Search Results - "Juba, Brian"
-
1
Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1‑((2S,5R)‑5-((7H‑Pyrrolo[2,3‑d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans
Published in Journal of medicinal chemistry (09-03-2017)“…Significant work has been dedicated to the discovery of JAK kinase inhibitors resulting in several compounds entering clinical development and two FDA approved…”
Get full text
Journal Article -
2
Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors
Published in Journal of medicinal chemistry (13-12-2018)“…Ongoing interest in the discovery of selective JAK3 inhibitors led us to design novel covalent inhibitors that engage the JAK3 residue Cys909 by cyanamide, a…”
Get full text
Journal Article -
3
Microfluidic-Enabled Intracellular Delivery of Membrane Impermeable Inhibitors to Study Target Engagement in Human Primary Cells
Published in ACS chemical biology (15-12-2017)“…Biochemical screening is a major source of lead generation for novel targets. However, during the process of small molecule lead optimization, compounds with…”
Get full text
Journal Article -
4
Aminopyrazole Carboxamide Bruton’s Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning
Published in ACS medicinal chemistry letters (10-01-2019)“…Potent covalent inhibitors of Bruton’s tyrosine kinase (BTK) based on an aminopyrazole carboxamide scaffold have been identified. Compared to acrylamide-based…”
Get full text
Journal Article -
5
ATP-Mediated Kinome Selectivity: The Missing Link in Understanding the Contribution of Individual JAK Kinase Isoforms to Cellular Signaling
Published in ACS chemical biology (18-07-2014)“…Kinases constitute an important class of therapeutic targets being explored both by academia and the pharmaceutical industry. The major focus of this effort…”
Get full text
Journal Article -
6
Efficacy of Vitamin D compounds to modulate estrogen receptor negative breast cancer growth and invasion
Published in Journal of steroid biochemistry and molecular biology (01-02-2003)“…In estrogen receptor (ER) positive breast cancer cells such as MCF-7 cells, the anti-tumor effects of 1,25(OH) 2D 3 (1,25D 3) may be secondary to disruption of…”
Get full text
Journal Article Conference Proceeding