S. Knapp

This study investigates how Parkinson's Disease mutations affect LRRK2 activation and subcellular localization through conformational changes and domain interactions.

The paper identifies DFG-1 residues as a target for designing selective kinase inhibitors with non-canonical binding modes, showing that bulky DFG-1 residues enable selectivity over smaller ones.

This paper describes the optimization of pyrazolopyrimidine compounds to develop a highly selective and potent CK2 inhibitor, IC20, with high in vitro potency and exclusive selectivity.

This study presents the structure of ULK4-ATPγS complex, identifies disease mutations affecting ATP binding, and reveals ULK4's interaction partners and evolutionary adaptations.

This study presents MKK7 crystal structures and identifies new allosteric targets, revealing structural mechanisms of activation and potential drug candidates.

This study identifies STK32A as a dual-specificity AGC kinase preferring acidic substrates, revealing structural and evolutionary features supporting its substrate specificity.

The paper develops a selective chemical probe, TP-008, for ALK4 and ALK5 kinases and provides a negative control, enabling mechanistic studies of their signaling pathway and disease roles.

The paper introduces the Kinase Chemogenomic Set (KCGS), a curated collection of 187 selective kinase inhibitors covering 215 human kinases, for use in cell-based screens.

The paper characterizes piperazine-urea derivatives as acetyl/acyl-lysine mimetics for MLLT1 and reveals distinct interaction mechanisms through crystal structures.

The paper shows that TAp63 uses a slow third phosphorylation step to set a threshold for apoptosis induction in response to DNA damage.

The paper presents the crystal structure of ULK2 with ATP inhibitors, identifies off-target effects of ULK1 inhibitors, and suggests structural insights for developing dual ULK1/2 inhibitors.

The paper identifies inhibitory fragments targeting the ENL YEATS domain using crystallography, providing starting points for chemical probe development.

The paper examines how dispersal events and climatic changes have shaped the diversification of the plant genus Solanum, finding that Old World lineages are diversifying more rapidly following a long-distance dispersal event.

The paper presents a set of 25 chemical probes targeting human bromodomains and demonstrates their utility in studying muscle cell differentiation and triple negative breast cancer.

The paper describes SGC-GAK-1, a selective GAK inhibitor, and identifies a related compound that inhibits RIPK2 without GAK activity, providing tools to study GAK and RIPK2 biology.

The paper identifies potential small molecule binding sites at domain-domain interfaces of epigenetic proteins using computational and experimental methods.

The paper shows that halogen-aromatic π-interactions increase inhibitor residence time in kinase-inhibitor complexes, providing a strategy to improve drug efficacy and selectivity.

This study uses molecular and morphological data to reconstruct the phylogeny of the butterfly genus Pteronymia, showing its origin in the Northern Andes and diversification patterns.

The paper shares progress on a kinase chemogenomic set, releases inhibitor profiling data, and calls for community collaboration to complete the set.