Mark S. Cooper
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View article: Structure-Based Optimization of Pyridone α-Ketoamides as Inhibitors of the SARS-CoV-2 Main Protease
Structure-Based Optimization of Pyridone α-Ketoamides as Inhibitors of the SARS-CoV-2 Main Protease Open
The main protease Mpro is a clinically validated target to treat infections by the coronavirus SARS-CoV-2. Among the first reported Mpro inhibitors was the peptidomimetic α-ketoamide 13b, whose cocrystal structure with Mpro paved the way f…
View article: Development of p300-targeting degraders with enhanced selectivity and onset of degradation
Development of p300-targeting degraders with enhanced selectivity and onset of degradation Open
p300 and CBP are paralogous epigenetic regulators and promising therapeutic targets for which TPD offers the potential to achieve paralog-selective degradation.
View article: Recycling glucocorticoids: therapeutic implications of the 11β-HSD1 enzyme system
Recycling glucocorticoids: therapeutic implications of the 11β-HSD1 enzyme system Open
Endogenous glucocorticoids and commonly used oral glucocorticoids have the property of existing in an inactive and active form in vivo . The inactive form can be converted back to the active form, or ‘recycled’ in cells and tissues that ex…
View article: Impaired alveolar macrophage 11β-hydroxysteroid dehydrogenase type 1 reductase activity contributes to increased pulmonary inflammation and mortality in sepsis-related ARDS
Impaired alveolar macrophage 11β-hydroxysteroid dehydrogenase type 1 reductase activity contributes to increased pulmonary inflammation and mortality in sepsis-related ARDS Open
Background Acute Respiratory Distress Syndrome (ARDS) is a devastating pulmonary inflammatory disorder, commonly precipitated by sepsis. Glucocorticoids are immunomodulatory steroids that can suppress inflammation. Their anti-inflammatory …
View article: Skin 11β-hydroxysteroid dehydrogenase type 1 enzyme expression regulates burn wound healing and can be targeted to modify scar characteristics
Skin 11β-hydroxysteroid dehydrogenase type 1 enzyme expression regulates burn wound healing and can be targeted to modify scar characteristics Open
Background Excessive scarring and fibrosis are the most severe and common complications of burn injury. Prolonged exposure to high levels of glucocorticoids detrimentally impacts on skin, leading to skin thinning and impaired wound healing…
View article: Whether Renal Pathology Is an Independent Predictor for End-Stage Renal Disease in Diabetic Kidney Disease Patients with Nephrotic Range Proteinuria: A Biopsy-Based Study
Whether Renal Pathology Is an Independent Predictor for End-Stage Renal Disease in Diabetic Kidney Disease Patients with Nephrotic Range Proteinuria: A Biopsy-Based Study Open
Aims: To investigate whether renal pathology is an independent predictor for end-stage renal disease (ESRD) in diabetic kidney diseases (DKD) with nephrotic range proteinuria. Methods: A total of 199 DKD patients with nephrotic range prote…
View article: CCDC 2113703: Experimental Crystal Structure Determination
CCDC 2113703: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Diastereomeric Resolution Yields Highly Potent Inhibitor of SARS-CoV-2 Main Protease
Diastereomeric Resolution Yields Highly Potent Inhibitor of SARS-CoV-2 Main Protease Open
SARS-CoV-2 is the causative agent behind the COVID-19 pandemic. The main protease (Mpro, 3CLpro) of SARS-CoV-2 is a key enzyme that processes polyproteins translated from the viral RNA. Mpro is therefore an attractive target for the design…
View article: 11β-Hydroxysteroid Dehydrogenase Type 1 within Osteoclasts Mediates the Bone Protective Properties of Therapeutic Corticosteroids in Chronic Inflammation
11β-Hydroxysteroid Dehydrogenase Type 1 within Osteoclasts Mediates the Bone Protective Properties of Therapeutic Corticosteroids in Chronic Inflammation Open
Therapeutic glucocorticoids (GCs) are powerful anti-inflammatory tools in the management of chronic inflammatory diseases such as rheumatoid arthritis (RA). However, their actions on bone in this context are complex. The enzyme 11β-hydroxy…
View article: Controlled dual release of dihydrotestosterone and flutamide from polycaprolactone electrospun scaffolds accelerate burn wound healing
Controlled dual release of dihydrotestosterone and flutamide from polycaprolactone electrospun scaffolds accelerate burn wound healing Open
Wound healing is a complex process involving multiple independent and overlapping sequential physiological mechanisms. In addition to cutaneous injury, a severe burn stimulates physiological derangements that induce a systemic hypermetabol…
View article: Effect of AZD4017, a Selective 11β-HSD1 Inhibitor, on Bone Turnover Markers in Postmenopausal Osteopenia
Effect of AZD4017, a Selective 11β-HSD1 Inhibitor, on Bone Turnover Markers in Postmenopausal Osteopenia Open
Context The causative link between circulating glucocorticoid excess and osteoporosis is well-established. The enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), which increases local cortisol production, is expressed in human oste…
View article: Inactivation of the CIC-DUX4 oncogene through P300/CBP inhibition, a therapeutic approach for CIC-DUX4 sarcoma
Inactivation of the CIC-DUX4 oncogene through P300/CBP inhibition, a therapeutic approach for CIC-DUX4 sarcoma Open
CIC-DUX4 sarcoma (CDS) is a highly aggressive and metastatic small round type of predominantly pediatric sarcoma driven by a fusion oncoprotein comprising the transcriptional repressor Capicua (CIC) fused to the C-terminal transcriptional …
