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Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors
Structure Mpro SARS-CoV-2 discovery inhibitors
2020/6/12
A new coronavirus, known as severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), is the aetiological agent responsible for the 2019–2020 viral pneumonia outbreak of coronavirus disease 2019 (...
Fusion mechanism of 2019-nCoV and fusion inhibitors targeting HR1 domain in spike protein
Fusion mechanism 2019-nCoV inhibitors targeting HR1 domain spike protein
2020/6/12
Very recently, a novel coronavirus, 2019-nCoV, emerged in Wuhan, China and then quickly spread worldwide, resulting in >17,388 confirmed cases and 361 deaths as of 3 February 2020, thus calling for th...
Anticancer drug discovery:structures of KDM5 histone demethylase inhibitors
Anticancer drug KDM5 histone demethylase inhibitors
2016/8/1
When doctors hurl toxic death at cancer cells, often a few will survive and come back. A family of enzymes called KDM5 histone demethylases is emerging as important for this resilience, and drugs that...
IDENTIFICATION OF NOVEL SMALL MOLECULE INHIBITORS OF PROTEINS REQUIRED FOR GENOMIC MAINTENANCE AND STABILITY
RPA cancer DNA repair
2015/5/25
Targeting uncontrolled cell proliferation and resistance to DNA damaging chemotherapeutics using small molecule inhibitors of proteins involved in these pathways has significant potential in cancer tr...
Identification, kinetic and structural characterization of small molecule inhibitors of aldehyde dehydrogenase 3a1 (Aldh3a1) as an adjuvant therapy for reversing cancer chemo-resistance
cyclophosphamide chemosensitivity structure activity relationships cell culture
2015/5/25
ALDH isoenzymes are known to impact the sensitivity of certain neoplastic cells toward cyclophosphamides and its analogs. Despite its bone marrow toxicity, cyclophos-phamide is still used to treat var...
New systemic therapies for metastatic melanoma – mapk inhibitors and immunotherapy
metastatic melanoma mapk inhibitors
2015/4/7
Metastatic melanoma has a poor prognosis and until recently systemic therapy was ineffective. Advances in the
understanding of tumour biology and immune regulation have led to the development of tar...
Role of APE1 in differentiated neuroblastoma SH-SY5Y cells in response to oxidative stress; Use of APE1 small molecule inhibitors to delineate APE1 functions
base excision repair APE1/Ref-1 oxidative stress
2014/12/12
Oxidative DNA damage has been implicated in a number of central nervous system pathologies. The base excision repair (BER) pathway is one of the most important cellular protection mechanisms that resp...
Small-molecule inhibitors of proteins involved in base excision repair potentiate the anti-tumorigenic effect of existing chemotherapeutics and irradiation
Ape1 inhibitor base excision repair biomarkers
2014/12/12
There has been a recent upsurge in the development of small-molecule inhibitors specific to DNA repair proteins or proteins peripherally involved in base excision repair and the DNA damage response. T...
Effects of Histone Deacetylase Inhibitors on Vitamin D Activity in Human Breast Cancer Cells
Sulforaphane histone deacetylase inhibitors vitamin D receptor
2014/11/7
Breast cancer is one of the leading causes of death in women cancer cases worldwide. Cancer is the result of environmental and genetic factors that contribute to alterations in cellular control, proli...
HISTONE DEACETYLASE INHIBITORS TRICHOSTATIN A (TSA) AND SULFORAPHANE (SFN) MODULATE VITAMIN D RESPONSIVE CYP24 GENE EXPRESSION in 3T3-L1 PREADIPOCYTES
TRICHOSTATIN A (TSA) SULFORAPHANE (SFN), CYP24 3T3-L1 PREADIPOCYTES
2014/11/7
Vitamin D plays an important role in preserving healthy bones, and has additional roles in the body, including modulation of cell growth, differentiation, neuromuscular and immune function, and anti-i...
Selective Serotonin Reuptake Inhibitors and Bone Mineral Density in a Population of U. S. Premenopausal Women
Selective Serotonin Reuptake Inhibitors Bone Mineral Density Bone Mineral Content Dual Energy X-ray Absorptiometry Premenopausal
2014/11/6
Low bone mineral density (BMD) in post-menopausal women is a risk factor for bone fractures and osteoporosis development. Prior studies in post-menopausal women have shown the use of antidepressant me...
Comparison of Bypassing Agents in Bleeding Reduction in Treatment of Bleeding Episodes in Patients With Haemophilia and Inhibitors
Haemophilia Meta-Analysis Bleeding
2015/10/16
Context: Mild-to-moderate bleeding disorders in haemophilia are primarily treated via recombinant activated factor VII a (rFVIIa) or activated prothrombin complex concentrate (aPCC). However, the effi...
Quality of Life in Hemophilia Complicated by Inhibitors
Quality Hemophilia Complicated Inhibitors
2015/9/25
Inhibitors in patients with hemophilia are a rare complication which leads to pain, disability and impairment in quality of life. Recent advances in treatment have improved this situation, doubtful of...
Pattern secretion of matrix Metalloproteinases and their biological tissue inhibitors by human glomerular mesangial cells in culture
Metalloproteinases Mesangial cell Glomerulosclerosis
2010/1/5
The glomerular mesangial cells (GMC) play a central role in the synthesis and turnover of the glomerular mesangial matrix. The breakdown of the matrix likely depends on the balance between of a variet...
Oral candidiasis in HIV+ patients under treatment with protease inhibitors
HIV Candida albicans Protease inhibitors
2009/10/16
The purpose of this work was to evaluate the influence of Protease Inhibitors (PI) on the occurrence of oral candidiasis in 111 HIV+ patients under PI therapy (Group A). The controls consisted of 56 p...