Discovery of a first-in-class receptor interacting protein 1 (RIP1) kinase specific clinical candidate (GSK2982772) for the treatment of inflammatory diseases

PA Harris, SB Berger, JU Jeong, R Nagilla… - 2017 - ACS Publications
RIP1 regulates necroptosis and inflammation and may play an important role in contributing
to a variety of human pathologies, including immune-mediated inflammatory diseases. Small…

Nasal route for direct delivery of solutes to the central nervous system: fact or fiction?

S Mathison, R Nagilla, UB Kompella - Journal of drug targeting, 1998 - Taylor & Francis
During this century, several investigators reported that certain viruses, metais, drugs, and
other solutes could bypass systemic circulation and enter the brain and/or cerebrospinal fluid …

DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors

…, R Lehr, DE McNulty, R Nagilla… - Journal of medicinal …, 2016 - ACS Publications
The recent discovery of the role of receptor interacting protein 1 (RIP1) kinase in tumor
necrosis factor (TNF)-mediated inflammation has led to its emergence as a highly promising …

AMTB, a TRPM8 channel blocker: evidence in rats for activity in overactive bladder and painful bladder syndrome

…, LA Leon, SD Gardner, R Nagilla… - American Journal …, 2008 - journals.physiology.org
The activation of the TRPM8 channel, a member of the large class of TRP ion channels, has
been reported to be involved in overactive bladder and painful bladder syndrome, although …

Discovery of small molecule RIP1 kinase inhibitors for the treatment of pathologies associated with necroptosis

…, KM Kahler, R Lehr, JD Lich, R Nagilla… - ACS medicinal …, 2013 - ACS Publications
Potent inhibitors of RIP1 kinase from three distinct series, 1-aminoisoquinolines, pyrrolo[2,3-b]pyridines,
and furo[2,3-d]pyrimidines, all of the type II class recognizing a DLG-out inactive …

The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a Highly Potent and …

…, MA Reilly, EJ Rivera, HH Sun, R Nagilla… - Journal of medicinal …, 2016 - ACS Publications
RIP2 kinase is a central component of the innate immune system and enables downstream
signaling following activation of the pattern recognition receptors NOD1 and NOD2, leading …

Optimization of a series of RIPK2 PROTACs

…, A Mares, AR Thawani, R Nagilla… - Journal of Medicinal …, 2021 - ACS Publications
Receptor-interacting serine/threonine protein kinase 2 (RIPK2) is an important kinase of the
innate immune system. Herein, we describe the optimization of a series of RIPK2 PROTACs …

Identification of a RIP1 kinase inhibitor clinical candidate (GSK3145095) for the treatment of pancreatic cancer

…, MK Mahajan, G Miller, R Nagilla… - ACS medicinal …, 2019 - ACS Publications
RIP1 regulates cell death and inflammation and is believed to play an important role in
contributing to a variety of human pathologies, including immune-mediated inflammatory …

Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2-((4-(Benzo[d]thiazol-5-ylamino)-6-(tert-butylsulfonyl) …

…, SB Berger, MK Mahajan, MA Reilly, R Nagilla… - 2019 - ACS Publications
RIP2 kinase has been identified as a key signal transduction partner in the NOD2 pathway
contributing to a variety of human pathologies, including immune-mediated inflammatory …

A comprehensive analysis of the role of correction factors in the allometric predictivity of clearance from rat, dog, and monkey to humans

R Nagilla, KW Ward - Journal of pharmaceutical sciences, 2004 - Elsevier
This study was conducted to comprehensively evaluate the performance of various allometric
scaling methods for the prediction of human clearance. Allometric scaling was used to …