Orally absorbed cyclic peptides
DS Nielsen, NE Shepherd, W Xu, AJ Lucke… - Chemical …, 2017 - ACS Publications
Peptides and proteins are not orally bioavailable in mammals, although a few peptides are
intestinally absorbed in small amounts. Polypeptides are generally too large and polar to …
intestinally absorbed in small amounts. Polypeptides are generally too large and polar to …
[HTML][HTML] Systemic delivery of peptides by the oral route: Formulation and medicinal chemistry approaches
In its 33 years, ADDR has published regularly on the po5tential of oral delivery of biologics
especially peptides and proteins. In the intervening period, analysis of the preclinical and …
especially peptides and proteins. In the intervening period, analysis of the preclinical and …
Drug–target kinetics in drug discovery
PJ Tonge - ACS chemical neuroscience, 2018 - ACS Publications
The development of therapies for the treatment of neurological cancer faces a number of
major challenges including the synthesis of small molecule agents that can penetrate the …
major challenges including the synthesis of small molecule agents that can penetrate the …
Orthosteric and allosteric action of the C5a receptor antagonists
The C5a receptor (C5aR) is a G-protein-coupled receptor (GPCR) that can induce strong
inflammatory response to the anaphylatoxin C5a. Targeting C5aR has emerged as a novel …
inflammatory response to the anaphylatoxin C5a. Targeting C5aR has emerged as a novel …
Preclinical pharmacokinetics of complement C5a receptor antagonists PMX53 and PMX205 in mice
The cyclic hexapeptides PMX53 and PMX205 are potent noncompetitive inhibitors of
complement C5a receptor 1 (C5aR1). They are widely utilized to study the role of C5aR1 in …
complement C5a receptor 1 (C5aR1). They are widely utilized to study the role of C5aR1 in …
Pharmacological characterisation of small molecule C5aR1 inhibitors in human cells reveals biased activities for signalling and function
The complement fragment C5a is a core effector of complement activation. C5a, acting
through its major receptor C5aR1, exerts powerful pro-inflammatory and immunomodulatory …
through its major receptor C5aR1, exerts powerful pro-inflammatory and immunomodulatory …
G protein–coupled receptors in asthma therapy: pharmacology and drug action
Asthma is a heterogeneous inflammatory disease of the airways that is associated with
airway hyperresponsiveness and airflow limitation. Although asthma was once simply …
airway hyperresponsiveness and airflow limitation. Although asthma was once simply …
Crystal structures of protein-bound cyclic peptides
Cyclization is an important post-translational modification of peptides and proteins that
confers key advantages such as protection from proteolytic degradation, altered solubility …
confers key advantages such as protection from proteolytic degradation, altered solubility …
Protein–ligand (un) binding kinetics as a new paradigm for drug discovery at the crossroad between experiments and modelling
In the last three decades, protein and nucleic acid structure determination and
comprehension of the mechanisms, leading to their physiological and pathological …
comprehension of the mechanisms, leading to their physiological and pathological …
Pharmacological inhibition of complement C5a‐C5a1 receptor signalling ameliorates disease pathology in the hSOD1G93A mouse model of amyotrophic lateral …
Background and Purpose Amyotrophic lateral sclerosis (ALS) is a fatal and rapidly
progressing motor neuron disease without effective treatment. The complement system is up …
progressing motor neuron disease without effective treatment. The complement system is up …