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Related Concept Videos

MAPK Signaling Cascades01:07

MAPK Signaling Cascades

Mitogen-activated protein kinase, or MAPK pathway, activates three sequential kinases to regulate cellular responses such as proliferation, differentiation, survival, and apoptosis. The canonical MAPK pathway starts with a mitogen or growth factor binding to an RTK. The activated RTKs stimulate Ras, which recruits Raf or MAP3 Kinase (MAPKKK), the first kinase of the MAPK signaling cascade. Raf further phosphorylates and activates MEK or MAP2 Kinases (MAPKK), which in turn phosphorylates MAP...
Inhibition of Cdk Activity02:34

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...
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

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...
PI3K/mTOR/AKT Signaling Pathway01:22

PI3K/mTOR/AKT Signaling Pathway

The mammalian target of rapamycin  (mTOR) is a serine/threonine kinase that regulates growth, proliferation, and cell survival in response to hormones, growth factors, or nutrient availability. This kinase exists in two structurally and functionally distinct forms: mTOR complex 1  (mTORC1) and mTOR complex 2  (mTORC2). The first form (mTORC1) is composed of a rapamycin-sensitive Raptor and proline-rich Akt substrate, PRAS40. In contrast,  mTORC2 consists of a rapamycin-insensitive companion...
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Transducer Mechanism: Enzyme-Linked Receptors

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.
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Related Experiment Video

Updated: Jun 29, 2026

Assaying Protein Kinase Activity with Radiolabeled ATP
08:05

Assaying Protein Kinase Activity with Radiolabeled ATP

Published on: May 26, 2017

'Reverse' alpha-ketoamide-based p38 MAP kinase inhibitors.

Antonio Garrido Montalban1, Erik Boman, Chau-Dung Chang

  • 1Drug Discovery, Kemia, Inc., 5871 Oberlin Drive, Suite 100, San Diego, CA 92121, USA. catalaba@hotmail.com

Bioorganic & Medicinal Chemistry Letters
|October 7, 2008
PubMed
Summary

Researchers developed new potent p38 inhibitors using an alpha-ketoamide scaffold. Reversing the scaffold

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Identification of Kinase-substrate Pairs Using High Throughput Screening
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Last Updated: Jun 29, 2026

Assaying Protein Kinase Activity with Radiolabeled ATP
08:05

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Identification of Kinase-substrate Pairs Using High Throughput Screening
11:13

Identification of Kinase-substrate Pairs Using High Throughput Screening

Published on: August 29, 2015

Area of Science:

  • Medicinal Chemistry
  • Pharmacology

Background:

  • p38 inhibitors are crucial therapeutic targets.
  • Previous research established an alpha-ketoamide scaffold for p38 inhibition.

Purpose of the Study:

  • To identify novel, potent p38 inhibitors.
  • To explore chemical modifications of the alpha-ketoamide scaffold.

Main Methods:

  • Synthesis of a new series of compounds based on an alpha-ketoamide scaffold.
  • Evaluation of inhibitory potency against p38.

Main Results:

  • A second series of potent p38 inhibitors was identified.
  • Reversing the ketoamide order enhanced chemical flexibility.
  • Improved potencies against p38 were achieved.

Conclusions:

  • The modified alpha-ketoamide scaffold offers a promising route to potent p38 inhibitors.
  • This structural modification enhances drug design flexibility and efficacy.