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Timothy P Heffron

Explore the profile of Timothy P Heffron including associated specialties, affiliations and a list of published articles. Areas
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Articles 36
Citations 731
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Recent Articles
1.
Tellis J, Wei B, Siu M, An L, Chan G, Chen Y, et al.
ACS Med Chem Lett . 2024 Sep; 15(9):1606-1614. PMID: 39291002
Hematopoietic progenitor kinase 1 (HPK1) serves a key immunosuppressive role as a negative regulator of T-cell receptor (TCR) signaling. HPK1 loss-of-function is associated with augmentation of immune function and has...
2.
Meng L, Chan E, Ng C, Aimi J, Tran J, Oh A, et al.
Anal Chem . 2022 Sep; 94(37):12927-12933. PMID: 36083155
is one of the most frequently mutated oncogenes, with KRAS G12C recently becoming an actionable target for small molecule intervention. GDC-6036 is an investigational KRAS G12C inhibitor that acts by...
3.
Chan B, Seward E, Lainchbury M, Brewer T, An L, Blench T, et al.
ACS Med Chem Lett . 2022 Jan; 13(1):84-91. PMID: 35059127
Hematopoietic progenitor kinase 1 (HPK1) is implicated as a negative regulator of T-cell receptor-induced T-cell activation. Studies using HPK1 kinase-dead knock-in animals have demonstrated the loss of HPK1 kinase activity...
4.
Song K, Edgar K, Hanan E, Hafner M, Oeh J, Merchant M, et al.
Cancer Discov . 2021 Sep; 12(1):204-219. PMID: 34544753
is one of the most frequently mutated oncogenes; the p110a protein it encodes plays a central role in tumor cell proliferation. Small-molecule inhibitors targeting the PI3K p110a catalytic subunit have...
5.
Liu X, Liang X, LeCouter J, Ubhayakar S, Chen J, Cheng J, et al.
Drug Metab Dispos . 2020 Mar; 48(5):408-419. PMID: 32132091
The objectives of the present study were to characterize GNE-947 for its phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) inhibitory activities, in vitro anti-cell migration activity in human...
6.
Bronner S, Merrick K, Murray J, Salphati L, Moffat J, Pang J, et al.
Bioorg Med Chem Lett . 2019 Jul; 29(16):2294-2301. PMID: 31307887
CDK4 and CDK6 are kinases with similar sequences that regulate cell cycle progression and are validated targets in the treatment of cancer. Glioblastoma is characterized by a high frequency of...
7.
Wu P, Sneeringer C, Pitts K, Day E, Chan B, Wei B, et al.
Structure . 2018 Dec; 27(1):125-133.e4. PMID: 30503777
Enhancement of antigen-specific T cell immunity has shown significant therapeutic benefit in infectious diseases and cancer. Hematopoietic progenitor kinase-1 (HPK1) is a negative-feedback regulator of T cell receptor signaling, which...
8.
Heffron T
Neuro Oncol . 2017 Oct; 20(3):307-312. PMID: 29016919
Despite biological rationale and significant clinical study, the pursuit of small-molecule kinase inhibitors for the treatment of brain cancers has had very limited success. This Advance-in-Brief discusses the need for...
9.
Levin V, Abrey L, Heffron T, Tonge P, Dar A, Weiss W, et al.
CNS Oncol . 2017 Jul; 6(3):167-177. PMID: 28718326
The 2016 second CNS Anticancer Drug Discovery and Development Conference addressed diverse viewpoints about why new drug discovery/development focused on CNS cancers has been sorely lacking. Despite more than 70,000...
10.
Salphati L, Alicke B, Heffron T, Shahidi-Latham S, Nishimura M, Cao T, et al.
Drug Metab Dispos . 2016 Sep; 44(12):1881-1889. PMID: 27638506
Glioblastoma multiforme (GBM) is the most common primary brain tumor in adults. Limited treatment options have only marginally impacted patient survival over the past decades. The phophatidylinositol 3-kinase (PI3K) pathway,...