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Torrice, C. D.

Publications and source records attributed to Torrice, C. D..

3 recordsLinked to original sources

SureCLIP and DrCLIP: Genetic manipulation-free, generalizable interactome mapping for cells and zebrafish

Unbiased interactome mapping currently relies on two types of approaches: co-immunoprecipitation coupled with mass spectrometry (co-IP/MS) and proximity-based tagging. Although co-IP/MS does not require genetic manipulation - thereby avoiding artifacts from exogenous protein expression and the time needed to generate stable cell or animal lines - it is increasingly being supplanted by proximity labeling techniques due to lower sensitivity and limited robustness. These drawbacks largely arise from the non-covalent nature of protein-protein interactions (PPIs) and carryover of bait and immunoglobulin (IgG) proteins in the final eluate. Here, we present a reversible crosslinker-mediated co-IP/MS workflow for endogenous proteins that (1) obviates the need for extensive lysis, wash, and elution optimization, (2) minimizes bait and IgG co-elution, and (3) captures several hundreds of interactors. We first describe subcellular-resolution, reversible crosslinker-mediated co-immunoprecipitation (SureCLIP), which enables PPI mapping of Hic-5, a focal adhesion protein, and lamin B1, a nuclear envelope protein, in cultured cells. We then introduce DrCLIP, a Danio rerio adaptation of SureCLIP, which allows comprehensive mapping of PPIs in zebrafish larvae. Using this approach, we profiled the kindlin-2 interactome in wild-type embryos without genetic manipulation. Both SureCLIP and DrCLIP exhibit high sensitivity and enable identification of novel interactors, providing a generalizable and powerful platform for defining native interactomes in 2D culture and whole animals.

cell biology↗

A new chemotype of chemically tractable nonsteroidal estrogens based on a thienopyrimidine core.

Despite continued interest in development of nonsteroidal estrogens and antiestrogens, there are only a few chemotypes of estrogen receptor ligands. Using targeted screening in a ligand sensing assay we identified a phenolic thieno[2,3-d]pyrimidine with affinity for estrogen receptor . An efficient three-step synthesis of the heterocyclic core and structure-guided optimization of the substituents resulted in a series of potent nonsteroidal estrogens. The chemical tractability of the thieno[2,3-d]pyrimidine chemotype will support the design of new estrogen receptor ligands as therapeutic hormones and antihormones. GRAPHICAL ABSTRACT O_FIG O_LINKSMALLFIG WIDTH=200 HEIGHT=48 SRC="FIGDIR/small/488344v1_ufig1.gif" ALT="Figure 1"> View larger version (16K): org.highwire.dtl.DTLVardef@4a0c18org.highwire.dtl.DTLVardef@16001f5org.highwire.dtl.DTLVardef@20a58forg.highwire.dtl.DTLVardef@1558bdf_HPS_FORMAT_FIGEXP M_FIG C_FIG

cell biology↗

Design and evaluation of novel 4-anilinoquinolines and quinazolines as EGFR inhibitors in lung cancer and chordoma

Epidermal growth factor receptor (EGFR) inhibitors have been used to target non-small cell lung cancer (NSCLC) and chordomas with varying amounts of success. We have probed several key structural features including an interaction with Asp855 within the EGFR DGF motif and interactions with the active site water network. The EGFR target engagement was then evaluated in an in-cell assay. Additionally, inhibitors were profiled in representative cellular models of NSCLC and chordomas. In addition to a structure activity relationship insights for EGFR inhibtior design, we also identified a compound (18) that is the most potent inhibitor (IC50 = 310 nM) on the UCH-2 chordoma cell line to date.

pharmacology and toxicology↗