Tom D Heightman
Overview
Explore the profile of Tom D Heightman including associated specialties, affiliations and a list of published articles.
Author names and details appear as published. Due to indexing inconsistencies, multiple individuals may share a name, and a single author may have variations. MedLuna displays this data as publicly available, without modification or verification
Snapshot
Snapshot
Articles
57
Citations
3483
Followers
0
Related Specialties
Related Specialties
Top 10 Co-Authors
Top 10 Co-Authors
Published In
Affiliations
Affiliations
Soon will be listed here.
Recent Articles
1.
Johannes J, Balazs A, Barratt D, Bista M, Chuba M, Cosulich S, et al.
J Med Chem
. 2024 Dec;
67(24):21717-21728.
PMID: 39655996
PARP inhibitors have attracted considerable interest in drug discovery due to the clinical success of first-generation agents such as olaparib, niraparib, rucaparib, and talazoparib. Their success lies in their ability...
2.
Tamanini E, Miyamura S, Buck I, Cons B, Dawson L, East C, et al.
ACS Med Chem Lett
. 2022 Oct;
13(10):1591-1597.
PMID: 36262388
Fragment-based ligand discovery was successfully applied to histone deacetylase HDAC2. In addition to the anticipated hydroxamic acid- and benzamide-based fragment screening hits, a low affinity (∼1 mM) α-amino-amide zinc binding...
3.
Norton D, Bonnette W, Callahan J, Carr M, Griffiths-Jones C, Heightman T, et al.
J Med Chem
. 2021 Oct;
64(21):15949-15972.
PMID: 34705450
The NRF2-mediated cytoprotective response is central to cellular homoeostasis, and there is increasing interest in developing small-molecule activators of this pathway as therapeutics for diseases involving chronic oxidative stress. The...
4.
Johannes J, Balazs A, Barratt D, Bista M, Chuba M, Cosulich S, et al.
J Med Chem
. 2021 Sep;
64(19):14498-14512.
PMID: 34570508
Poly-ADP-ribose-polymerase (PARP) inhibitors have achieved regulatory approval in oncology for homologous recombination repair deficient tumors including BRCA mutation. However, some have failed in combination with first-line chemotherapies, usually due to...
5.
Heightman T, Berdini V, Bevan L, Buck I, Carr M, Courtin A, et al.
J Med Chem
. 2021 Aug;
64(16):12286-12303.
PMID: 34387469
Aberrant activation of the mitogen-activated protein kinase pathway frequently drives tumor growth, and the ERK1/2 kinases are positioned at a key node in this pathway, making them important targets for...
6.
Munck J, Berdini V, Bevan L, Brothwood J, Castro J, Courtin A, et al.
Mol Cancer Ther
. 2021 Jul;
20(10):1757-1768.
PMID: 34330842
The MAPK signaling pathway is commonly upregulated in human cancers. As the primary downstream effector of the MAPK pathway, ERK is an attractive therapeutic target for the treatment of MAPK-activated...
7.
St Denis J, Hall R, Murray C, Heightman T, Rees D
RSC Med Chem
. 2021 May;
12(3):321-329.
PMID: 34041484
This Review describes the increasing demand for organic synthesis to facilitate fragment-based drug discovery (FBDD), focusing on polar, unprotected fragments. In FBDD, X-ray crystal structures are used to design target...
8.
Heightman T, Callahan J, Chiarparin E, Coyle J, Griffiths-Jones C, Lakdawala A, et al.
J Med Chem
. 2019 Apr;
62(9):4683-4702.
PMID: 30973731
The KEAP1-NRF2-mediated cytoprotective response plays a key role in cellular homoeostasis. Insufficient NRF2 signaling during chronic oxidative stress may be associated with the pathophysiology of several diseases with an inflammatory...
9.
Grainger R, Heightman T, Ley S, Lima F, Johnson C
Chem Sci
. 2019 Mar;
10(8):2264-2271.
PMID: 30881651
In fragment-based drug discovery (FBDD), a weakly binding fragment hit is elaborated into a potent ligand by bespoke functionalization along specific directions (growth vectors) from the fragment core in order...
10.
Lebraud H, Surova O, Courtin A, OReilly M, Valenzano C, Nordlund P, et al.
Chem Sci
. 2018 Dec;
9(45):8608-8618.
PMID: 30568786
Target engagement is a key concept in drug discovery and its direct measurement can provide a quantitative understanding of drug efficacy and/or toxicity. Failure to demonstrate target occupancy in relevant...