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#Inhibitors

Nature.com

Discovery of novel DprE1 inhibitors via computational bioactivity fingerprints and structure-based virtual screening

Decaprenylphosphoryl-β-D-ribose oxidase (DprE1) plays important roles in the biosynthesis of mycobacterium cell wall. DprE1 inhibitors have shown great potentials in the development of new regimens for tuberculosis (TB) treatment. In this study, an integrated molecular modeling strategy, which combined computational bioactivity fingerprints and structure-based virtual screening, was employed to identify potential DprE1 inhibitors. Two lead compounds (B2 and H3) that could inhibit DprE1 and thus kill Mycobacterium smegmatis in vitro were identified. Moreover, compound H3 showed potent inhibitory activity against Mycobacterium tuberculosis in vitro (MICMtb"‰="‰1.25"‰Î¼M) and low cytotoxicity against mouse embryo fibroblast NIH-3T3 cells. Our research provided an effective strategy to discover novel anti-TB lead compounds.
SCIENCE
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pharmacytimes.com

TAK1-Inhibitors Offer Potential Treatment Strategy for Patients With Multiple Myeloma

TAK1-inhibitors—alone and in combination with melphalan—are cytotoxic to multiple myeloma cells, which could indicate that TAK1 is a promising drug target for the treatment of multiple myeloma, according to a study published in Oncotarget. TAK1 restricts receptor-interacting serine/threonine-protein kinase 1 dependent cell death, and targeting TAK1 with inhibitors shifts cells from pro-survival programs to cell death, according to the study.
CANCER
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mdedge.com

Few JAK inhibitor users have diminished immune response to COVID-19 vaccines

Patients who are being treated with Janus kinase (JAK) inhibitors overall show a high immune response rate to COVID-19 vaccination, one that matches the rates seen in patients on other immunosuppressants, a new study has found. The patients taking a JAK inhibitor who are most at risk of a diminished...
SCIENCE
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TRENDING TOPICS
drugtargetreview.com

Medicenna’s MDNA11 a promising alternative to checkpoint inhibitors

Medicenna’s IL-2 super-agonist, MDNA11, successfully induced antitumour cells in animal models, a pre-clinical study has revealed. Medicenna has announced the presentation of positive pre-clinical data from its MDNA11 programme evaluating Medicenna’s selective, long-acting and novel IL-2 super-agonist, MDNA11, in murine and IND-enabling non-human primates (NHPs). Murine studies evaluated the anti-tumour...
MEDICAL & BIOTECH
Nature.com

A small molecule screen identifies novel inhibitors of mechanosensory nematocyst discharge in Hydra

Cnidarians are characterized by the possession of stinging organelles, called nematocysts, which they use for prey capture and defense. Nematocyst discharge is controlled by a mechanosensory apparatus with analogies to vertebrate hair cells. Members of the transient receptor potential (TRPN) ion channel family are supposed to be involved in the transduction of the mechanical stimulus. A small molecule screen was performed to identify compounds that affect nematocyst discharge in Hydra. We identified several [2.2]paracyclophanes that cause inhibition of nematocyst discharge in the low micro-molar range. Further structure"“activity analyses within the compound class of [2.2]paracyclophanes showed common features that are required for the inhibitory activity of the [2.2]paracyclophane core motif. This study demonstrates that Hydra can serve as a model for small molecule screens targeting the mechanosensory apparatus in native tissues.
SCIENCE
Medscape News

Few JAK Inhibitor Users Have Reduced Response to COVID Vaccines

Editor's note: Find the latest COVID-19 news and guidance in Medscape's Coronavirus Resource Center. Patients who are being treated with Janus kinase (JAK) inhibitors overall show a high immune response rate to COVID-19 vaccination, one that matches the rates seen in patients on other immunosuppressants, a new study has found.
SCIENCE
masterdoctor.net

Aromatase inhibitors may be beneficial in endometrial stromal sarcomas

In a study of patients with endometrial stromal sarcomas treated with aromatase inhibitors the objective response rate was more modest than expected, but a majority did achieve stable disease, according to a study presented at the ASCO Annual Meeting. Because account for only 7% to 25% of uterine mesenchymal tumors,...
MedPage Today

Slowly Expanding Lesions in MS Reduced with BTK Inhibitor

Evobrutinib, a highly selective Bruton's tyrosine kinase inhibitor (BTK) targeting B cells and myeloid cells, reduced the volume of slowly expanding lesions (SELs) in people with relapsing multiple sclerosis (MS), a post hoc analysis of a phase II trial showed. Treatment with investigational evobrutinib reduced SEL volume compared with placebo,...
onclive.com

Novel Strategies With BTK Inhibitors Seek to Impact Frontline MCL Treatment Landscape

Brad S. Kahl, MD, discusses personalizing frontline treatment in mantle cell lymphoma, clinical trials further examining BTK inhibitors, and research opportunities with CAR T-cell therapy. The mantle cell lymphoma (MCL) paradigm continues to expand, and efforts are underway to evaluate novel approaches with BTK inhibitors to continue to improve outcomes...
CANCER
crarydrug.com

Get Healthy!

