LRRK2 inhibitors induce reversible changes in nonhuman primate lungs without measurable pulmonary deficits

…, K Rudolph, AK Sharma, A Stepan, S Steyn… - Science translational …, 2020 - science.org
The kinase-activating mutation G2019S in leucine-rich repeat kinase 2 (LRRK2) is one of the
most common genetic causes of Parkinson’s disease (PD) and has spurred development …

PF-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy

…, L Pustilnik, AM Rossi, SJ Steyn… - Molecular cancer …, 2010 - AACR
The Aurora family of highly related serine/threonine kinases plays a key role in the regulation
of mitosis. Aurora1 and Aurora2 play important but distinct roles in the G 2 and M phases of …

High throughput ADME screening: practical considerations, impact on the portfolio and enabler of in silico ADME models

…, W Mitchell, M Snyder, SJ Steyn… - Current drug …, 2008 - ingentaconnect.com
Evaluation and optimization of drug metabolism and pharmacokinetic data plays an important
role in drug discovery and development and several reliable in vitro ADME models are …

RORγt inhibition ameliorates IL-23 driven experimental psoriatic arthritis by predominantly modulating γδ-T cells

…, C Ambler, M Hegen, P Symanowicz, S Steyn… - …, 2023 - academic.oup.com
Objective Divergent therapeutic outcomes on different disease domains have been noted
with IL-23 and IL-17A-blockade in PsA. Therefore, elucidating the role of RORγt, the master …

Projecting ADME behavior and drug-drug interactions in early discovery and development: application of the extended clearance classification system

AF El-Kattan, MV Varma, SJ Steyn, DO Scott… - Pharmaceutical …, 2016 - Springer
Purpose To assess the utility of Extended Clearance Classification System (ECCS) in
understanding absorption, distribution, metabolism, and elimination (ADME) attributes and …

Insights from an integrated physiologically based pharmacokinetic model for brain penetration

…, E Belova, JL Liras, DO Scott, SJ Steyn - Journal of pharmaceutical …, 2016 - Elsevier
Central-nervous-system, physiologically based pharmacokinetic (PBPK) models predict
exposure profiles in the brain, that is, the rate and extent of distribution. The current work …

A Novel CC Chemoattractant Cytokine (Chemokine) Receptor 6 (CCR6) Antagonist (PF-07054894) Distinguishes between Homologous Chemokine Receptors …

…, L Newman, AP Vargas, SW Kumpf, SJ Steyn… - … of Pharmacology and …, 2023 - ASPET
Blocking chemokine receptor CC chemoattractant cytokine (chemokine) receptor (CCR) 6-dependent
T cell migration has therapeutic promise in inflammatory diseases. PF-07054894 …

LRRK2 kinase inhibitors induce a reversible effect in the lungs of non-human primates with no measurable pulmonary deficits

…, C Royer, K Rudolph, AK Sharma, A Stepan, S Steyn… - BioRxiv, 2018 - biorxiv.org
Putative gain-of-function mutations in leucine-rich repeat kinase 2 (LRRK2), resulting in
increased kinase activity and cellular toxicity, are a leading genetic cause of Parkinson’s …

Biochemical and pharmacological characterization of human c-Met neutralizing monoclonal antibody CE-355621

…, KG Coleman, V Bedian, P Vincent, S Kajiji, SJ Steyn… - MAbs, 2012 - Taylor & Francis
The c-Met proto-oncogene is a multifunctional receptor tyrosine kinase that is stimulated by
its ligand, hepatocyte growth factor (HGF), to induce cell growth, motility and morphogenesis. …

Identification and characterization of PF-03814735, an oral aurora inhibitor for cancer therapy

…, L Pustilnik, K Rafidi, AM Rossi, R Shepard, S Steyn… - Cancer Research, 2008 - AACR
5647 The Aurora kinases, a family of highly related serine/threonine kinases are key regulators
of mitosis. Aurora1 and Aurora2 (also known as AuroraB and AuroraA, respectively) play …