Micah Niphakis
@MJNiphakis
Chemical biologist @ LLJRC | Covalent ligands, chemical probes, target engagement, chemoproteomics | Tweets are my own
Check out our recent Opinion in @TrendsinPharma on chemical proteomic binding site determination for non-covalent compounds
Chemical proteomic mapping of reversible small molecule binding sites in native systems dlvr.it/TFMRnc
Excited to see our work online! Please check it out with the link 👇
Ben Cravatt and @YuanjinZhang1 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
The Cravatt Lab, with @brumelillo and @EvertNjomen, identified novel proteins that could be targeted to delay or even prevent #cancer cell division. Published in @NatureChemistry, this study paves the way for developing innovative cancer therapies. More: ow.ly/jaWL50TeCWB
Check out our most recent work developing new strategies that leverage massive mRNA-displayed macrocyclic peptide libraries for covalent ligand discovery! Congrats @LanT_763 and thanks for @mbogyo and Scott Snyder for collaboration! pubs.acs.org/doi/10.1021/ja…
Online now! Covalent targeting of splicing in T cells by Kevin A. Scott, Hiroyuki Kojima, Nathalie Ropek, Ekaterina V. Vinogradova @katenokv and colleagues at @RockefellerUniv @TPCB_NYC @WeillCornell @MSKCancerCenter @scrippsresearch dlvr.it/TGR63y #chembiol
Excited to see the final version of our manuscript out in @CellChemBiol! In this study, we investigate the mechanism of action of an immunosuppressive small-molecule electrophile, which targets a core splicing factor SF3B1! @RockefellerUniv authors.elsevier.com/a/1k9mh8jWWJxM…
Online now! Chemical tools to expand the ligandable proteome: Diversity-oriented synthesis-based photoreactive stereoprobes by @d_ogasa, @brumelillo, @bencravatt, et al at @scrippsresearch @broadinstitute @harvardmed dlvr.it/TGFYHz
(1/5) Excited to share this collab with the Cravatt lab at @scrippsresearch! A structurally diverse library of photoreactive, stereoselective chemical probes can be used for high-throughput #proteomics experiments in living systems. authors.elsevier.com/c/1k5v78jWWJxM…
Awesome paper from Jack Taunton’s lab @UCSF : Mutant-selective AKT inhibition through lysine targeting and neo-zinc chelation | Nature nature.com/articles/s4158…
Interesting paper by the group of @MichaelBollong of @scrippsresearch in @J_A_C_S. A high-throughput assay for cysteine-reactive electrophiles based on luciferase activity allows identification of azetidinyl oxadiazoles as cysteine-reactive electrophiles. pubs.acs.org/doi/10.1021/ja…
Pioneer TFs have long been considered "undruggable" 💊 🧬 However, @scrippsresearch teams led by Ben Cravatt and @Michael_A_Erb have elegantly developed a first-in-class ligand for the pioneer TF FOXA1. In @MolecularCell, we commented on this groundbreaking work:…
Thrilled to share our new study in @nchembio describing the proteome-wide impacts of electrophile stress in the context of covalent fragments. Big congratulations to first authors Ashley Julio @AshleyJulio4 and Flowreen Shikwana @FShikwana ! 1/5 nature.com/articles/s4158…
Open season on FOXA1! Our paper with the Cravatt group is out today in @MolecularCell. Please check out the updated data, including a new discovery that FOXA1 ligands mirror the effects of a nearby prostate cancer mutation. authors.elsevier.com/a/1jxLO3vVUPRn… (1/2)
Online Now: Redirecting the pioneering function of FOXA1 with covalent small molecules dlvr.it/TFN91y
Suppression of NRF2-dependent cancer growth by a covalent allosteric molecular glue biorxiv.org/cgi/content/sh… #biorxiv_cancer
We really enjoyed putting this accounts paper together , placing our contributions to the covalent stabilization of ternary complexes in the context of induced proximity pubs.acs.org/doi/abs/10.102…
the first project of my PhD is now out @J_A_C_S ! super proud to introduce ABAP (my first acronym!) and share our findings on how lysine acetylation modulates protein function & interactions. so surreal to see this in print pubs.acs.org/doi/10.1021/ja…
If you are interested in Activity-Based Protein Profiling, definitely already mark your calendars for the 14th ABPP conference @abpp2025london on March 30th to April 2nd, 2025, at the Francis Crick Institute. An amazing lineup of speakers. eventcreate.com/e/abpp2025
#Review Ligand discovery by activity-based protein profiling by @MJNiphakis and @bencravatt at Lundbeck La Jolla Research Center Inc. and @scrippsresearch dlvr.it/TDTXhF
Excited to share this @CellChemBiol 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