View article: Endogenous Glucocorticoid Metabolism in Bone: Friend or Foe
Endogenous Glucocorticoid Metabolism in Bone: Friend or Foe Open
The role of tissue specific metabolism of endogenous glucocorticoids (GCs) in the pathogenesis of human disease has been a field of intense interest over the last 20 years, fuelling clinical trials of metabolism inhibitors in the treatment…
View article: Global Deletion of 11β-HSD1 Prevents Muscle Wasting Associated with Glucocorticoid Therapy in Polyarthritis
Global Deletion of 11β-HSD1 Prevents Muscle Wasting Associated with Glucocorticoid Therapy in Polyarthritis Open
Glucocorticoids provide indispensable anti-inflammatory therapies. However, metabolic adverse effects including muscle wasting restrict their use. The enzyme 11beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1) modulates peripheral glucoc…
View article: The contradictory role of androgens in cutaneous and major burn wound healing
The contradictory role of androgens in cutaneous and major burn wound healing Open
Wound healing is a complex process involving four overlapping phases: haemostasis, inflammation, cell recruitment and matrix remodeling. In mouse models, surgical, pharmacological and genetic approaches targeting androgen actions in skin h…
View article: Thermally processed diet-induced albuminuria, Enterobacteriaceae expansion and cecal metabolome alterations are attenuated by resistant starch in diabetes
Thermally processed diet-induced albuminuria, Enterobacteriaceae expansion and cecal metabolome alterations are attenuated by resistant starch in diabetes Open
Background: Modern, processed diets are replete in dietary advanced glycation endproducts (AGEs) which contribute to chronic renal injury. This study investigated whether excess consumption of dietary AGEs alters gut ecology and exacerbate…
View article: Skeletal glucocorticoid signalling determines leptin resistance and obesity in aging mice
Skeletal glucocorticoid signalling determines leptin resistance and obesity in aging mice Open
Skeletal glucocorticoid signalling is critical for the development of leptin resistance, obesity and insulin resistance during aging. These findings underscore the skeleton's importance in the regulation of body weight and implicate osteob…
View article: Cumulative dispensing of high oral corticosteroid doses for treating asthma in Australia
Cumulative dispensing of high oral corticosteroid doses for treating asthma in Australia Open
Cumulative exposure to OCS in Australia reaches levels associated with toxicity in one-quarter of patients with asthma using ICS. Cumulative dispensing of potentially toxic OCS amounts often accompanies inadequate inhaler controller dispen…
View article: Dihydrotestosterone (DHT) Enhances Wound Healing of Major Burn Injury by Accelerating Resolution of Inflammation in Mice
Dihydrotestosterone (DHT) Enhances Wound Healing of Major Burn Injury by Accelerating Resolution of Inflammation in Mice Open
Androgens have been known to inhibit cutaneous wound healing in men and male mice. However, in children with major burn injuries, a synthetic androgen was reported clinically to improve wound healing. The aim of this study is to investigat…
View article: SUN-217 Skin Glucocorticoid Metabolism in Burn Injury: Towards Novel Treatments That Reduce Scarring
SUN-217 Skin Glucocorticoid Metabolism in Burn Injury: Towards Novel Treatments That Reduce Scarring Open
The most common and severe complication of burn injury is the development of excessive scarring/tissue fibrosis. No current treatments reduce scarring after burns. Prolonged exposure to high levels of glucocorticoids (Cushing’s syndrome) d…
View article: SAT-006 Dihydrotestosterone (DHT) Enhances Major Burn Injury Wound Healing by Regulating the Inflammatory Response in Mice
SAT-006 Dihydrotestosterone (DHT) Enhances Major Burn Injury Wound Healing by Regulating the Inflammatory Response in Mice Open
Androgen analogy (Oxandrolone) have been reported to better maintain lean body mass, with improved hypermetabolic responses and shortened healing time for major burn injured patients. This is contradictory to that androgens inhibit local w…
View article: SAT-003 Therapeutic Glucocorticoids Prevent Local and Systemic Bone Loss but Exacerbate Muscle Wasting When Administered in Chronic Inflammation
SAT-003 Therapeutic Glucocorticoids Prevent Local and Systemic Bone Loss but Exacerbate Muscle Wasting When Administered in Chronic Inflammation Open
Glucocorticoids (GCs) are used in the treatment of chronic inflammatory diseases due to their potent anti-inflammatory actions. Their use is limited due to major systemic side effects including osteoporosis and muscle wasting. This is furt…
View article: Vitamin D to Prevent Lung Injury Following Esophagectomy—A Randomized, Placebo-Controlled Trial*
Vitamin D to Prevent Lung Injury Following Esophagectomy—A Randomized, Placebo-Controlled Trial* Open
Objectives: Observational studies suggest an association between vitamin D deficiency and adverse outcomes of critical illness and identify it as a potential risk factor for the development of lung injury. To determine whether preoperative…
View article: Glucocorticoids and Bone: Consequences of Endogenous and Exogenous Excess and Replacement Therapy
Glucocorticoids and Bone: Consequences of Endogenous and Exogenous Excess and Replacement Therapy Open
Osteoporosis associated with long-term glucocorticoid therapy remains a common and serious bone disease. Additionally, in recent years it has become clear that more subtle states of endogenous glucocorticoid excess may have a major impact …