April, 2023

article thumbnail

Gene Accessibility May Explain Why Alzheimer’s Gene, APOE4, is Less Dangerous for People of African Descent

Drug Discovery Today

(MIAMI) Researchers at the John P. Hussman Institute for Human Genomics at the University of Miami Miller School of Medicine have found that variations in chromatin accessibility, and thus gene expression, may explain why people of European descent with APOE4 gene variants have a greater risk of developing Alzheimer’s disease than people of African descent with similar genetics.

Disease 201
article thumbnail

Hydrazonyl Sultones as Stable Tautomers of Highly Reactive Nitrile Imines for Fast Bioorthogonal Ligation Reaction

Covalent Modifiers

Ming Fang, Gangam Srikanth Kumar, Stefano Racioppi, Heyang Zhang, Johnathan D. Rabb, Eva Zurek, and Qing Lin Journal of the American Chemical Society 2023 DOI: 10.1021/jacs.2c12325 Here we report the design and synthesis of a new class of bioorthogonal reagents called hydrazonyl sultones (HS) that serve as stable tautomers of highly reactive nitrile imines (NI).

130
130
Insiders

Sign Up for our Newsletter

This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.

article thumbnail

cdd-vault-update-april-2023-2

Collaborative Drug

Ketcher: Drawing all types of S-Groups Consolidated into 1 Tool Drawing all types of S-Groups (data, superatoms, polymers, etc) in Ketcher has been consolidated into a single tool located on the left side of the structure editor. CDD Vault: Batch Links in Protocol & Run Fields When creating Protocol and Run fields, the Vault Administrator may now designate Batch Link data types.

130
130
article thumbnail

Drug Hunter Journal Club: March 2023

Drug Hunter

There were plenty of scientific highlights from the literature that we didn’t have space for in Molecules of the Month – here’s a reader’s digest rounding up ~20 molecules of potential interest that we didn’t have space to highlight, including Pfizer’s covalent heterobifunctional BTK degrader, BMS’ brain-penetrant GSK-3β inhibitor, the discovery story of futibatinib from Taiho, and more snippets to jumpstart your reading!

article thumbnail

Bridging Innovation & Patient Care: The Growing Role of AI

Speaker: Simran Kaur, Co-founder & CEO at Tattva.Health

AI is transforming clinical trials—accelerating drug discovery, optimizing patient recruitment, and improving data analysis. But its impact goes far beyond research. As AI-driven innovation reshapes the clinical trial process, it’s also influencing broader healthcare trends, from personalized medicine to patient outcomes. Join this new webinar featuring Simran Kaur for an insightful discussion on what all of this means for the future of healthcare!

article thumbnail

Getting Ozempic And Other Drugs From Canada? Not Likely.

Forbes: Drug Truths

Clearly, Canada would find such a situation untenable and the steps now being taken by British Columbia for Ozempic would be adopted across Canada.

Drugs 130

More Trending

article thumbnail

Strata Oncology Announces Launch and Medicare Coverage for Strata Select, a First-of-its-kind Immunotherapy Test

Drug Discovery Today

New diagnostic test stratifies the likelihood of immunotherapy benefit across solid tumors

113
113
article thumbnail

CysDB: a human cysteine database based on experimental quantitative chemoproteomic [@Keribackus]

Covalent Modifiers

Lisa M. Boatner , Maria F. Palafox, Devin K. Schwepp, Keriann M. Backus Cell Chem. Bio. 2023 [link] Cysteine chemoproteomics provides proteome-wide portraits of the ligandability or potential “druggability” for thousands of cysteine residues. Consequently, these studies are facilitating resources for closing the druggability gap, namely, achieving pharmacological manipulation of ∼96% of the human proteome that remains untargeted by U.S.

article thumbnail

The effects of MYC on exosomes derived from cancer cells in the context of breast cancer

Chemical Biology and Drug Design

MYC regulates main genes of exosome biogenesis in breast cancer. Furthermore, MYC regulates oncogenic roles of breast cancer cells-derived exosomes in breast cancer and MYC-expressing cancer cells-secreted exosomes induce higher cellular activity of recipient cells in breast cancer. Abstract MYC amplification and overexpression in breast cancer occur 16% and 22%, respectively, and MYC has a linchpin role in breast carcinogenesis.

article thumbnail

Small Molecule of the Year – 2022

Drug Hunter

We asked the global drug discovery community to nominate and vote on their favorite molecule from 2022, and the results are in. The 2022 winner, with the most overall votes across the ten finalist molecules , is BMS’ oral, deuterated allosteric TYK2 inhibitor, deucravacitinib, the first new treatment for plaque psoriasis in nearly a decade. Here, we highlight what makes deucravacitinib so impressive to the drug discovery community.

article thumbnail

From Diagnosis to Delivery: How AI is Revolutionizing the Patient Experience

Speaker: Simran Kaur, Founder & CEO at Tattva Health Inc.

