Unleashing the therapeutic potential of human kallikrein-related serine proteases
Tissue kallikreins are a family of fifteen secreted serine proteases encoded by the largest
protease gene cluster in the human genome. In the past decade, substantial progress has …
protease gene cluster in the human genome. In the past decade, substantial progress has …
Disulfide-rich macrocyclic peptides as templates in drug design
Recently disulfide-rich head-to-tail cyclic peptides have attracted the interest of medicinal
chemists owing to their exceptional thermal, chemical and enzymatic stability brought about …
chemists owing to their exceptional thermal, chemical and enzymatic stability brought about …
Sunflower trypsin Inhibitor‐1 (SFTI‐1): sowing seeds in the fields of chemistry and biology
Nature‐derived cyclic peptides have proven to be a vast source of inspiration for advancing
modern pharmaceutical design and synthetic chemistry. The focus of this Review is …
modern pharmaceutical design and synthetic chemistry. The focus of this Review is …
The kallikrein-related peptidase family: Dysregulation and functions during cancer progression
Cancer is the second leading cause of death with 14 million new cases and 8.2 million
cancer-related deaths worldwide in 2012. Despite the progress made in cancer therapies …
cancer-related deaths worldwide in 2012. Despite the progress made in cancer therapies …
Design and synthesis of truncated EGF-A peptides that restore LDL-R recycling in the presence of PCSK9 in vitro
CI Schroeder, JE Swedberg, JM Withka… - Chemistry & biology, 2014 - cell.com
Disrupting the binding interaction between proprotein convertase (PCSK9) and the
epidermal growth factor-like domain A (EGF-A domain) in the low-density lipoprotein …
epidermal growth factor-like domain A (EGF-A domain) in the low-density lipoprotein …
Diarylethene‐Based Photoswitchable Inhibitors of Serine Proteases
A bicyclic peptide scaffold was chemically adapted to generate diarylethene‐based
photoswitchable inhibitors of serine protease Bos taurus trypsin 1 (T1). Starting from a …
photoswitchable inhibitors of serine protease Bos taurus trypsin 1 (T1). Starting from a …
Engineered protease inhibitors based on sunflower trypsin inhibitor-1 (SFTI-1) provide insights into the role of sequence and conformation in Laskowski mechanism …
Laskowski inhibitors regulate serine proteases by an intriguing mode of action that involves
deceiving the protease into synthesizing a peptide bond. Studies exploring naturally …
deceiving the protease into synthesizing a peptide bond. Studies exploring naturally …
Design of potent and selective cathepsin G inhibitors based on the sunflower trypsin inhibitor-1 scaffold
Neutrophils are directly responsible for destroying invading pathogens via reactive oxygen
species, antimicrobial peptides, and neutrophil serine proteases (NSPs). Imbalance …
species, antimicrobial peptides, and neutrophil serine proteases (NSPs). Imbalance …
Kallikrein-related peptidases (KLKs) as emerging therapeutic targets: focus on prostate cancer and skin pathologies
M Avgeris, A Scorilas - Expert opinion on therapeutic targets, 2016 - Taylor & Francis
Introduction: Tissue kallikrein and the kallikrein-related peptidases (KLKs) constitute a family
of 15 homologous secreted serine proteases with trypsin-or chymotrypsin-like activities …
of 15 homologous secreted serine proteases with trypsin-or chymotrypsin-like activities …
Metastasis of ovarian cancer is mediated by kallikrein related peptidases
Y Dong, D Loessner, H Irving-Rodgers… - Clinical & experimental …, 2014 - Springer
Ovarian cancer, in particular epithelial ovarian cancer (EOC), is commonly diagnosed when
the tumor has metastasized into the abdominal cavity with an accumulation of ascites fluid …
the tumor has metastasized into the abdominal cavity with an accumulation of ascites fluid …