Remodelling of the tumour microenvironment by the kallikrein-related peptidases
Kallikrein-related peptidases (KLKs) are critical regulators of the tumour microenvironment.
KLKs are proteolytic enzymes regulating multiple functions of bioactive molecules including …
KLKs are proteolytic enzymes regulating multiple functions of bioactive molecules including …
The versatility of boron in biological target engagement
DB Diaz, AK Yudin - Nature Chemistry, 2017 - nature.com
Boron-containing molecules have been extensively used for the purposes of chemical
sensing, biological probe development and drug discovery. Due to boron's empty p orbital, it …
sensing, biological probe development and drug discovery. Due to boron's empty p orbital, it …
Boron containing compounds as protease inhibitors
R Smoum, A Rubinstein, VM Dembitsky… - Chemical …, 2012 - ACS Publications
Proteases form one of the largest and more important groups of enzymes. They selectively
catalyze the hydrolysis of peptide bonds and can be divided into four major classes …
catalyze the hydrolysis of peptide bonds and can be divided into four major classes …
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 …
Boron chemicals in diagnosis and therapeutics
Advances in the field of boron chemistry have expanded the application of boron from
material use to medicine. Boron-based drugs represent a new class of molecules that …
material use to medicine. Boron-based drugs represent a new class of molecules that …
Boronic acids in medicinal chemistry: anticancer, antibacterial and antiviral applications
PC Trippier, C McGuigan - MedChemComm, 2010 - pubs.rsc.org
In 2003, bortezomib, a first-in-class therapeutic, gained approval from the US Federal Drug
Administration for the treatment of relapsed multiple myeloma and mantle cell lymphoma …
Administration for the treatment of relapsed multiple myeloma and mantle cell lymphoma …
α-Aminoboronates: recent advances in their preparation and synthetic applications
W Ming, HS Soor, X Liu, A Trofimova… - Chemical Society …, 2021 - pubs.rsc.org
α-Aminoboronic acids and their derivatives are useful as bioactive agents. Thus far, three
compounds containing an α-aminoboronate motif have been approved by the Food and …
compounds containing an α-aminoboronate motif have been approved by the Food and …
Beyond the biomarker role: prostate-specific antigen (PSA) in the prostate cancer microenvironment
The prostate-specific antigen (PSA) blood test is the accepted biomarker of tumor
recurrence. PSA levels in serum correlate with disease progression, though its diagnostic …
recurrence. PSA levels in serum correlate with disease progression, though its diagnostic …
[HTML][HTML] Natural and synthetic inhibitors of kallikrein-related peptidases (KLKs)
P Goettig, V Magdolen, H Brandstetter - Biochimie, 2010 - Elsevier
Including the true tissue kallikrein KLK1, kallikrein-related peptidases (KLKs) represent a
family of fifteen mammalian serine proteases. While the physiological roles of several KLKs …
family of fifteen mammalian serine proteases. While the physiological roles of several KLKs …
Aminoboronic acids and esters: from synthetic challenges to the discovery of unique classes of enzyme inhibitors
S Touchet, F Carreaux, B Carboni, A Bouillon… - Chemical Society …, 2011 - pubs.rsc.org
Although boronic acids have attracted considerable interest as versatile intermediates in
organic synthesis, their contributions in chemical biology and drug discovery programs have …
organic synthesis, their contributions in chemical biology and drug discovery programs have …