Covalent Modifiers

MAY 31, 2024

Winter, Bioorganic & Medicinal Chemistry Letters , 2024 [link] Targeted protein degradation is mediated by small molecules that induce or stabilize protein–protein interactions between targets and the ubiquitin–proteasome machinery. Gary Tin, Marko Cigler, Matthias Hinterndorfer, Kevin D. Dong, Hana Imrichova, Steven P.

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Targeted Protein Degradation Small Molecule 189

Covalent Modifiers

FEBRUARY 1, 2024

Nat Commun 15 , 859 (2024). link] Proteins labelled site-specifically with small molecules are valuable assets for chemical biology and drug development. The unique reactivity profile of the 1,2-aminothiol moiety of N -terminal cysteines ( N -Cys) of proteins renders it highly attractive for regioselective protein labelling.

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Biophysical Assays Small Molecule Drug Development Production 200

Covalent Modifiers

JANUARY 29, 2024

Moore Journal of Medicinal Chemistry 2024 DOI: 10.1021/acs.jmedchem.3c01835 3c01835 Building on recent advances in peptide science, medicinal chemists have developed a hybrid class of bioconjugates, called peptide–drug conjugates, that demonstrate improved efficacy compared to peptides and small molecules independently.

Small Molecule 173

Small Molecule Drugs Science Disease 173

Covalent Modifiers

FEBRUARY 29, 2024

Gray ACS Central Science 2024 DOI: 10.1021/acscentsci.3c01245 Currently, all FDA-approved covalent small molecules feature one electrophile, leaving open a facile route to acquired resistance.

Small Molecule 217

Small Molecule FDA Approval FDA Science 217

LifeSciVC

JANUARY 16, 2024

Small molecule GLP1s? Tirzepatide is also trialing in a Phase 3 obese HFpEF trial, and top-line readout in 2H 2024 will suggest whether the increased weight loss achieved with dual GLP1/GIPR modulation further improves QoL and functional endpoints. ALT) continue to build momentum in the indication.

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Small Molecule Trials Therapies Disease 138

Covalent Modifiers

APRIL 28, 2024

Johnson, and Euna Yoo ACS Chemical Biology 2024 [link] Electrophilic small molecules with novel reactivity are powerful tools that enable activity-based protein profiling and covalent inhibitor discovery. Byun, Kalyani Thakur, Jennifer Ritchie, Yixin Xie, Ronald Holewinski, Kiall F.

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Small Molecule 189

Covalent Modifiers

JANUARY 13, 2024

Thomas Kodadek Angewandte Chemie International Edition 2024 e202316726 [link] Many of the highest priority targets in a wide range of disease states are difficult-to-drug proteins.

Small Molecule 195

Small Molecule International Disease Drugs 195

Covalent Modifiers

MAY 25, 2024

Backus Journal of the American Chemical Society 2024 DOI: 10.1021/jacs.3c12240 Complementary to genetic approaches, small-molecule probes have emerged as useful tools for modulating caspase activity. Complementary to genetic approaches, small-molecule probes have emerged as useful tools for modulating caspase activity.

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Small Molecule DNA Virus Regulations 162

Covalent Modifiers

MAY 21, 2024

Rivers ACS Medicinal Chemistry Letters 2024 DOI: 10.1021/acsmedchemlett.4c00113 A DNA-encoded chemical library (DEL) screen against Bfl-1 identified the first known reversible covalent small-molecule ligand for Bfl-1.

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DNA Small Molecule Drugs 182

Drug Hunter

MAY 31, 2023

This article compiles 20+ recent small molecules of general interest in the news in April 2023, with structures where they are available.

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Small Molecule Clinical Trials Trials Drugs 196

Covalent Modifiers

JUNE 24, 2024

Rullo, Molecular Therapy: Oncology , 2024 , 200842, [link] Proximity-induction of cell-cell interactions via small molecules represents an emerging field in basic and translational sciences. Hammill, Jonathan L. Bramson, Anthony F.

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Small Molecule Engineering Science Therapies 130

Covalent Modifiers

JANUARY 17, 2024

Maciag Journal of Biological Chemistry , 2024 [link] Individual oncogenic KRAS mutants confer distinct differences in biochemical properties and signaling for reasons that are not well understood. Sharma,Jun Pei,Yue Yang,Marcin Dyba,Brian Smith,Dana Rabara,Erik Larsen,Felice C. Lightstone,Dominic Esposito,Andrew G. Stephen,Bin Wang,Pedro J.

Small Molecule 195

Small Molecule Regulations Drugs 195

Covalent Modifiers

OCTOBER 24, 2024

Backus Nat Chem Biol 2024 [link] Covalent modulators and covalent degrader molecules have emerged as drug modalities with tremendous therapeutic potential. Julio, Flowreen Shikwana, Cindy Truong, Nikolas R. Burton, Emil R. Dominguez III, Alexandra C. Turmon, Jian Cao & Keriann M.

