Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

Receptor Tyrosine Kinases01:26

Receptor Tyrosine Kinases

20.5K
Receptor tyrosine kinases or RTKs are membrane-bound receptors that phosphorylate specific tyrosine on protein substrates. RTKs regulate cellular growth, differentiation, survival, and migration. They contain an extracellular ligand binding domain, a transmembrane domain, and a cytosolic tail with intrinsic kinase activity. Several extracellular signaling molecules activate RTKs in one or more ways and relay the signal downstream. Ligands such as platelet-derived growth factor (PDGF) or...
20.5K
Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers01:26

Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers

631
Receptor tyrosine kinase inhibitors (TKIs) and calcium channel blockers (CCBs) are two critical categories of drugs employed in the treatment of pulmonary artery hypertension (PAH). PAH is a disease that causes high blood pressure in the pulmonary arteries, resulting in chest pain, fatigue, and shortness of breath.
TKIs, such as imatinib (Gleevec), are particularly effective in tackling the growth and mitogenic factors that become upregulated in PAH patients. These factors contribute to the...
631
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

9.1K
The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
9.1K
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

4.8K
Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
4.8K
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase01:11

Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase

65
Genetic polymorphisms in drug targets have emerged as critical determinants of interindividual variability in drug response and toxicity. Pharmacogenomic investigations increasingly focus on identifying these variations to personalize and optimize therapeutic interventions. A drug target may be a receptor, enzyme, or signaling protein involved in pharmacologic responses or disease-related pathways. While early pharmacogenetic studies focused primarily on drug metabolism, current research...
65
Enzyme-linked Receptors01:00

Enzyme-linked Receptors

88.7K
Enzyme-linked receptors are proteins that act as both receptor and enzyme, activating multiple intracellular signals. This is a large group of receptors that include the receptor tyrosine kinase (RTK) family. Many growth factors and hormones bind to and activate the RTKs.
Neurotrophin (NT) receptors are a family of RTKs, including trkA, trkB, and trkC (tropomyosin-related kinase) receptors. TrkA is specific for nerve growth factor (NGF), neurotrophin-6, and neurotrophin-7. TrkB binds...
88.7K

You might also read

Related Articles

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

Sort by
Same author

Choice of Frontline Tyrosine-Kinase Inhibitor and Early Events in Very Elderly Patients With Chronic Myeloid Leukemia in Chronic Phase: A "Campus CML" Study.

European journal of haematology·2024
Same author

Treatment discontinuation following low-dose TKIs in 248 chronic myeloid leukemia patients: Updated results from a campus CML real-life study.

Frontiers in pharmacology·2023
Same author

European LeukemiaNet 2020 recommendations for treating chronic myeloid leukemia.

Leukemia·2020
Same author

A phase II, multicentre trial of decitabine in higher-risk chronic myelomonocytic leukemia.

Leukemia·2017
Same author

Altered Erythropoiesis in Mouse Models of Type 3 Hemochromatosis.

BioMed research international·2017
Same author

Treatment-free remission following frontline nilotinib in patients with chronic myeloid leukemia in chronic phase: results from the ENESTfreedom study.

Leukemia·2017
Same journal

Deconvoluting MLL1-dependent pathways in hematopoiesis and leukemogenesis.

Leukemia supplements·2016
Same journal

New Abelson interactor-1 (Abi-1)-driven mechanism of acquired drug resistance.

Leukemia supplements·2016
Same journal

STAT3 as a mediator of BCR-ABL1-independent resistance in chronic myeloid leukemia.

Leukemia supplements·2016
Same journal

Dissecting reprogramming, differentiation and conversion with network biology.

Leukemia supplements·2016
Same journal

Insights into the pathophysiology and therapy of myeloproliferative neoplasms from mouse models.

Leukemia supplements·2016
Same journal

Myeloid differentiation and the leukemia-initiating cell.

Leukemia supplements·2016
See all related articles

Related Experiment Video

Updated: Mar 21, 2026

Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays
07:42

Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays

Published on: September 19, 2018

8.4K

Second-generation TKIs: which and when?

G Saglio1

  • 1Department of Clinical and Biological Sciences, Division of Hematology and Internal Medicine, University of Turin, 'San Luigi Gonzaga' University Hospital , Turin, Italy.

Leukemia Supplements
|May 14, 2016
PubMed
Summary
This summary is machine-generated.

Imatinib is a standard therapy for chronic myeloid leukemia (CML), but some patients require alternative treatments. Second-generation tyrosine kinase inhibitors (TKIs) like dasatinib and nilotinib offer effective options for CML patients resistant to imatinib.

Keywords:
BCR-ABLCMLPh-chromosomeTKIs

More Related Videos

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia
10:49

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia

Published on: September 18, 2013

18.7K
Establishment and Characterization of Three Afatinib-resistant Lung Adenocarcinoma PC-9 Cell Lines Developed with Increasing Doses of Afatinib
09:38

Establishment and Characterization of Three Afatinib-resistant Lung Adenocarcinoma PC-9 Cell Lines Developed with Increasing Doses of Afatinib

Published on: June 26, 2019

8.5K

Related Experiment Videos

Last Updated: Mar 21, 2026

Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays
07:42

Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays

Published on: September 19, 2018

8.4K
Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia
10:49

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia

Published on: September 18, 2013

18.7K
Establishment and Characterization of Three Afatinib-resistant Lung Adenocarcinoma PC-9 Cell Lines Developed with Increasing Doses of Afatinib
09:38

Establishment and Characterization of Three Afatinib-resistant Lung Adenocarcinoma PC-9 Cell Lines Developed with Increasing Doses of Afatinib

Published on: June 26, 2019

8.5K

Area of Science:

  • Hematology
  • Oncology
  • Pharmacology

Background:

  • Imatinib is the standard frontline therapy for chronic myeloid leukemia (CML).
  • Approximately one-third of CML patients exhibit suboptimal responses or resistance to imatinib.
  • Established guidelines exist for monitoring CML and managing imatinib treatment failures.

Purpose of the Study:

  • To review the current landscape of CML treatment beyond frontline imatinib.
  • To discuss the role of second-generation tyrosine kinase inhibitors (TKIs) in managing imatinib resistance.
  • To highlight emerging TKIs for imatinib-resistant CML.

Main Methods:

  • Review of published clinical trial data and treatment guidelines.
  • Analysis of efficacy and safety profiles of various TKIs.
  • Consideration of expert recommendations for CML management.

Main Results:

  • Second-generation TKIs, dasatinib and nilotinib, demonstrate clear efficacy as second-line therapies for imatinib-resistant/intolerant CML.
  • Four-year efficacy updates for dasatinib and nilotinib are now available.
  • Bosutinib and ponatinib are other TKIs under investigation for imatinib-resistant CML.

Conclusions:

  • Treatment modification, including switching to a second-generation TKI, is crucial for CML patients with suboptimal responses or failure to imatinib.
  • Individual patient characteristics and TKI profiles guide the selection of optimal second-line therapy.
  • Ongoing research continues to expand therapeutic options for imatinib-resistant CML.