Patients who use proton pump inhibitors (PPIs) for heartburn have healthier gums, researchers say. Health News is provided as a service to Crary Drug site users by HealthDay. Crary Drug nor its employees, agents, or contractors, review, control, or take responsibility for the content of these articles. Please seek medical advice directly from your pharmacist or physician.
HEALTH
byardmercer.com

Heartburn Drugs May Improve Gum Disease, Study Finds

Patients who use proton pump inhibitors (PPIs) for heartburn have healthier gums, researchers say. Health News is provided as a service to Byard-Mercer Pharmacy site users by HealthDay. Byard-Mercer Pharmacy nor its employees, agents, or contractors, review, control, or take responsibility for the content of these articles. Please seek medical advice directly from your pharmacist or physician.
DISEASES & TREATMENTS
StreetInsider.com

Ventyx Biosciences (VTYX) Files IPO Registration Statement

News and research before you hear about it on CNBC and others. Claim your 1-week free trial to StreetInsider Premium here. Ventyx Biosciences (NASDAQ: VTYX) files registration statement for a proposed IPO. The company describes itself as: "We are a clinical-stage biopharmaceutical company focused on advancing new therapies for millions...
MEDICAL & BIOTECH
Medscape News

Optimal Use of SGLT2 Inhibitors and GLP-1 Agonists: 5 Things to Know

For the first time in any trial of hypoglycemic therapy, the EMPA-REG OUTCOME study demonstrated a significant reduction in major adverse cardiovascular events (MACE). This started a plethora of cardiovascular (CV) outcome studies that were positive for reduction in CV death, hospitalizations related to heart failure (HF), improvements in renal function, and prevention of adverse renal outcomes, which added to the positive benefits of these new agents. Coupled with weight reduction — a welcome "side effect" of both the sodium glucose cotransporter 2 (SGLT2) inhibitors and glucagon-like peptide 1 (GLP-1) agonists — these medications should become a cornerstone of therapy for our high-risk patients in cardiology.
HEALTH
targetedonc.com

Disease Progression and Resistance to BTK Inhibitors

Mazyar Shadman, MD, MPH: Ibrutinib, acalabrutinib, and we have zanubrutinib, another second-generation medication. Again, for all these drugs, the mechanism of action is very similar. For example, please talk about the resistance mechanism with ibrutinib, at least for CLL [chronic lymphocytic leukemia]. That’s the disease that’s studied more for treatment failure. There are mutations in CLL we have found that are responsible for most of the treatment failures. Maybe you should talk about that, and then we’ll move to the next BTK [Bruton tyrosine kinase] inhibitor, zanubrutinib.
CANCER
pharmaceutical-technology.com

EASD 2021: SGLT2 inhibitors improve efficacy in quadruple combination therapy

At the 57th annual European Association for the Study of Diabetes (EASD) meeting recently, new results were presented from a three-year prospective study. The results demonstrated that sodium glucose cotransporter 2 (SGLT2) inhibitors (SGLT2Is), either empagliflozin (Jardiance) or dapagliflozin (Farxiga), are efficacious as part of a quadruple combination therapy with metformin, dipeptidyl peptidase-4 inhibitor (DPP-4I) and glimepiride in patients with type 2 diabetes (T2D). Boehringer Ingelheim and Eli Lilly’s Jardiance is a leading SGLT2I that is prescribed for the treatment of T2D. AstraZeneca’s Farxiga is also prescribed for the treatment of T2D.
SCIENCE
gastroenterologyadvisor.com

Proton Pump Inhibitors, Antiglaucoma Meds Linked to Dry Eye

Proton pump inhibitors (PPIs), antiglaucoma and anticholinergic medications are significantly associated with dry eye symptoms, according to a study published in The Ocular Surface. This large, population-based research notes that medication use should always be evaluated in every patient with dry eyes. Previous studies on the association between dry eye...
docwirenews.com

A patent review on SARS coronavirus main protease (3CLpro) inhibitors

ChemMedChem. 2021 Oct 15. doi: 10.1002/cmdc.202100576. Online ahead of print. The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) pandemic is an unprecedented global health emergency causing more than 4.2 million fatalities as of 30 July 2021. Only three antiviral therapies have been approved or granted emergency use authorization by the FDA. The SARS-CoV-2 3CL protease (3CLpro) is deemed an attractive drug target as it plays an essential role in viral polyprotein processing and pathogenesis, although no inhibitors have been approved. This patent review discusses SARS coronavirus 3CLpro inhibitors that have been filed up to 30 July 2021, giving an overview on the types of inhibitors that have generated commercial interest, especially amongst drug companies. Insights into the common structural motifs required for active site binding is also discussed.
MEDICAL & BIOTECH
News-Medical.net

A survey on computational methods in discovering protein inhibitors of SARS-CoV-2

Since the coronavirus Disease (COVID-19) was first detected in Wuhan, China, over 238 million people have been infected with the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), of which over 4.86 million have succumbed to. The impact of this global pandemic has not only devastated the worldwide health systems but has also caused significant economic impacts.
SCIENCE
bioworld.com

Potent selective pan-serotype dengue inhibitor developed

Blocking the interaction between two dengue virus (DENV) nonstructural proteins, NS3 and NS4B, with a newly developed small-molecule inhibitor resulted in potent antiviral activity in mouse models, according to an international collaborative study led by scientists at the University of Leuven (KU Leuven), CD3 the Centre for Drug Design and Discovery in Leuven, and Janssen Pharmaceutica in Beerse, Belgium.
SCIENCE
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