ArticleCell2024
DrugMap: A quantitative pan-cancer analysis of cysteine ligandability.
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Article in Cell, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 57 papers.
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57citing papers in PubMed
19.7field-weighted citation impact, top 1% of its field
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57 citing papers in PubMed, 79 citations in OpenAlex.
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Authors and funding
71 authors at 5 institutions in 1 country.
Mariko TakahashiKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA. Electronic address: mtaka@umich.edu.
Harrison B ChongKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Siwen ZhangKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Tzu-Yi YangKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Matthew J LazarovKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Stefan HarryKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA; Department of Chemistry and Chemical Biology, Harvard University, Cambridge, MA 02138, USA.
Michelle MaynardScorpion Therapeutics, Boston, MA 02110, USA.
Brendan HilbertScorpion Therapeutics, Boston, MA 02110, USA.
Ryan D WhiteScorpion Therapeutics, Boston, MA 02110, USA.
Heather E MurreyScorpion Therapeutics, Boston, MA 02110, USA.
Chih-Chiang TsouScorpion Therapeutics, Boston, MA 02110, USA.
Kira VordermarkKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Jonathan AssaadKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Magdy GoharKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Benedikt R DürrKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Marianne RichterKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Himani PatelKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Gregory KryukovScorpion Therapeutics, Boston, MA 02110, USA.
Natasja BrooijmansScorpion Therapeutics, Boston, MA 02110, USA.
Aliyu Sidi Omar AlghaliDepartment of Pathology, Massachusetts General Hospital, Boston, MA 02114, USA.
Karla RubioDepartment of Pathology, Massachusetts General Hospital, Boston, MA 02114, USA.
Antonio VillanuevaDepartment of Pathology, Massachusetts General Hospital, Boston, MA 02114, USA.
Junbing ZhangKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Maolin GeKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Farah MakramKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Hanna GriesshaberKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Drew HarrisonKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Ann-Sophie KoglinKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Samuel OjedaKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Barbara KarakyriakouKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Alexander HealyKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
George PopoolaKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Inbal RachminCutaneous Biology Research Center, Massachusetts General Hospital, Boston, MA 02114, USA.
Neha KhandelwalKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Jason R NeilScorpion Therapeutics, Boston, MA 02110, USA.
Pei-Chieh TienKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Nicholas ChenKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA; Department of Pathology, Harvard Medical School, Boston, MA 02114, USA.
Tobias HospKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Sanne van den OuwelandKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Toshiro HaraDepartment of Pathology, Massachusetts General Hospital, Boston, MA 02114, USA.
Lillian BussemaDepartment of Pathology, Massachusetts General Hospital, Boston, MA 02114, USA.
Rui DongDepartment of Pathology, Massachusetts General Hospital, Boston, MA 02114, USA.
Lei ShiKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Martin Q RasmussenKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Ana Carolina DominguesKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Aleigha LawlessDepartment of Surgery, Massachusetts General Hospital, Boston, MA 02114, USA; Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA.
Jacy FangKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA; Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA.
Satoshi YodaKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Linh Phuong NguyenKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Sarah Marie ReevesKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Farrah Nicole WakefieldKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Adam AckerKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Sarah Elizabeth ClarkKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Taronish DubashKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
John KastanosKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA.
Eugene OhKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA; Department of Medicine, Harvard Medical School, Boston, MA 02114, USA.
David E FisherCutaneous Biology Research Center, Massachusetts General Hospital, Boston, MA 02114, USA.
Shyamala MaheswaranKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA; Department of Medicine, Harvard Medical School, Boston, MA 02114, USA.
Daniel A HaberKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA; Department of Medicine, Harvard Medical School, Boston, MA 02114, USA; Howard Hughes Medical Institute, Chevy Chase, MD 20815, USA.
Genevieve M BolandKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA; Department of Surgery, Massachusetts General Hospital, Boston, MA 02114, USA; Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA; Department of Surgery, Harvard Medical School, Boston, MA 02114, USA.
