Kallikrein-related peptidase 6 (KLK6) is a secreted serine protease that belongs to the family of tissue kallikreins. Aberrant expression of KLK6 has been found in different cancers and neurodegenerative diseases, and KLK6 is currently studied as a potential target in these pathologies. We report a novel series of KLK6 inhibitors discovered in a high-throughput screen within the European Lead Factory program. Structure-guided design based on docking studies enabled rapid progression of a hit cluster to inhibitors with improved potency, selectivity and pharmacokinetic properties. In particular, inhibitors 32 ((5R)-3-(4-carbamimidoylphenyl)-N-((S)-1-(naphthalen-1-yl)propyl)-2-oxooxazolidine-5-carboxamide) and 34 ((5R)-3-(6-carbamimidoylpyridi...
Les KLK6 et KLK8 sont des protéases à sérine (PAS) essentielles pour l'homéostasie du système nerveu...
Although kallikrein-related peptidase 10 (KLK10) is expressed in a variety of human tissues and body...
As cancer-associated factors, kallikrein-related peptidases (KLKs) are components of the tumour micr...
Pancreatic cancer has the lowest survival rate of all common cancers due to late diagnosis and limit...
AbstractIncluding the true tissue kallikrein KLK1, kallikrein-related peptidases (KLKs) represent a ...
Kallikrein-related peptidase 6 (KLK6) is a secreted serine protease that belongs to the family of ti...
Kallikrein-related peptidase 6 (KLK6) is a secreted serine protease that belongs to the family of ti...
Introduction: Novel therapeutic compounds are needed for prostate cancer (CaP), given the limitation...
Pancreatic cancer has the lowest survival rate of all common cancers due to late diagnosis and limit...
International audienceThe activity of kallikrein-related peptidase 6 (KLK6) is deregulated in variou...
The kallikreins and kallikrein-related peptidases are serine proteases that control a plethora of de...
Human kallikrein 5 (KLK5) and 7 (KLK7) are potential targets for the treatment of skin inflammation ...
Including the true tissue kallikrein KLK1, kallikrein-related peptidases (KLKs) represent a family o...
Although kallikrein-related peptidase 10 (KLK10) is expressed in a variety of human tissues and body...
Human kallikrein-related peptidases (KLKs) are 15 homologous serine proteases involved in several (p...
Les KLK6 et KLK8 sont des protéases à sérine (PAS) essentielles pour l'homéostasie du système nerveu...
Although kallikrein-related peptidase 10 (KLK10) is expressed in a variety of human tissues and body...
As cancer-associated factors, kallikrein-related peptidases (KLKs) are components of the tumour micr...
Pancreatic cancer has the lowest survival rate of all common cancers due to late diagnosis and limit...
AbstractIncluding the true tissue kallikrein KLK1, kallikrein-related peptidases (KLKs) represent a ...
Kallikrein-related peptidase 6 (KLK6) is a secreted serine protease that belongs to the family of ti...
Kallikrein-related peptidase 6 (KLK6) is a secreted serine protease that belongs to the family of ti...
Introduction: Novel therapeutic compounds are needed for prostate cancer (CaP), given the limitation...
Pancreatic cancer has the lowest survival rate of all common cancers due to late diagnosis and limit...
International audienceThe activity of kallikrein-related peptidase 6 (KLK6) is deregulated in variou...
The kallikreins and kallikrein-related peptidases are serine proteases that control a plethora of de...
Human kallikrein 5 (KLK5) and 7 (KLK7) are potential targets for the treatment of skin inflammation ...
Including the true tissue kallikrein KLK1, kallikrein-related peptidases (KLKs) represent a family o...
Although kallikrein-related peptidase 10 (KLK10) is expressed in a variety of human tissues and body...
Human kallikrein-related peptidases (KLKs) are 15 homologous serine proteases involved in several (p...
Les KLK6 et KLK8 sont des protéases à sérine (PAS) essentielles pour l'homéostasie du système nerveu...
Although kallikrein-related peptidase 10 (KLK10) is expressed in a variety of human tissues and body...
As cancer-associated factors, kallikrein-related peptidases (KLKs) are components of the tumour micr...