Publications

AACR 2024

McKeown et al., KB-0742, an oral highly selective CDK9 inhibitor, demonstrates preclinical activity in transcription factor fusion driven adenoid cystic carcinoma patient-derived models

Lenoir et al., p300 catalytic inhibition selectively targets IRF4 oncogenic activity in multiple myeloma

Miguel Villalona-Calero et al., A dose escalation and cohort expansion study of the CDK9 inhibitor KB-0742 in relapsed, refractory and transcriptionally addicted solid tumors

ASH 2023

Pandey, Akanksha, et al., The Novel Profiling Relative Inhibition Simultaneously in Mixtures (PRISM) Platform Identifies Synergistic Activity of Lanraplenib and Ruxolitinib in Hematological Malignancies

Journal of Medicinal Chemistry, November 2023

Freeman, David, et al., Discovery of KB-0742, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of CDK9 for MYC-Dependent Cancers

CTOS 2023

Clinical Poster

Van Tine, Brian, et al., A First-in-human study of CDK9 inhibitor KB-0742 demonstrates preliminary evidence of clinical activity in transcriptionally addicted sarcomas.

AACR-NCI-EORTC 2023

Clinical Poster

Villalona-Calero, Miguel, et al., A First-In-Human Study of CDK9 Inhibitor KB-0742 Demonstrates Evidence of Tolerability and Clinical Activity

Discovery Posters

Cohen, Emily B., et al., Small molecule microarray lysate screen identifies bromodomain ligands that target the MYC transcription regulatory network

Kobylarz, Marek, et al., Small molecule microarray screening identifies novel androgen receptor ligands

SLAS 2023

Walker, William, et. al., Small Molecule Microarray Screening Scale-Up and Automation at Kronos Bio

ASH 2022

Carvajal, Luis A., et. al., SYK Inhibitors Entospletinib and Lanraplenib Show Potent Antileukemic Activity in Combination With Targeted Agent

Carvajal, Luis A., et. al., Development of a Standardized, DNA-Based Next-Generation Sequencing Assay for Assessment of Measurable Residual Disease (MRD) in Acute Myeloid Leukemia (AML)

Döhner, Konstanze, et al., Analysis of Patient-Level Data From 3 Cooperative Group Trials Confirms a Survival Advantage for NPM1-mutated Patients Achieving MRD-Negative CR After Intensive Induction

EORTC-NCI-AACR 2022

Saffran, Douglas C., et al., Regulation of Oncogenic Transcription and Tumor Growth in Pediatric Cancers by the CDK9 Inhibitor KB-0742

EHA 2022

Byrd, John C., et al. AGILITY: A Phase 3, Randomized, Double-Blind, Placebo-Controlled Study of the Efficacy and Safety of Entospletinib Added to Intensive Induction and Consolidation Chemotherapy in Newly Diagnosed NPM1-Mutated AML

Carvajal, Luis A., et al. Pharmacological Inhibition of SYK Confers Anti-proliferative and Novel Anti-tumor Immune Responses in AML

McKeown, Michael, et al. SYK Inhibition Drives Deep Responses in a Biomarker Guided Subset of AML Alone and in Rational Combinations

Stein, Eytan M., et al. Phase 1b/2 Study on Safety, PK, PD and Preliminary Efficacy of the Selective SYK Inhibitor Lanraplenib in Combination with the FLT3 Inhibitor Gilteritinib in FLT3-mutated R/R AML (KB-LANRA 1001)

AACR 2022

Day, Melinda A.L., et al. CDK9 Inhibitor KB-0742 Is Active in Preclinical Models of Small-Cell Lung Cancer. AACR poster, 2022.

Day, Melinda A.L., et al. CDK9 Inhibition via KB-0742 is a Potential Strategy to Treat Transcriptionally Addicted Cancers. AACR poster, 2022.

Day, Melinda A.L., et al. KB-0742 Is Active in Preclinical MYC-High Models of TNBC, Ovarian, and DLBCL Cancers. AACR poster, 2022.

Naffar-Abu Amara, Suha. Development of a Liquid Biopsy Assay to Longitudinally Monitor Changes in Mutations’ Allelic Frequency in Response to KB-0742. AACR poster, 2022.

2021

Byrd, John C., et al. AGILITY: A Phase 3, Randomized, Double-Blind, Placebo-Controlled Study to Assess the Efficacy and Safety of Entospletinib in Combination With Intensive Induction and Consolidation Chemotherapy in Adults With Newly Diagnosed Nucleophosmin 1–Mutated Acute Myeloid Leukemia. ASH poster, 2021

Day, Melinda A.L., et al. Preclinical Activity of Selective SYK Inhibitors, Entospletinib and Lanraplenib, Alone or Combined With Targeted Agents in Ex Vivo AML Models With Diverse Mutational Backgrounds. ASH poster, 2021

Saffran, Douglas C, et al. Preclinical Activity of KB-0742, An Oral, Highly Selective, CDK9 Inhibitor, in Cell Lines and in MYC-High Expressing, Patient-Derived Models of Multiple Breast Cancer Subtypes. SABCS poster, 2021

Day, Melinda, et al. CDK9 inhibition by KB-0742 is selective for transcriptionally addicted tumors harboring MYC genomic amplifications. AACR abstract 1141, 2021

2020

Richters, A et al. Modulating Androgen Receptor-Driven Transcription in Prostate Cancer with Selective CDK9 Inhibitors. Cell Chem. Biol. 2020, 28, 1-14

Richters, A, et al. Targeting oncogenic transcription in prostate cancer with a novel, oral bioavailable, and ultra-selective CDK9 inhibitor. AACR poster, 2020

2019

Struntz N, et al. Stabilization of the Max Homodimer with a Small Molecule Attenuates Myc-Driven Transcription. Cell Chem. Biol. 2019, 26, 1-13

2018

Walker A et al. Results of a Phase 1b/2 Study of Entospletinib Monotherapy and In Combination With Induction Chemotherapy In Newly Diagnosed Patients With Acute Myeloid Leukemia. EHA abstract S118, 2018

Tyner, J et al. Functional genomic landscape of acute myeloid leukemia. Nature. 2018, 562, 526-552

2017 and older

Mohr, S et al. Hoxa9 and Meis1 Cooperatively Induce Addition to Syk Signaling by Suppressing miR-146a in Acute Myeloid Leukemia. Cancer Cell. 2017, 31, 549-562

Pop, M et al. Probing Small-Molecule Microarrays. Curr. Protoc. Chem. Biol. 2014, 6, 209-220

Bradner, J et al. A method for the covalent capture and screening of diverse small molecules. Nature Protocols. 2006, 1(5), 2344-2352

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