The healthcare landscape is being revolutionized by AI and cutting-edge digital technologies, reshaping how patients receive care and interact with providers. In this webinar led by Simran Kaur, we will explore how AI-driven solutions are enhancing patient communication, improving care quality, and empowering preventive and predictive medicine. You'll also learn how AI is streamlining healthcare processes, helping providers offer more efficient, personalized care and enabling faster, data-driven

article thumbnail

Mechanistically weighted metric to predict in vivo antibody-receptor occupancy: An analytical approach [Drug Discovery and Translational Medicine]

ASPET

In situ clinical measurement of receptor occupancy (RO) is challenging, particularly for solid tumors, necessitating the use of mathematical models that predict tumor receptor occupancy to guide dose decisions. A potency metric, average free tissue target to initial target ratio (AFTIR), was previously described based on a mechanistic compartmental model, and is informative for near-saturating dose regimens.

Drugs 100
article thumbnail

Pharmacovigilance Services for Signal Management: Process as per US FDA

ProRelix Research

Pharmacovigilance is defined by the World Health Organization (WHO) as “the science and activities relating to the detection, assessment, understanding, and prevention of adverse events or any other drug-related problems.” […] The post Pharmacovigilance Services for Signal Management: Process as per US FDA appeared first on ProRelix Research.

FDA 98
article thumbnail

Domainex secures a prestigious King's Award for Enterprise

Drug Discovery Today

Domainex is honoured to announce it has received a King’s Award for Enterprise: International Trade 2023.

article thumbnail

Rational Design of Highly Potent and Selective Covalent MAP2K7 Inhibitors

Covalent Modifiers

Dalton R. Kim, Meghan J. Orr, Ada J. Kwong, Kristine K. Deibler, Hasan H. Munshi, Cory Seth Bridges, Taylor Jie Chen, Xiaoyu Zhang, H. Daniel Lacorazza, and Karl A. Scheidt ACS Medicinal Chemistry Letters 2023 DOI: 10.1021/acsmedchemlett.3c00029 The mitogen-activated protein kinase signaling cascade is conserved across eukaryotes, where it plays a critical role in the regulation of activities including proliferation, differentiation, and stress responses.

article thumbnail

How Machine Learning Drives Clinical Trial Efficiency

Clinical trial data management is increasingly challenging as studies grow in complexity. Quickly accessing and analyzing study data is vital for assessing trial progress and patient safety. In this paper, we explore real-time data access and analysis for proactive study management. We investigate using adverse event (AE) data to monitor safety and discuss a clinical analytics platform that supports collaboration and data review workflows.

article thumbnail

Geraniol protects hippocampal CA1 neurons and improves functional outcomes in global model of stroke in rats

Chemical Biology and Drug Design

Geraniol (GE) by its antioxidant, anti-inflammatory, and anti-apoptotic properties ameliorated global ischemia-reperfusion induced cascade of events such as oxidative stress, apoptosis, and inflammation. Thus, improved functional outcomes, and prevented neuronal infarction in rats. Abstract Geraniol (GE), an acyclic monoterpene, is a chief constituent of essential oils of herbs and fruits.

Treatment 100
article thumbnail

20 Blog post ideas for your health blog

Antidote

For individuals and companies that write health-focused blogs, continually finding topics to cover can be a challenge at times. Whether you’re a health influencer, patient advocacy organization, or another player in the clinical trial industry, finding unique topics to differentiate a blog is not always easy. However, through the below ideas and a unique voice, it is possible to write a plethora of clinical trial blogs that stick out from the rest.

article thumbnail

DCI’s Top 15 Specialty Pharmacies of 2022: Five Key Trends About Today’s Marketplace

Drug Channels

In Drug Channels Institute’s list of the top 15 pharmacies of 2022 , we show that central-fill, mail pharmacies operated by large PBMs and health insurers have displaced retail chains as the largest prescription drug dispensers by revenues. To complement that broader ranking, we rummaged around our DreamHouse to update our exclusive list of the top 15 pharmacies based on specialty drug dispensing revenues in 2022.

article thumbnail

Which pharmaceutical companies have the most SPCs in Netherlands?

Drug Patent Watch

This chart shows the pharmaceutical companies with the most supplementary protection certificates (SPCs) in Netherlands. SPCs are used in European Union and select others to encourage pharmaceutical innovation by compensating… The post Which pharmaceutical companies have the most SPCs in Netherlands? appeared first on DrugPatentWatch - Make Better Decisions.

article thumbnail

Deliver Fast, Flexible Clinical Trial Insights with Spotfire

Clinical research has entered a new era, one that requires real-time analytics and visualization to allow trial leaders to work collaboratively and to develop, at the click of a mouse, deep insights that enable proactive study management. Learn how Revvity Signals helps drug developers deliver clinical trial data insights in real-time using a fast and flexible data and analytics platform to empower data-driven decision-making.

article thumbnail

Sygnature Discovery and Daewoong Pharma announce drug discovery research collaboration

