1-Thiazol-2-yl-N-3-methyl-1H-pyrozole-5-carboxylic acid derivatives as antitumor agents.

  title={1-Thiazol-2-yl-N-3-methyl-1H-pyrozole-5-carboxylic acid derivatives as antitumor agents.},
  author={Alan B. Cooper and Stephane Ciblat and Gerald W. Shipps and Jedd F. Levine and Matthew Kostura and Vibha B. Oza and L{\'e}a Constantineau-Forget and Martin D{\'e}ry and Chantal Grand-Ma{\^i}tre and Nicolas Bruneau-Latour and {\'E}dith Bellavance and Michael A. Patane and Arshad M Siddiqui and Michael Luther},
  journal={Bioorganic \& medicinal chemistry letters},
  volume={27 18},

Pharmacological activation of the mitochondrial stress protease OMA1 reveals a therapeutic liability in Diffuse Large B-Cell Lymphoma

BTM-3566 represents a first- of-its kind approach of selectively hyperactivating the mitochondrial ISR for treating DLBCL and identifies the mitochondrial protein FAM210B as a negative regulator of B TM-3528 and BTM- 3566 activity.

Targeting aggressive B-cell lymphomas through pharmacological activation of the mitochondrial protease OMA1

(140/150 words) Constitutive activation of the ATF4-mediated integrated stress response (ATF4-ISR) is common in cancer and buffers the metabolic challenges imposed by rapid proliferation. However,



3‐Substituted Indazoles as Configurationally Locked 4EGI‐1 Mimetics and Inhibitors of the eIF4E/eIF4G Interaction

In a structure–activity relationship study directed towards probing the structural latitude of this new chemotype as an inhibitor of eIF4E/eIF4G interaction and translation initiation, compound 1 d, an indazole‐based 4EGI‐1 mimetic, is identified as a new and improved lead inhibitor and a promising molecular probe candidate for elucidation of the role of cap‐dependent translation initiation in a host of pathophysiological states.

Suzuki Cross Coupling Reaction- A Review

Suzuki cross coupling reaction is one of the most famous reaction in the field of chemistry. It is a very effective method for making carbon – carbon bonds. It has been extensively utilized in the

A chemical method for fast and sensitive detection of DNA synthesis in vivo

The method does not require sample fixation or DNA denaturation and permits good structural preservation, and the small size of the fluorescent azides used for detection results in a high degree of specimen penetration, allowing the staining of whole-mount preparations of large tissue and organ explants.

Current progress in Structure-Based Rational Drug Design marks a new mindset in drug discovery

The role of SBDD with respect to two different classes of widely investigated pharmaceutical targets: (a) protein kinases (PK) and (b) G-protein coupled receptors (GPCR) is discussed.

Molecular mechanism of the dual activity of 4EGI-1: Dissociating eIF4G from eIF4E but stabilizing the binding of unphosphorylated 4E-BP1

The major finding is that the C-terminal extension (motif 3) is critical to 4E-BP1–mediated cell cycle arrest and that it partially overlaps with the binding site of 4EGI-1.

PTEN loss defines a PI3K/AKT pathway-dependent germinal center subtype of diffuse large B-cell lymphoma

The results indicate that PTEN loss defines a PI3K/AKT-dependent GCB DLBCL subtype that is addicted to PI3k and MYC signaling and suggest that pharmacologic inhibition of PI3 k might represent a promising therapeutic approach in these lymphomas.

Structure of the eukaryotic translation initiation factor eIF4E in complex with 4EGI-1 reveals an allosteric mechanism for dissociating eIF4G

It is found that inhibition of eIF4G binding must be allosteric, because the 4EGI-1 and eif4G bind at distant epitopes on eIF 4E, and 4EGi-1 acts allosterically by binding to a site on e IF4E distant from the eIF3G binding epitope.