Chemical genetic discovery of PARP targets reveals a role for PARP-1 in transcription elongation
Poly[adenosine diphosphate (ADP)–ribose] polymerases (PARPs) are a family of enzymes
that modulate diverse biological processes through covalent transfer of ADP-ribose from the …
that modulate diverse biological processes through covalent transfer of ADP-ribose from the …
An enzymatic TMPRSS2 assay for assessment of clinical candidates and discovery of inhibitors as potential treatment of COVID-19
JH Shrimp, SC Kales, PE Sanderson… - ACS pharmacology & …, 2020 - ACS Publications
SARS-CoV-2 is the viral pathogen causing the COVID19 global pandemic. Consequently,
much research has gone into the development of preclinical assays for the discovery of new …
much research has gone into the development of preclinical assays for the discovery of new …
[HTML][HTML] SULT1A1-dependent sulfonation of alkylators is a lineage-dependent vulnerability of liver cancers
Adult liver malignancies, including intrahepatic cholangiocarcinoma and hepatocellular
carcinoma, are the second leading cause of cancer-related deaths worldwide. Most individuals …
carcinoma, are the second leading cause of cancer-related deaths worldwide. Most individuals …
[HTML][HTML] Assay interference and off-target liabilities of reported histone acetyltransferase inhibitors
…, S Organ, M Cuellar, G Singh, JH Shrimp… - Nature …, 2017 - nature.com
Many compounds with potentially reactive chemical motifs and poor physicochemical properties
are published as selective modulators of biomolecules without sufficient validation and …
are published as selective modulators of biomolecules without sufficient validation and …
[HTML][HTML] An OpenData portal to share COVID-19 drug repurposing data in real time
The National Center for Advancing Translational Sciences (NCATS) has developed an online
open science data portal for its COVID-19 drug repurposing campaign–named OpenData–…
open science data portal for its COVID-19 drug repurposing campaign–named OpenData–…
[PDF][PDF] Dynamic imaging of LDH inhibition in tumors reveals rapid in vivo metabolic rewiring and vulnerability to combination therapy
…, D Crooks, J Jackson, A Joshi, BT Mott, JH Shrimp… - Cell reports, 2020 - cell.com
The reliance of many cancers on aerobic glycolysis has stimulated efforts to develop lactate
dehydrogenase (LDH) inhibitors. However, despite significant efforts, LDH inhibitors (LDHi) …
dehydrogenase (LDH) inhibitors. However, despite significant efforts, LDH inhibitors (LDHi) …
Identifying the functional contribution of the defatty-acylase activity of SIRT6
…, NA Spiegelman, JH Shrimp, RA Cerione, H Lin - Nature chemical …, 2016 - nature.com
Mammalian sirtuin 6 (SIRT6) exhibits many pivotal functions and multiple enzymatic activities,
but the contribution of each activity to the various functions is unclear. We identified a …
but the contribution of each activity to the various functions is unclear. We identified a …
[PDF][PDF] Discovering targets of non-enzymatic acylation by thioester reactivity profiling
RA Kulkarni, AJ Worth, TT Zengeya, JH Shrimp… - Cell chemical …, 2017 - cell.com
Non-enzymatic protein modification driven by thioester reactivity is thought to play a major
role in the establishment of cellular lysine acylation. However, the specific protein targets of …
role in the establishment of cellular lysine acylation. However, the specific protein targets of …
A chemoproteomic portrait of the oncometabolite fumarate
…, D Wei, SE Bergholtz, CA Briney, JH Shrimp… - Nature chemical …, 2019 - nature.com
Hereditary cancer disorders often provide an important window into novel mechanisms
supporting tumor growth. Understanding these mechanisms thus represents a vital goal. Toward …
supporting tumor growth. Understanding these mechanisms thus represents a vital goal. Toward …
Discovery of TMPRSS2 inhibitors from virtual screening as a potential treatment of COVID-19
The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) pandemic has prompted
researchers to pivot their efforts to finding antiviral compounds and vaccines. In this study, …
researchers to pivot their efforts to finding antiviral compounds and vaccines. In this study, …