Drug Discovery Today

Global integrated drug discovery company, Sygnature Discovery and global healthcare group Daewoong Pharmaceutical, have entered into a research collaboration agreement to accelerate the discovery of a novel small molecule to target autoimmune disease.

article thumbnail

Discovery of Futibatinib: The First Covalent FGFR Kinase Inhibitor in Clinical Use

Covalent Modifiers

Satoru Ito, Sachie Otsuki, Hirokazu Ohsawa, Atsushi Hirano, Hideki Kazuno, Satoshi Yamashita, Kosuke Egami, Yoshihiro Shibata, Ikuo Yamamiya, Fumiaki Yamashita, Yasuo Kodama, Kaoru Funabashi, Hiromi Kazuno, Toshiharu Komori, Satoshi Suzuki, Hiroshi Sootome, Hiroshi Hirai, and Takeshi Sagara ACS Medicinal Chemistry Letters 2023 14 (4), 396-404 DOI: 10.1021/acsmedchemlett.3c00006 Deregulating fibroblast growth factor receptor (FGFR) signaling is a promising strategy for cancer therapy.

Therapies 130
article thumbnail

Leishmania species: A narrative review on surface proteins with structural aspects involved in host–pathogen interaction

Chemical Biology and Drug Design

The key virulence factors like Kinetoplastid Membrane Protein–11 (KMP-11), Leishmanolysin (GP63), Proteophosphoglycan (PPG), Lipophosphoglycan (LPG), Glycosylinositol Phospholipids (GIPL), and others that play a role in the pathogenicity-host-pathogen relationship of the parasite. Abstract In tropical and subtropical regions of the world, leishmaniasis is endemic and causes a range of clinical symptoms in people, from severe tegumentary forms (such as cutaneous, mucocutaneous, and diffuse leishm

article thumbnail

What to know about homocystinuria

Antidote

Homocystinuria, an inherited disorder, is a rare metabolic condition that impacts 1 in 335,000 people worldwide and is present from birth. Often abbreviated as HCU or HCY, homocystinuria is a genetic disorder that inhibits the body from processing certain amino acids found in proteins, causing a harmful buildup of homocysteine and methionine.

98
article thumbnail

Clinical Data Like You´ve Never Seen It Before: Why Spotfire Is the Leading Tool for Clinical Analytics

Clinical development organizations face a wide array of challenges when it comes to data, many of which can impact the operational effectiveness of their clinical trials. In this whitepaper, experts from Revvity Signals explore how solutions like TIBCO® Spotfire® enable better, more streamlined studies. The whitepaper also features a success story from Ambrx, a leading biopharmaceutical company, detailing how it has leveraged Spotfire to tackle data quality and collaboration challenges in clinic

article thumbnail

Revolutionary nanoparticles enable gene-editing in lungs

Drug Target Review

Scientists from the Massachusetts Institute of Technology (MIT) and the University of Massachusetts Medical School (UMass), US, have collaborated to create a novel type of nanoparticle that can deliver messenger RNA that encodes for beneficial proteins to the lungs. Gene-editing methods allow researchers to modify DNA, resulting in alterations in physical characteristics such as eye colour and susceptibility to diseases.

RNA 98
article thumbnail

New patent expiration for Wyeth Pharms drug ZOSYN IN PLASTIC CONTAINER

Drug Patent Watch

Annual Drug Patent Expirations for ZOSYN+IN+PLASTIC+CONTAINER Zosyn In Plastic Container is a drug marketed by Wyeth Pharms and is included in one NDA. It is available from two suppliers. There… The post New patent expiration for Wyeth Pharms drug ZOSYN IN PLASTIC CONTAINER appeared first on DrugPatentWatch - Make Better Decisions.

Drugs 98
article thumbnail

Championing sustainability and innovation at Lab Innovations 2023

Drug Discovery Today

The home of the UK’s lab industry expands floor plan to accommodate increased interest in this year’s show

113
113
article thumbnail

Discovery of a spirocyclic 3-bromo-4,5-dihydroisoxazole covalent inhibitor of hGAPDH with antiproliferative activity against pancreatic cancer cells,

Covalent Modifiers

Andrea Galbiati, Stefania Bova, Raffaella Pacchiana, Chiara Borsari, Marco Persico, Aureliano Zana, Stefano Bruno, Massimo Donadelli, Caterina Fattorusso, Paola Conti, European Journal of Medicinal Chemistry, 2023 [link] Glyceraldehyde-3-phosphate dehydrogenase (GAPDH), a key glycolytic enzyme, plays a crucial role in the energy metabolism of cancer cells and has been proposed as a valuable target for the development of anticancer agents.

Drugs 100
article thumbnail

Explainability and white box in drug discovery

Chemical Biology and Drug Design

Explainable artificial intelligence transparently influences the pre-drug development process with SHAP and LIME annotation methods. Abstract Recently, artificial intelligence (AI) techniques have been increasingly used to overcome the challenges in drug discovery. Although traditional AI techniques generally have high accuracy rates, there may be difficulties in explaining the decision process and patterns.

Drugs 100