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Small Molecule Drugs 147

KIF1A

JANUARY 27, 2024

Drugs that treat symptoms in other HSP types could inform treatments for similar symptoms in KAND, so we’re always on the lookout for small molecule or technological interventions that work in other SPGs. Read the Article The post #ScienceSaturday: January 27, 2024 appeared first on KIF1A.

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Therapies Small Molecule DNA Treatment 111

Covalent Modifiers

SEPTEMBER 26, 2024

Changliu Wang, Zhenguang Zhao, Reem Ghadir, Dechun Yang, Zhenjia Zhang, Zhe Ding, Yuan Cao, Yuqing Li, Rosi Fassler, Dana Reichmann, Yujie Zhang, Yongli Zhao, Can Liu, Xiaobao Bi, Norman Metanis, and Junfeng Zhao ACS Central Science 2024 10 (9), 1742-1754 DOI: 10.1021/acscentsci.4c01148

Small Molecule 147

Small Molecule Science Drugs 147

Covalent Modifiers

OCTOBER 25, 2024

We demonstrated the employability of ring-opening chemistry in isatoic anhydride as a drug delivery modality for the release of a small molecule and doxorubicin in cancer cells. Broadly, the tunable reactivity of isatoic anhydride could be leveraged for developing lysine-selective probes and drug delivery cargos.

Small Molecule 133

Small Molecule Drugs Science 133

PPD

NOVEMBER 11, 2024

According to the United Nation’s 2024 World Population Prospects data, the global population of those 65 years old and over will grow from 0.8 From an aging population increasing health care demand to urgent, unmet medical needs, there are clear drivers to advance safe and effective medicines to patients faster than ever. billion in 2035.

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Drug Development Clinical Trials Drugs Small Molecule 97

Broad Institute

MARCH 14, 2024

By Leah Eisenstadt March 14, 2024 Credit: Courtesy of the authors. In one approach, they mark targeted proteins with “destroy me” tags that work with small molecules known as molecular glues to prompt the cell’s own protein-clearing machinery to gobble up the proteins. March 14, 2024. Paper cited Mercer JAM, et al.

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Targeted Protein Degradation Small Molecule Medical Schools Science 141

SCIENMAG: Medicine & Health

MARCH 26, 2024

Credit: Redox Medicine […]

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Small Molecule International Drug Development Drugs 78

Alta Sciences

DECEMBER 29, 2023

PBSS—ADME/DMPK Studies for IND and NDA Filing for Small Molecules: Nuts, Bolts and Best Practices lperez Fri, 12/29/2023 - 16:20 Image GettyImages-1075448458.jpg jpg Synopsis Foster City, CA URL [link] Event End Date Fri, 01/19/2024 - 12:00 Event Start Date Fri, 01/19/2024 - 12:00 Weight 1

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Small Molecule 40

Drug Target Review

SEPTEMBER 25, 2024

Applying our technology has enabled us to develop a new small molecule, TT125-802, and to assign a new role to the epigenetic regulator CBP/p300 as a novel master regulator of non-oncogene resistance. This orally available small molecule binds to the bromodomain of CBP/p300 in a highly specific manner. Bell CC, Gilan O.

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Small Molecule Therapies Regulations Treatment 105

FDA Law Blog: Biosimilars

AUGUST 27, 2024

The American Conference Institute (“ACI”) will hold (virtually) its 4th Annual Passport to Proficiency on the Essentials of Hatch-Waxman and BPCIA from October 8-24, 2024. This program lays the groundwork for understanding the patent life cycles of biopharmaceutical products and business development plans.

Small Molecule 59

Small Molecule FDA Regulations Science 59

Broad Institute

SEPTEMBER 23, 2024

New approach may yield modified messenger RNAs for treating a wide range of conditions By Ari Navetta September 23, 2024 Breadcrumb Home New approach may yield modified messenger RNAs for treating a wide range of conditions The LEGO framework could help scientists create mRNA therapies that last longer and require smaller doses.

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RNA Vaccine Small Molecule Therapies 134

New Drug Approvals

SEPTEMBER 12, 2024

ZASTAPRAZAN 2133852-18-1 362.5 ZASTAPRAZAN 2133852-18-1 362.5 Zastaprazan can be used for the research of gastrointestinal inflammatory diseases or gastric acid-related diseases.

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Small Molecule Trials Disease Research 62

Fierce BioTech

MARCH 11, 2024

Safety Considerations for the Development of ADCs dwunderlin Mon, 03/11/2024 - 16:44 Tue, 04/30/2024 - 11:00 Resource Type Webinar Maciej Czerwinski, PhD Duration 60 Minutes Antibody-drug conjugates (ADCs) are a novel modality leveraging monoclonal antibody (mAb)-mediated delivery of a cytotoxic payload molecule to its target.

