Targeting apoptosis in cancer therapy
For over three decades, a mainstay and goal of clinical oncology has been the development
of therapies promoting the effective elimination of cancer cells by apoptosis. This …
of therapies promoting the effective elimination of cancer cells by apoptosis. This …
MDM2 inhibitors for cancer therapy: the past, present, and future
Since its discovery over 35 years ago, MDM2 has emerged as an attractive target for the
development of cancer therapy. MDM2's activities extend from carcinogenesis to immunity to …
development of cancer therapy. MDM2's activities extend from carcinogenesis to immunity to …
Discovery of Sulanemadlin (ALRN-6924), the first cell-permeating, stabilized α-helical peptide in clinical development
V Guerlavais, TK Sawyer, L Carvajal… - Journal of Medicinal …, 2023 - ACS Publications
We report the discovery of sulanemadlin (ALRN-6924), the first cell-permeating, stabilized α-
helical peptide to enter clinical trials. ALRN-6924 is a “stapled peptide” that mimics the N …
helical peptide to enter clinical trials. ALRN-6924 is a “stapled peptide” that mimics the N …
Phase 1 Trial of ALRN-6924, a Dual Inhibitor of MDMX and MDM2, in Patients with Solid Tumors and Lymphomas Bearing Wild-type TP53
Purpose: We describe the first-in-human dose-escalation trial for ALRN-6924, a stabilized,
cell-permeating peptide that disrupts p53 inhibition by mouse double minute 2 (MDM2) and …
cell-permeating peptide that disrupts p53 inhibition by mouse double minute 2 (MDM2) and …
AZD4573 is a highly selective CDK9 inhibitor that suppresses MCL-1 and induces apoptosis in hematologic cancer cells
J Cidado, S Boiko, T Proia, D Ferguson… - Clinical cancer …, 2020 - AACR
Abstract Purpose: Cyclin-dependent kinase 9 (CDK9) is a transcriptional regulator and
potential therapeutic target for many cancers. Multiple nonselective CDK9 inhibitors have …
potential therapeutic target for many cancers. Multiple nonselective CDK9 inhibitors have …
A phase 2 biomarker-driven study of ruxolitinib demonstrates effectiveness of JAK/STAT targeting in T-cell lymphomas
AJ Moskowitz, P Ghione, E Jacobsen… - Blood, The Journal …, 2021 - ashpublications.org
Signaling through JAK1 and/or JAK2 is common among tumor and nontumor cells within
peripheral T-cell lymphoma (PTCL). No oral therapies are approved for PTCL, and better …
peripheral T-cell lymphoma (PTCL). No oral therapies are approved for PTCL, and better …
Peptide-based agents for cancer treatment: current applications and future directions
Peptide-based strategies have received an enormous amount of attention because of their
specificity and applicability. Their specificity and tumor-targeting ability are applied to …
specificity and applicability. Their specificity and tumor-targeting ability are applied to …
Small-molecule MDM2 inhibitors in clinical trials for cancer therapy
S Wang, FE Chen - European journal of medicinal chemistry, 2022 - Elsevier
Disruption of the MDM2-p53 protein-protein interaction by small-molecule inhibitors has
been highly pursued by many academic laboratories and pharmaceutical companies as a …
been highly pursued by many academic laboratories and pharmaceutical companies as a …
DT2216—a Bcl-xL-specific degrader is highly active against Bcl-xL-dependent T cell lymphomas
Background Patients with advanced T cell lymphomas (TCLs) have limited therapeutic
options and poor outcomes in part because their TCLs evade apoptosis through …
options and poor outcomes in part because their TCLs evade apoptosis through …
Peripheral T cell lymphomas: from the bench to the clinic
Peripheral T cell lymphomas (PTCLs) are a heterogeneous group of orphan neoplasms.
Despite the introduction of anthracycline-based chemotherapy protocols, with or without …
Despite the introduction of anthracycline-based chemotherapy protocols, with or without …