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Pembrolizumab for the treatment of non-small-cell lung cancer.
TLDR
Pembrolizumab had an acceptable side-effect profile and showed antitumor activity in patients with advanced non-small-cell lung cancer and PD-L1 expression in at least 50% of tumor cells correlated with improved efficacy of pembrolIZumab. Expand
Vascular Endothelial Growth Factor Receptor KDR Tyrosine Kinase Activity Is Increased by Autophosphorylation of Two Activation Loop Tyrosine Residues*
TLDR
It is demonstrated that tyrosine kinase antagonists can preferentially inhibit either the unactivated or activated form of the enzyme, which is a consequence of an increased affinity for both ATP and the peptide substrate and has no effect on k cat, the intrinsic catalytic activity of the enzymes. Expand
Effect of the CGRP receptor antagonist BIBN4096BS in human cerebral, coronary and omental arteries and in SK-N-MC cells.
TLDR
CGRP was a weaker agonist on coronary arteries as compared to intracranial arteries; however, BIBN4096BS was an equally effective antagonist; in human omental arteries, CGRP did not induce relaxation. Expand
Characterisation of the effects of a non-peptide CGRP receptor antagonist in SK-N-MC cells and isolated human cerebral arteries.
TLDR
CGRP induced a concentration-dependent relaxation in human cerebral arteries which was antagonized by both C GRP-(8-37) and Compound 1 in a competitive manner, and in guinea pig basilar arteries, CGRP antagonised the CGRp-induced relaxation while Compound1 had a weak blocking effect. Expand
Synthesis and initial SAR studies of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines: a new class of KDR kinase inhibitors.
TLDR
3,6-disubstituted pyrazolo[1,5-a]pyrimidines as a new class of KDR kinase inhibitors and potency against isolated KDR was fully optimized with 3-thienyl and 4-methoxyphenyl substituents at the 6- and 3-positions. Expand
Optimizing PD-L1 as a biomarker of response with pembrolizumab (pembro; MK-3475) as first-line therapy for PD-L1–positive metastatic non-small cell lung cancer (NSCLC): Updated data from KEYNOTE-001.
TLDR
In patients receiving platinum doublets for treatment-naive, metastatic NSCLC without driver mutations, PD-L1 positivity correlated with improved ORR, PFS, and OS, and the relationship between PD- L1 expression levels and efficacy was explored in KEYNOTE-001. Expand
Caprolactams as potent CGRP receptor antagonists for the treatment of migraine.
TLDR
Replacements for the benzodiazepine core of an earlier lead structure 1 including 5-, 6-, and 7-membered lactams were explored and phenyl substitution at various positions afforded the potent (3R)-amino-(6S)-phenyl caprolactam template. Expand
Optimization of a pyrazolo[1,5-a]pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharmacokinetics.
TLDR
Improvements in physical properties of a 3,6-disubstituted pyrazolo[1,5-a]pyrimidine series of KDR kinase inhibitors result in marked increases in cellular activity and more favorable pharmacokinetics in rats. Expand
RPR 107393, a potent squalene synthase inhibitor and orally effective cholesterol-lowering agent: comparison with inhibitors of HMG-CoA reductase.
TLDR
RPR 107393 is an orally effective hypocholesterolemic agent in rats and marmosets that has greater efficacy than lovastatin or pravastatin in the marmoset and in vitro data demonstrate that these compounds are inhibitors of squalene synthase. Expand
LBA43ANTITUMOR ACTIVITY OF PEMBROLIZUMAB (PEMBRO; MK-3475) AND CORRELATION WITH PROGRAMMED DEATH LIGAND 1 (PD-L1) EXPRESSION IN A POOLED ANALYSIS OF PATIENTS (PTS) WITH ADVANCED NON–SMALL CELL LUNG
TLDR
Pembro is tolerable and provides antitumor activity in treatment-naive or previously treated advanced NSCLC, regardless of dose/schedule and may derive particular benefit from pembro with strong PD-L1 tumor expression. Expand
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