Publications + Posters

A duplexed high-throughput mass spectrometry assay for bifunctional POLB polymerase and lyase activity

MTA-cooperative PRMT5 inhibitors: mechanism switching through structure-based design

Discovery of TNG908: A selective, brain penetrant, MTA-cooperative PRMT5 inhibitor that is synthetically lethal with MTAP-deleted cancers

Experimental ‘loss-of function’ annotation of STK11 mutations with prognostic and therapeutic implications

Evaluation of the impact of homozygous MTAP truncations on the activity and selectivity of MTA-cooperative PRMT5 inhibitors

Genome-wide drug anchor screens identify CAAP1 and AKAP17A as regulators of PRMT5 inhibitor sensitivity

TNG348 is synergistic with PARP inhibitors in tumor models with elevated replication stress

LIG1 inactivation selectively inhibits growth of BRCA1 mutant cells in vitro and in vivo

TNG917 is a clinical-grade, potent and selective inhibitor of EHMT1/2 for the treatment of immune cold tumors

Stearoyl-CoA desaturase is a synthetic lethal target in SMAD4-deficient cancers

MTA-cooperative PRMT5 inhibitors for the treatment of MTAP-deleted cancers

Discovery of TNG348: A selective and potent inhibitor of USP1 for treatment of BRCA1, BRCA2-mutant and other HRD+ cancers

POLB knockout is synthetic lethal with PARP inhibition leading to complete and durable responses in BRCA-mutant tumor xenografts

TNG908, a brain-penetrant MTA-cooperative PRMT5 inhibitor, is efficacious in preclinical MTAP-deleted models, including glioblastoma

MTA-cooperative PRMT5 inhibitors are efficacious in MTAP-deleted malignant peripheral nerve sheath tumor models

CoREST inhibition by TNG260 increases expression of immunomodulatory genes in STK11-mutant cancer and sensitizes to immune checkpoint blockade

Inducible activation of sgRNA libraries in tumor xenografts empowers large-scale in vivo target discovery screens

MTA-cooperative PRMT5 inhibitors selectively modulate RNA splicing in MTAP-deleted cancer cells across histologies

Unbiased in vitro and in vivo drug anchor screens identify mechanisms of resistance and sensitization for MTA-cooperative PRMT5 inhibitors in MTAP-deleted cancer models

TNG348, a selective USP1 inhibitor, shows strong preclinical combination activity with PARP inhibitors and other agents targeting DNA repair

Cancer-specific AI identifies multi-modal biomarkers of therapeutic response for 1,951 drugs including TNG348, a highly selective USP1 inhibitor

Discovery of TNG462: A highly potent and selective MTA-cooperative PRMT5 inhibitor synthetic lethal for MTAP deleted cancers

TNG462 is a potential best-in-class MTA-cooperative PRMT5 inhibitor for the treatment of MTAP-deleted solid tumors

TNG348 is a potent and selective inhibitor of USP1 for the treatment of BRCA1/2mut and HRD+ cancers

TNG908, a brain-penetrant MTA-cooperative PRMT5 inhibitor, is efficacious in preclinical glioblastoma models

TNG260: A novel, orally active, CoREST-selective deacetylase inhibitor for the treatment of STK11-mutant cancers

Ubiquitinated PCNA drives USP1 synthetic lethality in cancer

TNG260, a CoREST-selective deacetylase inhibitor, reverses anti-PD1 resistance driven by loss of STK11

In vivo CRISPR screens identify HDAC1 as an immune sensitizer reversing immune resistance driven by STK11 loss

Whole genome CRISPR-Cas9 screens in a cancer cell line panel co-cultured with antigen-specific cytotoxic CD8 T cells are a powerful engine for immuno-oncology drug target discovery

Leveraging CRISPR-Cas9 screening platform for discovery of novel tumor intrinsic phagocytosis modulators

Biochemical characterization of TNG908 as a novel, potent MTA-cooperative PRMT5 inhibitor for the treatment of MTAP-deleted cancers

TNG908 is a brain-penetrant, MTA-cooperative PRMT5 inhibitor for the treatment of MTAP-deleted cancer

TNG462 is a potential best-in-class MTA-cooperative PRMT5 inhibitor for the treatment of peripheral MTAP-deleted solid tumors

VRK1 is a Synthetic Lethal Target in VRK2-deficient Glioblastoma

TNG908 is an MTAP^null-selective PRMT5 inhibitor that drives tumor regressions in MTAP-deleted xenograft models across multiple histologies

USP1 inhibitor synthetic lethality in BRCA1/2 mutant cancer is driven by PCNA ubiquitination

UMIBB: A novel nonparametric Bayesian method improves robustness and sensitivity of analysis in pooled CRISPR Cas9 screens leveraging unique molecular identifiers

Evidence for synergy between TNG908, an MTAP^null-selective PRMT5 inhibitor, and sotorasib in an MTAP^null/KRASG12C xenograft model

TNG908 is an MTAP^null-selective PRMT5 inhibitor that drives tumor regression in MTAP-deleted xenograft models across histologies

VRK1 is a novel synthetic lethal target in VRK2-methylated glioblastoma

CRISPR screens identify sensitizers to trametinib in KRAS mutant cancer cell lines

Loss of HS2ST1 cooperates with MAPK inhibition to impair growth of mesenchymal KRAS mutant NSCLC

Isogenic CRISPR anchor screens identified actionable nodes to CHK1/2 inhibitor Prexasertib in TP53 mutant cancer

In vivo CRISPR screen identifies tumor suppressors as drivers of tumor cell-intrinsic immune evasion

Optimizing the Therapeutic Window of Targeted Drugs in Oncology: Potency-guided First-in-Human Studies

Synthetic lethality as an engine for cancer drug target discovery

EGLN1 is a synthetic lethal target in ARID1A-mutant ovarian cancer