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Small Molecule FDA Approval FDA Treatment 52

The ChEMBL-og

JUNE 18, 2024

Our flagship resource, ChEMBL , is a database of high-quality quantitative small-molecule bioactivity data curated from the scientific literature and direct data depositions. ChEBI is a database of small molecules relevant to biology. ChEBI is a database of small molecules relevant to biology.

Small Molecule 48

Small Molecule Drugs 48

Drug Target Review

OCTOBER 23, 2024

Technologies for the rapid and efficient testing of small molecules and biologics have greatly accelerated drug discovery. Intermediate-sized molecules such as macrocycles combining the beneficial properties of both small molecules and biologics may enable the targeting of currently undruggable targets.

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Small Molecule DNA Drugs Pharmaceuticals 64

Alta Sciences

APRIL 17, 2024

Five Promising Treatment Areas in Early-Phase Drug Development in 2024 aasimakopoulos Wed, 04/17/2024 - 15:52 Early-phase drug development is an ever-changing landscape, as emerging science leads to new promising areas of research for the treatment of human health issues.

Drug Development 52

Drug Development Treatment FDA Approval Drugs 52

Broad Institute

SEPTEMBER 26, 2024

Recently published literature has identified three proteins (Lap2β, H3K9me3, and HP1γ) that exhibit decreased expression in aged fibroblasts and a “senescence cocktail” of small molecules that have been observed to reduce the expression of these chromatin proteins in a way that models aged cells.

Small Molecule 52

Small Molecule Protein Expression Disease Science 52

FDA Law Blog: Biosimilars

JULY 24, 2024

The American Conference Institute (“ACI”) is holding its 10th Anniversary Paragraph IV Disputes Master Symposium from October 15-16, 2024, at the Hyatt Regency McCormick Place in Chicago, Illinois.

Small Molecule 52

Small Molecule Clinical Trials FDA Pharmaceuticals 52

Molecular Design

DECEMBER 31, 2024

My pulse will be quickenin' With each drop of strychnine We feed to a pigeon It just takes a smidgin To poison a pigeon in the park Tom Lehrer, Poisoning Pigeons in the Park | video ** Ill be reviewing the H2024 study (Occurrence of Natural Selection in Successful Small Molecule Drug Discovery) in this post.

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Small Molecule Drugs Production Science 85

LifeSciVC

AUGUST 5, 2024

But that initial quote isn’t from 2024, it is from an interview in 2021 with Mark Levin, CEO at Millennium (MIT Technology Review). Now fast forward to 2024, and the drug discovery community is fully invested in determining how best to apply the capabilities of AI throughout its work. One final parallel to 2001.

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Molecular Biology Production Drug Development Small Molecule 88

FDA Law Blog: Biosimilars

MARCH 3, 2024

3558 ) on January 25, 2024. Gonzalez & JP Ellison — The most recent version of the BIOSECURE Act (the “Act”) was introduced in the U.S. House of Representatives ( H.B. 7085 ) and Senate ( S.B. This proposed legislation should be of interest to any biotechnology companies that want to do business with the federal government in the future.

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Small Molecule Government FDA Approval Regulations 102

Elrig

APRIL 30, 2024

One aim of this work was to develop a set of tools to be later used in a high-throughput screen to identify small molecules for potential therapeutic uses as the current large molecule therapeutics do not show good selectivity.

Small Molecule 52

Small Molecule Doctors Pharmacy Disease 52

Alta Sciences

SEPTEMBER 27, 2024

The growing understanding of the immune system's role in various diseases, along with advancements in drug development, have led to a natural evolution from traditional vaccines, small molecules , and cytokines , to increased targeted biologics and innovative approaches in gene therapy and vaccines.

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Clinical Trials Trials Pharmacokinetics Small Molecule 52

Metabolite Tales Blog

FEBRUARY 16, 2024

The paper, written by a consortium of scientists from several big pharma companies, points out that discussions around multi labelling are happening with more frequency due to the increase in larger molecular weight small molecules being developed. January 12, 2024. Eur J Drug Metab Pharmacokinet 48 , 411–425 (2023).

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Small Molecule Pharma Companies Pharmacokinetics Drugs 52

Alta Sciences

NOVEMBER 5, 2024

This blog was originally posted 07/26/2021 and updated on 11/05/2024 Reference [link] Image Thumbnail_Blog-LFHSCs-alt.jpg Synopsis Liquid-filled capsules can be rapidly developed and tested, moving quickly from R&D to clinic. Last but not least, they offer patient benefits with increased bioavailability and sustained release drug delivery.

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Marketing Small Molecule Production Pharmaceuticals 52