Hematopoietic progenitor kinase 1 in tumor immunology: a medicinal chemistry perspective

Q Zhu, N Chen, X Tian, Y Zhou, QD You… - Journal of Medicinal …, 2022 - ACS Publications
Hematopoietic progenitor kinase 1 (HPK1), a hematopoietic cell-restricted member of the
serine/threonine Ste20-related protein kinases, is a negative regulator of the T cell receptor …

The development of small-molecule inhibitors targeting HPK1

L Zhou, T Wang, K Zhang, X Zhang, S Jiang - European Journal of …, 2022 - Elsevier
Abstract Hematopoietic progenitor kinase 1 (HPK1), a 97-kDa serine/threonine Ste20-
related protein kinase, is a negative regulator of T cells, B cells, and dendritic cells-mediated …

Small-molecule in cancer immunotherapy: Revolutionizing cancer treatment with transformative, game-changing breakthroughs

S Chattopadhyay, R Hazra, A Mallick, S Gayen… - … et Biophysica Acta (BBA …, 2024 - Elsevier
Immunotherapy has revolutionized cancer management, with antibody-based treatments
leading the charge due to their superior pharmacodynamics, including enhanced …

Design, synthesis, and pharmacological evaluation of isoindoline analogues as new HPK1 inhibitors

C Xie, B Liu, Z Song, Y Yang, M Dai… - Journal of Medicinal …, 2023 - ACS Publications
Hematopoietic progenitor kinase 1 (HPK1) is an important negative regulator in T-cell
receptor signaling and as a promising key target for immunotherapy. Herein, based on the …

Discovery of 7H-Pyrrolo [2, 3-d] pyrimidine Derivatives as potent hematopoietic progenitor kinase 1 (HPK1) inhibitors

F Wu, H Li, Q An, Y Sun, J Yu, W Cao, P Sun… - European Journal of …, 2023 - Elsevier
Abstract Hematopoietic progenitor kinase 1 (HPK1) is predominantly expressed in
hematopoietic cells and is a negative regulator of T cell receptor (TCR) signaling. Recent …

Inhibitors of immuno-oncology target HPK1–a patent review (2016 to 2020)

ID Linney, N Kaila - Expert Opinion on Therapeutic Patents, 2021 - Taylor & Francis
Introduction: Hematopoietic progenitor kinase (HPK1), a serine/threonine kinase, which is
primarily expressed in hematopoietic cells is a negative regulator of T-cell receptor and B …

Discovery of diaminopyrimidine carboxamide HPK1 inhibitors as preclinical immunotherapy tool compounds

BA Vara, SM Levi, A Achab, DA Candito… - ACS Medicinal …, 2021 - ACS Publications
Hematopoietic progenitor kinase 1 (HPK1), a serine/threonine kinase, is a negative immune
regulator of T cell receptor (TCR) and B cell signaling that is primarily expressed in …

Identification of potent reverse indazole inhibitors for HPK1

EC Yu, JL Methot, X Fradera, CA Lesburg… - ACS Medicinal …, 2021 - ACS Publications
Hematopoietic progenitor kinase (HPK1), a negative regulator of TCR-mediated T-cell
activation, has been recognized as a novel antitumor immunotherapy target. Structural …

Pharmacological inhibition of hematopoietic progenitor kinase 1 positively regulates T-cell function

Y Wang, K Zhang, P Georgiev, S Wells, H Xu… - Plos one, 2020 - journals.plos.org
Hematopoietic progenitor kinase 1 (HPK1), a hematopoietic cell-specific Ste20-related
serine/threonine kinase, is a negative regulator of signal transduction in immune cells …

Development of a series of quinazoline-2, 5-diamine derivatives as potent hematopoietic progenitor kinase 1 (HPK1) inhibitors

H Shi, H Tang, Y Li, D Chen, T Liu, Y Chen… - European Journal of …, 2023 - Elsevier
Abstract Hematopoietic progenitor kinase 1 (HPK1) is a serine/threonine kinase that serves
as the negative regulator of multiple immune signaling pathways. Genetic studies using …