Search research articles

ABOUT JoVE

Overview Leadership Blog JoVE Help Center

AUTHORS

Publishing Process Editorial Board Scope & Policies Peer Review FAQ Submit

LIBRARIANS

Testimonials Subscriptions Access Resources Library Advisory Board FAQ

RESEARCH

JoVE Journal Methods Collections JoVE Encyclopedia of Experiments Archive

EDUCATION

JoVE Core JoVE Business JoVE Science Education JoVE Lab Manual Faculty Resource Center Faculty Site

Terms & Conditions of Use

Related Concept Videos

Inhibition of Cdk Activity

Inhibition of Cdk Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...

Drugs that Destabilize Microtubules

Drugs that Destabilize Microtubules

Microtubules are dynamic structures and can be regulated by microtubule targeting agents (MTAs). Microtubule destabilizing drugs are a class of MTAs that destabilize and prevent microtubules' polymerization. Both natural and synthetic chemicals can be found under this class of drugs. Vincristine and vinblastine, two vinca alkaloids, and colchicine were among the first to be discovered. These drugs can affect cells in various ways, either by inducing a change in cell morphology, preventing...

Drugs that Stabilize Microtubules

Drugs that Stabilize Microtubules

Microtubules are dynamic structures that undergo cycles of catastrophe and rescue. The microtubules play a central role in cell division by forming the spindle apparatus for segregating the chromosomes. This makes them ideal targets for regulating dividing cells in tumors and malignant cancer cells. Microtubule stabilizing drugs help stabilize the microtubule formation and promote its polymerization. Paclitaxel was the first microtubule stabilizing agent used as anticancer drug in chemotherapy...

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by

Same author

Establishment of the Genetic Transformation System of <i>Trichoderma longibrachiatum</i> 40418 and Its Induced Resistance Against <i>Meloidogyne incognita</i> in Tomato.

Journal of fungi (Basel, Switzerland)·2026

Same author

Solubility-Driven Lead Optimization of PAR4 Antagonists and Evaluation of a Phosphate Ester Prodrug Delivery Strategy.

ACS medicinal chemistry letters·2026

Same author

Optimization of Covalent Warhead Trajectory for KRAS<sup>G12C</sup> Active-State Inhibition.

Journal of medicinal chemistry·2026

Same author

Analysis of the TGA gene family and the role of SlTGA03 in tomato resistance to Meloidogyne enterolobii.

BMC genomics·2026

Same author

From Lead to Clinical Candidate: Discovery of BMS-986331 as a Potent and Selective <i>N</i>-Formyl Peptide Receptor 2 Agonist.

Journal of medicinal chemistry·2026

Same author

Covalent inhibitor design confers activity against both GDP- and GTP-bound forms of KRAS G12C.

Nature communications·2026

Same journal

Solid-phase synthesis and antimicrobial activities of lipid-neomycin conjugates.

Bioorganic & medicinal chemistry letters·2026

Same journal

Discovery of a potent sGC stimulator with once-daily dosing potential for the treatment of hypertension.

Bioorganic & medicinal chemistry letters·2026

Same journal

OracleScreen-LILRB4 (HTS-Oracle v3): machine learning-guided discovery of myeloid immune checkpoint binders validated in patient-derived cells.

Bioorganic & medicinal chemistry letters·2026

Same journal

Rational design and N-terminal acylation of a lactam-cyclized 11-residue antimicrobial peptide for improved antibacterial potency.

Bioorganic & medicinal chemistry letters·2026

Same journal

Rational design, synthesis, and biological evaluation of chalcone hybrids including benzoylpiperazin (phenylacetylpiperazin)-thiophene as anti- Alzheimer's agents.

Bioorganic & medicinal chemistry letters·2026

Same journal

New aminopiperidine-azoles as antifungal agents against Candida albicans with mechanistic insights into the cAMP-PKA pathway.

Bioorganic & medicinal chemistry letters·2026

See all related articles

Search research articles

Related Experiment Video

Updated: Feb 25, 2026

Multidimensional Coculture System to Model Lung Squamous Carcinoma Progression

Multidimensional Coculture System to Model Lung Squamous Carcinoma Progression

Published on: March 17, 2020

Macrocyclic factor XIa inhibitors.

Cailan Wang¹, James R Corte¹, Karen A Rossi¹

¹Bristol-Myers Squibb Company, Research and Development, 350 Carter Road, Hopewell, NJ 08540 United States.

Bioorganic & Medicinal Chemistry Letters

|August 7, 2017

Summary

This summary is machine-generated.

Researchers developed potent macrocyclic factor XIa (FXIa) inhibitors. These compounds show high selectivity and efficacy in clotting assays, offering potential therapeutic benefits.

Keywords:

Activated partial thromboplastin time FXIa Factor XIa inhibitors Thrombosis aPTT

More Related Videos

Automated Imaging and Analysis for the Quantification of Fluorescently Labeled Macropinosomes

Automated Imaging and Analysis for the Quantification of Fluorescently Labeled Macropinosomes

Published on: August 24, 2021

Author Spotlight: Integrating Traditional Chinese Medicine with Modern Pharmacology and Genomics for Assessing Postmenopausal Osteoporosis in Mice

Author Spotlight: Integrating Traditional Chinese Medicine with Modern Pharmacology and Genomics for Assessing Postmenopausal Osteoporosis in Mice

Published on: August 23, 2024

Related Experiment Videos

Last Updated: Feb 25, 2026

Multidimensional Coculture System to Model Lung Squamous Carcinoma Progression

Multidimensional Coculture System to Model Lung Squamous Carcinoma Progression

Published on: March 17, 2020

Automated Imaging and Analysis for the Quantification of Fluorescently Labeled Macropinosomes

Automated Imaging and Analysis for the Quantification of Fluorescently Labeled Macropinosomes

Published on: August 24, 2021

Author Spotlight: Integrating Traditional Chinese Medicine with Modern Pharmacology and Genomics for Assessing Postmenopausal Osteoporosis in Mice

Author Spotlight: Integrating Traditional Chinese Medicine with Modern Pharmacology and Genomics for Assessing Postmenopausal Osteoporosis in Mice

Published on: August 23, 2024

Area of Science:

Medicinal Chemistry
Biochemistry
Pharmacology

Background:

Factor XIa (FXIa) is a key enzyme in the intrinsic pathway of blood coagulation.
Inhibitors of FXIa are being investigated as novel anticoagulants.
Previous research involved acyclic phenylimidazole compounds.

Purpose of the Study:

To design and optimize novel macrocyclic FXIa inhibitors.
To achieve high affinity and selectivity for FXIa.
To evaluate the in vitro anticoagulant activity of the designed inhibitors.

Main Methods:

Structure-based drug design utilizing crystal structure analysis.
Synthesis and chemical optimization of macrocyclic compounds.
Biochemical assays to determine enzyme inhibition and selectivity.
Coagulation assays (aPTT) to assess functional potency.

Main Results:

Successfully designed macrocyclic FXIa inhibitors with picomolar (pM) affinity.
Achieved excellent selectivity against a panel of serine proteases.
Demonstrated good anticoagulant potency in the activated partial thromboplastin time (aPTT) assay.

Conclusions:

Macrocyclic FXIa inhibitors can be effectively designed using structure-based approaches.
The developed inhibitors possess desirable pharmacological properties for potential therapeutic use.
Further development of these FXIa inhibitors is warranted for anticoagulant therapy.