Discovery of a Potent and Selective STAT5 PROTAC Degrader with Strong Antitumor Activity In Vivo in Acute Myeloid Leukemia

A selective small-molecule STAT5 PROTAC degrader capable of achieving tumor regression in vivo

(2023) Atsunori Kaneshige et al.   Nature Chemical Biology

SD-91 as A Potent and Selective STAT3 Degrader Capable of Achieving Complete and Long-Lasting Tumor Regression

(2021) Haibin Zhou et al.   ACS Medicinal Chemistry Letters

High activation of STAT5A drives peripheral T-cell lymphoma and leukemia

(2019) Barbara Maurer et al.   HAEMATOLOGICA

A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo

(2019) Longchuan Bai et al.   CANCER CELL

Structure-Based Discovery of SD-36 as a Potent, Selective, and Efficacious PROTAC Degrader of STAT3 Protein

(2019) Haibin Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Small molecule targeting of the STAT5/6 Src homology 2 (SH2) domains to inhibit allergic airway disease

(2018) J. Morgan Knight et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Pharmacologic inhibition of STAT5 in acute myeloid leukemia

(2018) Bettina Wingelhofer et al.   LEUKEMIA

STAT5 in Cancer and Immunity

(2016) Aradhana Rani et al.   JOURNAL OF INTERFERON AND CYTOKINE RESEARCH

Nanomolar Inhibitors of the Transcription Factor STAT5b with High Selectivity over STAT5a

(2015) Nagarajan Elumalai et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Targeting the Src Homology 2 (SH2) Domain of Signal Transducer and Activator of Transcription 6 (STAT6) with Cell-Permeable, Phosphatase-Stable Phosphopeptide Mimics Potently Inhibits Tyr641 Phosphorylation and Transcriptional Activity

(2015) Pijus K. Mandal et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Screen Identifies a Potent Small Molecule Inhibitor of Stat5a/b with Therapeutic Potential for Prostate Cancer and Chronic Myeloid Leukemia

(2015) Z. Liao et al.   MOLECULAR CANCER THERAPEUTICS

Nanomolar-Potency Small Molecule Inhibitor of STAT5 Protein

(2014) Abbarna A. Cumaraswamy et al.   ACS Medicinal Chemistry Letters

Synthesis and in Vitro Evaluation of a Peptidomimetic Inhibitor Targeting the Src Homology 2 (SH2) Domain of STAT6

(2013) Pietro Morlacchi et al.   ACS Medicinal Chemistry Letters

Essential role for Stat5a/b in myeloproliferative neoplasms induced by BCR-ABL1 and JAK2V617F in mice

(2012) C. Walz et al.   BLOOD

JAK/STAT signaling in hematological malignancies

(2012) W Vainchenker et al.   ONCOGENE

Potent and Selective Phosphopeptide Mimetic Prodrugs Targeted to the Src Homology 2 (SH2) Domain of Signal Transducer and Activator of Transcription 3

(2011) Pijus K. Mandal et al.   JOURNAL OF MEDICINAL CHEMISTRY

Small Molecule STAT5-SH2 Domain Inhibitors Exhibit Potent Antileukemia Activity

(2011) Brent D. G. Page et al.   JOURNAL OF MEDICINAL CHEMISTRY

Features and development ofCoot

(2010) P. Emsley et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Stat5 is indispensable for the maintenance ofbcr/abl-positive leukaemia

(2010) Andrea Hoelbl et al.   EMBO Molecular Medicine

FLT3-ITD up-regulates MCL-1 to promote survival of stem cells in acute myeloid leukemia via FLT3-ITD-specific STAT5 activation

(2009) G. Yoshimoto et al.   BLOOD