keep stumbling on molecular glues, but how can they be made for a pre-selected target? We’ve been working on this question, envisioning a high-throughput chemistry (HTC)-based approach to convert pre-existing ligands into molecular glues. biorxiv.org/content/10.110…

New findings in Molecular Cell by Ben Cravatt and Michael Erb identify a ligandable site on the “undruggable” FOXA1 transcription factor in hormone-driven cancers. Dual ABPP maps FOXA1-small molecule interactions, guiding therapeutic design. More at: ow.ly/cB2M50TM2gb

For years, scientists have considered transcription factors to be undruggable, but new research published this month in Molecular Cell shows they may be druggable after all. cen.acs.org/biological-che… .

Today #CancerGrandChallenges team eDyNAmiC and their international collaborators published 3️⃣ papers in nature 📣 They show the prevalence of ecDNA in cancer, identify fundamental mechanisms and an actionable target now being tested in the clinic. More: bit.ly/4dUMU00

Online now! Chemical tools to expand the ligandable proteome: Diversity-oriented synthesis-based photoreactive stereoprobes by Daisuke Ogasawara, Bruno Melillo, Ben Cravatt, et al at Scripps Research Broad Institute Harvard Medical School dlvr.it/TGFYHz

#Technology Chemical tools to expand the ligandable proteome: Diversity-oriented synthesis-based photoreactive stereoprobes by Daisuke Ogasawara, Bruno Melillo, Ben Cravatt at Scripps Research Broad Institute Harvard Medical School MassGeneral News dlvr.it/TGwBK2

Excited to share this work profiling a new P(V)-electrophile using our stereoprobe platform, where we discover a first-in-class, cell-active inhibitor of integral membrane protein TLCD1 and ID critical catalytic residues! Great collab w/Baran Lab biorxiv.org/content/10.110…