Protease inhibitors: current status and future prospects
D Leung, G Abbenante, DP Fairlie - Journal of medicinal chemistry, 2000 - ACS Publications
The four major classes of protease enzymes1-4 (aspartic, serine, cysteine, and metallo)
selectively catalyze the hydrolysis of polypeptide bonds. Their control over protein synthesis, …
selectively catalyze the hydrolysis of polypeptide bonds. Their control over protein synthesis, …
Protease inhibitors in the clinic
G Abbenante, DP Fairlie - Medicinal Chemistry, 2005 - ingentaconnect.com
This review describes the clinical status (based on available information) of experimental
drugs that inhibit enzymes called proteases, or more precisely a sub-class of proteases called …
drugs that inhibit enzymes called proteases, or more precisely a sub-class of proteases called …
[HTML][HTML] Macrocyclic peptidomimetics-forcing peptides into bioactive conformations
DP Fairlie, G Abbenante… - Current medicinal …, 1995 - books.google.com
Cyclic peptides that are potent regulators of biological processes are rapidly emerging as
important mechanistic probes and drug leads. Nature clearly uses macrocycles to, constrain …
important mechanistic probes and drug leads. Nature clearly uses macrocycles to, constrain …
[HTML][HTML] Activity of recombinant dengue 2 virus NS3 protease in the presence of a truncated NS2B co-factor, small peptide substrates, and inhibitors
…, H White, NX Fang, MJ Stoermer, G Abbenante… - Journal of Biological …, 2001 - ASBMB
… trityl resin (substitution value = 0.96 mmol/g) and subsequently cleaved from the solid
support with 95% TFA, 2.5% triisopropylsilane, and 2.5% water (15 ml/g resin) for 1 h at room …
support with 95% TFA, 2.5% triisopropylsilane, and 2.5% water (15 ml/g resin) for 1 h at room …
Single turn peptide alpha helices with exceptional stability in water
NE Shepherd, HN Hoang, G Abbenante… - Journal of the …, 2005 - ACS Publications
… (∼1.0 mmol/g) and Rink-amide MBHA resin (∼0.70 mmol/g) encouraging intermolecular …
resin (Tentagel S RAM 0.25 mmol/g) 34 significantly improved the yield and purity of the …
resin (Tentagel S RAM 0.25 mmol/g) 34 significantly improved the yield and purity of the …
[HTML][HTML] Isolation and characterization of a cone snail protease with homology to CRISP proteins of the pathogenesis-related protein superfamily
… Extracted material was collected and centrifuged at 10,000 × g for 30 min (4 C). The
supernatant was concentrated with an Ultrafree 15 Biomax 5K cutoff centrifugal filter (Millipore) in …
supernatant was concentrated with an Ultrafree 15 Biomax 5K cutoff centrifugal filter (Millipore) in …
[HTML][HTML] A small molecule C5a receptor antagonist protects kidneys from ischemia/reperfusion injury in rats
TV Arumugam, IA Shiels, AJ Strachan, G Abbenante… - Kidney international, 2003 - Elsevier
… Female Wistar rats (250 to 300 g) were fasted and given water only for 12 hours prior to all
experiments. Animals were anesthetized by intraperitoneal injection of zolazepam (25 mg/kg -…
experiments. Animals were anesthetized by intraperitoneal injection of zolazepam (25 mg/kg -…
Downsizing human, bacterial, and viral proteins to short water-stable alpha helices that maintain biological potency
…, VS Desai, PR Young, G Abbenante… - Proceedings of the …, 2010 - National Acad Sciences
… We also chose to mimic a “superagonist” of the G protein-coupled receptor known as ORL-1
based on the native ligand nociceptin(1–17), a peptide hormone important in sensory …
based on the native ligand nociceptin(1–17), a peptide hormone important in sensory …
Conformational selection of inhibitors and substrates by proteolytic enzymes: implications for drug design and polypeptide processing
…, RC Reid, AK Wong, G Abbenante… - Journal of Medicinal …, 2000 - ACS Publications
Inhibitors of proteolytic enzymes (proteases) are emerging as prospective treatments for
diseases such as AIDS and viral infections, cancers, inflammatory disorders, and Alzheimer's …
diseases such as AIDS and viral infections, cancers, inflammatory disorders, and Alzheimer's …
Over one hundred peptide-activated G protein-coupled receptors recognize ligands with turn structure
JDA Tyndall, B Pfeiffer, G Abbenante… - Chemical …, 2005 - ACS Publications
G protein-coupled receptors (GPCRs) are seven transmembrane helical bundle proteins (Figure
1) found on the surface of all cells. 1-3 They mediate cellular responses to a diverse …
1) found on the surface of all cells. 1-3 They mediate cellular responses to a diverse …