Functional interrogation of the kinome using nucleotide acyl phosphates

…, AK Szardenings, M Liyanage, TK Nomanbhoy… - Biochemistry, 2007 - ACS Publications
The central role of protein kinases in signal transduction pathways has generated intense
interest in targeting these enzymes for a wide range of therapeutic indications. Here we report …

Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2

…, Q Yang, JD Lee, MP Patricelli, TK Nomanbhoy… - Nature chemical …, 2011 - nature.com
Mutations in leucine-rich repeat kinase 2 (LRRK2) are strongly associated with late-onset
autosomal dominant Parkinson's disease. We employed a new, parallel, compound-centric …

[PDF][PDF] Discovery of potent and selective covalent inhibitors of JNK

…, H Park, PV LoGrasso, M Patricelli, TK Nomanbhoy… - Chemistry & biology, 2012 - cell.com
The mitogen-activated kinases JNK1/2/3 are key enzymes in signaling modules that transduce
and integrate extracellular stimuli into coordinated cellular response. Here, we report the …

[PDF][PDF] In situ kinase profiling reveals functionally relevant properties of native kinases

MP Patricelli, TK Nomanbhoy, J Wu, H Brown, D Zhou… - Chemistry & biology, 2011 - cell.com
Protein kinases are intensely studied mediators of cellular signaling, yet important
questions remain regarding their regulation and in vivo properties. Here, we use a probe-based …

Mechanistic and pharmacological characterization of PF-04457845: a highly potent and selective fatty acid amide hydrolase inhibitor that reduces inflammatory and …

…, SN Bhattachar, C Stiff, TK Nomanbhoy… - … of Pharmacology and …, 2011 - ASPET
The endogenous cannabinoid (endocannabinoid) anandamide is principally degraded by the
integral membrane enzyme fatty acid amide hydrolase (FAAH). Pharmacological blockade …

Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity

…, ET Lund, RA Nugent, TK Nomanbhoy… - Biochemistry, 2007 - ACS Publications
Fatty acid amide hydrolase (FAAH) is an integral membrane enzyme that degrades the fatty
acid amide family of signaling lipids, including the endocannabinoid anandamide. Genetic …

Discovery of PF-04457845: a highly potent, orally bioavailable, and selective urea FAAH inhibitor

…, SJ Kesten, TK Nomanbhoy… - ACS medicinal …, 2011 - ACS Publications
Fatty acid amide hydrolase (FAAH) is an integral membrane serine hydrolase that degrades
the fatty acid amide family of signaling lipids, including the endocannabinoid anandamide. …

[HTML][HTML] C-terminal binding domain of Rho GDP-dissociation inhibitor directs N-terminal inhibitory peptide to GTPases

YQ Gosser, TK Nomanbhoy, B Aghazadeh, D Manor… - Nature, 1997 - nature.com
The Rho GDP-dissociation inhibitors (GDIs) negatively regulate Rho-family GTPases 1 , 2 .
The inhibitory activity of GDI derives both from an ability to bind the carboxy-terminal …

ERK5 kinase activity is dispensable for cellular immune response and proliferation

…, CM Amantea, TK Nomanbhoy… - Proceedings of the …, 2016 - National Acad Sciences
Unlike other members of the MAPK family, ERK5 contains a large C-terminal domain with
transcriptional activation capability in addition to an N-terminal canonical kinase domain. …

[HTML][HTML] Characterization of the Interaction between RhoGDI and Cdc42Hs Using Fluorescence Spectroscopy (∗)

TK Nomanbhoy, RA Cerione - Journal of Biological Chemistry, 1996 - ASBMB
The GDP-dissociation-inhibitor (GDI) for Rho-like GTP-binding proteins is capable of three
different biochemical activities. These are the inhibition of GDP dissociation, the inhibition of …