Structural biology and drug discovery

G Scapin - Current pharmaceutical design, 2006 - ingentaconnect.com
In the past few years macromolecular crystallography has become a standard technique
used by many pharmaceutical and biotechnology companies. This methodology offers …

New approaches to the treatment of inflammatory disorders small molecule inhibitors of p38 MAP kinase

C Peifer, G Wagner, S Laufer - Current topics in medicinal …, 2006 - ingentaconnect.com
The therapy of chronic inflammatory diseases like rheumatoid arthritis (RA) and
inflammatory bowel disease (IBD) has recently been enriched by the successful launch of …

P38 inhibitors and methods of use thereof

M Munson, DA Mareska, Y Kim… - US Patent …, 2010 - Google Patents
2009-02-04 Assigned to ARRAY BIOPHARMA, INC. reassignment ARRAY BIOPHARMA,
INC. ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS) …

Structural basis for p38α MAP kinase quinazolinone and pyridol-pyrimidine inhibitor specificity

CE Fitzgerald, SB Patel, JW Becker… - Nature Structural & …, 2003 - nature.com
The quinazolinone and pyridol-pyrimidine classes of p38 MAP kinase inhibitors have a
previously unseen degree of specificity for p38 over other MAP kinases. Comparison of the …

SAR of 3, 4-Dihydropyrido [3, 2-d] pyrimidone p38 Inhibitors

L Liu, JE Stelmach, SR Natarajan, MH Chen… - Bioorganic & medicinal …, 2003 - Elsevier
Development for a class of potent 3, 4-dihydropyrido (3, 2-d) pyrimidone inhibitors of p38a
MAP kinase is described. Modification of N-1 aryl and C-6 arylsulfide in 3, 4-dihydropyrido …

Small molecular anti‐cytokine agents

G Wagner, S Laufer - Medicinal research reviews, 2006 - Wiley Online Library
The recent successful introduction of the anti‐cytokine biologicals Etanercept, Infliximab,
Adalimumab, and Anakinra has stimulated the search for anti‐cytokine small‐molecules. A …

P38 inhibitors and methods of use thereof

M Munson, J Rizzi, M Rodriguez, G Kim - US Patent 7,135,575, 2006 - Google Patents
This invention relates to inhibitors of p38, and methods for producing these inhibitors. The
invention also provides pharmaceutical compositions comprising the inhibitors of the …

Inhibition of p38 MAPK activity leads to cell type-specific effects on the molecular circadian clock and time-dependent reduction of glioma cell invasiveness

CS Goldsmith, SM Kim, N Karunarathna, N Neuendorff… - BMC cancer, 2018 - Springer
Background The circadian clock is the basis for biological time keeping in eukaryotic
organisms. The clock mechanism relies on biochemical signaling pathways to detect …

Kinase inhibitors as drugs for chronic inflammatory and immunological diseases: progress and challenges

LL Rokosz, JR Beasley, CDI Carroll, T Lin… - Expert opinion on …, 2008 - Taylor & Francis
At the time of writing, there are seven marketed kinase inhibitor drugs. The first kinase
inhibitor, imatinib mesilate (Gleevec®, Novartis), came to market in 2001, an inhibitor of the …

Microwave-assisted ullmann C− S bond formation: synthesis of the P38α MAPK clinical candidate VX-745

MC Bagley, T Davis, MC Dix, V Fusillo… - The Journal of …, 2009 - ACS Publications
Microwave irradiation promotes the rapid and efficient reaction of a thiophenol and aryl or
heteroaryl halide using a copper or palladium catalyst and a range of ligands, depending …