Promega Corporation

Celtaxsys, Inc.

Celltaxis, LLC

Celltaxsis, LLC

Estrellita Pharmaceuticals, LLC

Thomas A Kirkland

Keith V Wood

Mary P Hall

Thomas Machleidt

Poncho Meisenheimer

Lance P Encell

Rachel Friedman Ohana

Melanie Dart

Brock Binkowski

Matthew B Robers

Joel R Walker

Nidhi Nath

Anton Shakhmin

Carolyn Woodroofe Hitko

Marie Schwinn

Monika G Wood

Said A Goueli

James Unch

Andrew S Dixon

Hicham Zegzouti

Subhanjan Mondal

Dileep K Pulukkunat

Ce Shi

Harry Tetsuo Uyeda

William J Guilford

Wenhui Zhou

Arwed Cleve

Monica J Kochanny

David Richard Light

Bin Ye

Guo Ping Wei

John V Parkinson

Seock-Kyu Khim

Sergiy Levin

Greg Brown

Emmanuel Claret

Ji Zhu

Amy Liang

David D Davey

Mark McDougall

Damian O Arnaiz

Robin Hurst

Dieter Klaubert

Paul Otto

Marjeta Urh

Stephen J Dwight

Michael Killoran

Matt Robers

Andrew L Niles

David Vogel

Martha A O'Brien

Min Zhou

Thomas P Smith

David Davey

Brock F Binkowski

Mark G Mcdougall

Mark Mcdougall

Martha O'BRIEN

Described are substituted imidazo[1,2-a]pyrazine compounds, which are coelenterazine analogues, kits comprising the analogues, and methods of using the compounds for the detection of luminescence in luciferase-based assays. Also described are methods from making the compounds, such as a method using aminopyrazine acetophosphonates as synthesis intermediates.

Substituted imidazo[1,2-α]pyrazines as luciferase substrates

Provided herein are compositions and methods for the assembly of a bioluminescent complex from two or more non-luminescent (e.g., substantially non-luminescent) peptide and/or polypeptide units. In particular, bioluminescent activity is conferred upon a non-luminescent polypeptide via structural complementation with another, complementary non-luminescent peptide.

Activation of bioluminescence by structural complementation

The present invention provides haloalkane substrates, and linkers for connecting such substrates to functional elements (e.g., tags, labels, surfaces, etc.). Substrates and linkers described herein find use, for example, in labeling, detection, and immobilization of proteins, cells, and molecules. In particular, the linkers provided herein find use within substrates for dehalogenase variants that form covalent bonds with their haloalkane substrates.

Substrates for covalent tethering of proteins to functional groups or solid surfaces

This invention is directed to compounds of formula (I): where r, q, R, R, R, R, R, R, R, R, R, R, R, R, and Rare described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene Ahydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

Diamine derivatives as inhibitors of leukotriene Ahydrolase

Provided herein are compositions and methods for photoaffinity labeling of molecular targets. In particular, probes that specifically interact with cellular targets based on their affinity and are then covalently linked to the cellular target via a photoreactive group (PRG) on the probe.

Photoaffinity probes

Provided herein are systems and methods for characterizing target/ligand engagement. In particular, luciferase-labeled polypeptide targets are used to detect or quantify target/ligand engagement (e.g., within a cell or cell lysate).

Luciferase-based thermal shift assays

Described are processes for preparing substituted imidazo[1,2-a]pyrazine compounds of formula (I): by reacting a compound of formula (xi): with carbonyldiimidazole to form the compound of formula (I).

Process for preparing substituted imidazo[1,2-&#x3b1;]pyrazines

Provided herein are enhanced luciferase enzymes for use with thermostable luciferin analogs for bioluminescent assays. In particular, the present disclosure provides compositions, assays, and methods for performing a bioluminescent assay using enhanced, high-activity luciferase enzymes compatible with thermostable luciferins, such as 5,5-disubstituted luciferin analogs.

Luciferase enzymes for use with thermostable luciferins in bioluminescent assays

Provided herein are compositions and methods for detection and analysis of intracellular binding of a bioactive agent to a cellular target. In particular, bioactive agents tethered to fluorophores, cellular targets fused to bioluminescent reporters, and methods of detecting and analyzing the interaction of bioactive agents with cellular targets therewith.

Recognition of cellular target binding by a bioactive agent using intracellular bioluminescence resonance energy transfer

Described are coelenterazine analogues, methods for making the analogues, kits comprising the analogues, and methods of using the compounds for the detection of luminescence in luciferase-based assays.

Coelenterazine analogues

Provided herein are cell-permeable, cell-compatible, and chemoselectively-cleavable linkers for tethering (e.g., covalently) functional elements (e.g., a cellular interaction element and a capture element), and methods of use (e.g., intracellular capture and extracellular release of cellular targets) therewith.

Cell-permeable, cell-compatible, and cleavable linkers for covalent tethering of functional elements

Provided herein are compositions and methods for stabilizing coelenterazine and analogs or derivatives thereof, and for improving the solubility and reconstitution efficiency of coelenterazine and analogs and derivatives thereof.

Compositions and methods for stabilizing coelenterazine and analogs and derivatives thereof

Activation of bioluminescene by structural complementation

Growing community of inventors

Atascadero, CA, United States of America

Thomas A Kirkland