RN486, a selective Bruton's tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents

D Xu, Y Kim, J Postelnek, MD Vu, DQ Hu, C Liao… - … of Pharmacology and …, 2012 - ASPET
Genetic mutation and pharmacological inhibition of Bruton's tyrosine kinase (Btk) both have
been shown to prevent the development of collagen-induced arthritis (CIA) in mice, …

Selective Itk inhibitors block T-cell activation and murine lung inflammation

…, DJ Shuster, XX Yang, R Townsend, J Postelnek… - Biochemistry, 2004 - ACS Publications
Nonreceptor protein tyrosine kinases including Lck, ZAP-70, and Itk play essential roles in T-cell
receptor (TCR) signaling. Gene knockout studies have revealed that mice lacking these …

Suppression of glomerulonephritis in lupus‐prone NZB× NZW mice by RN486, a selective inhibitor of Bruton's tyrosine kinase

…, M Giron, KY Lau, J Hang, J Postelnek… - Arthritis & …, 2013 - Wiley Online Library
Objective Bruton's tyrosine kinase (BTK) plays a critical role in B cell development and function.
We recently described a selective BTK inhibitor, RN486, that blocks B cell receptor (BCR…

Abstract CT180: Preliminary phase 1 profile of BMS-986179, an anti-CD73 antibody, in combination with nivolumab in patients with advanced solid tumors

…, E Hilt, M Donovan, A Gipson, P Basciano, J Postelnek… - Cancer Research, 2018 - AACR
Background: CD73 is an ectonucleotidase that converts adenosine monophosphate to
adenosine, a potent immunosuppressive soluble mediator that inhibits the cytotoxic function of …

A highly selective inhibitor of IκB kinase, BMS-345541, augments graft survival mediated by suboptimal immunosuppression in a murine model of cardiac graft …

RM Townsend, J Postelnek, V Susulic… - …, 2004 - journals.lww.com
Background. We previously demonstrated in vitro and in vivo that an IκB kinase (IKK) inhibitor
blocks cytokine production and suppresses immune responses. These results indicate that …

Novel Pyrrolidine Ureas as C− C Chemokine Receptor 1 (CCR1) Antagonists

…, R Liu, R Zhang, B Jacob, J Postelnek… - Journal of medicinal …, 2009 - ACS Publications
Monocyte infiltration is implicated in a variety of diseases including multiple myeloma,
rheumatoid arthritis, and multiple sclerosis. C−C chemokine receptor 1 (CCR1) is a chemokine …

[HTML][HTML] 606 Biomarker analyses of baseline tumor specimens and on-treatment changes in sera samples of patients enrolled in the RELATIVITY-047 trial to …

…, E Lipson, D Schadendorf, J Wojcik, J Postelnek… - 2022 - jitc.bmj.com
Background The phase 2/3 RELATIVITY-047 clinical trial (NCT03470922) in patients with
previously untreated metastatic or unresectable melanoma met its primary endpoint of …

Development and validation of electrochemiluminescence assays to measure free and total sSLAMF7 in human serum in the absence and presence of elotuzumab

J Postelnek, RJ Neely, MD Robbins, CR Gleason… - The AAPS journal, 2016 - Springer
Elotuzumab is a first in class humanized IgG1 monoclonal antibody for the treatment of
multiple myeloma (MM). Elotuzumab targets the glycoprotein signaling lymphocyte activation …

Fit-for-purpose protein biomarker assay validation strategies using hybrid immunocapture-liquid chromatography-tandem-mass spectrometry platform: quantitative …

Y Zhao, H Gu, J Postelnek, M DeMichele, L Yuan… - Analytica Chimica …, 2020 - Elsevier
In recent years, biomarkers have played more extensive roles as indicators of disease
progression, safety, and drug efficacy. Targeted quantitative analysis of biomarkers including drug …

Novel pyrrolidine heterocycles as CCR1 antagonists

…, MJ Ohlmeyer, E Quadros, P Wines, J Postelnek… - Bioorganic & medicinal …, 2010 - Elsevier
A novel series of pyrrolidine heterocycles was prepared and found to show potent inhibitory
activity of CCR1 binding and CCL3 mediated chemotaxis of a CCR1-expressing cell line. A …