Moshe Sade-FeldmanKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA; Department of Medicine, Harvard Medical School, Boston, MA 02114, USA.
Russell W JenkinsKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA; Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA; Department of Medicine, Harvard Medical School, Boston, MA 02114, USA.
Aaron N HataKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA; Department of Medicine, Harvard Medical School, Boston, MA 02114, USA.
Nabeel M BardeesyKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA; Department of Medicine, Harvard Medical School, Boston, MA 02114, USA.
Mario L SuvàKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA; Department of Pathology, Massachusetts General Hospital, Boston, MA 02114, USA; Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA; Department of Pathology, Harvard Medical School, Boston, MA 02114, USA.
Brent R MartinScorpion Therapeutics, Boston, MA 02110, USA.
Brian B LiauDepartment of Chemistry and Chemical Biology, Harvard University, Cambridge, MA 02138, USA.
Christopher J OttKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA; Department of Medicine, Harvard Medical School, Boston, MA 02114, USA.
Miguel N RiveraKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA; Department of Pathology, Massachusetts General Hospital, Boston, MA 02114, USA; Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA; Department of Pathology, Harvard Medical School, Boston, MA 02114, USA.
Michael S LawrenceKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA; Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA; Department of Pathology, Harvard Medical School, Boston, MA 02114, USA. Electronic address: mslawrence@mgh.harvard.edu.
Liron Bar-PeledKrantz Family Center for Cancer Research, Massachusetts General Hospital Cancer Center, Charlestown, MA 02129, USA; Department of Medicine, Harvard Medical School, Boston, MA 02114, USA. Electronic address: lbar-peled@mgh.harvard.edu.
Massachusetts General Hospital · USHarvard University · USScorpion Therapeutics (United States) · USBroad Institute · USHoward Hughes Medical Institute · US
Funding
Transcriptional mechanisms and melanomaP01CA163222 · NCI · MASSACHUSETTS GENERAL HOSPITAL · PI DAVID E FISHER · 2013 to 2026
$25.3MThe MITF transcriptional network: melanoma risk and carcinogenesisR01AR043369 · NIAMS · MASSACHUSETTS GENERAL HOSPITAL · PI DAVID E FISHER · 1996 to 2026
$9.4MModeling Metastasis and Acquired Drug Resistance Using Circulating Tumor CellsR01CA129933 · NCI · MASSACHUSETTS GENERAL HOSPITAL · PI Daniel A. Haber · 2008 to 2026
$7.5MThe Activation of ERBB3 Signaling as a Resistance Mechanism to Targeted TherapiesR01CA137008 · NCI · MASSACHUSETTS GENERAL HOSPITAL · PI Aaron N Hata, ZOFIA PIOTROWSKA · 2009 to 2026
$5.7MOvercoming Resistance Mechanisms to Anaplastic Lymphoma Kinase InhibitorsR01CA164273 · NCI · MASSACHUSETTS GENERAL HOSPITAL · PI Aaron N Hata, Jessica Jiyeong Lin · 2012 to 2026
$5.5MTherapeutic strategies for treatment of giant congenital melanocytic neviR01AR072304 · NIAMS · MASSACHUSETTS GENERAL HOSPITAL · PI DAVID E FISHER · 2017 to 2026
$3.9MDissecting the cellular hierarchies of malignant gliomas by single-cell functional genomicsR37CA245523 · NCI · MASSACHUSETTS GENERAL HOSPITAL · PI Mario Luca Suva · 2020 to 2026
$2.8MMapping Structure-Activity Relationships of Chemical Inhibitors via Genome-EditingDP2GM137494 · NIGMS · HARVARD UNIVERSITY · PI LIAU, BRIAN · 2019 to 2019
$2.5MControl of histone ubiquitylation during the cell cycleR35GM146933 · NIGMS · MASSACHUSETTS GENERAL HOSPITAL · PI Eugene Oh · 2022 to 2026
$2.1MIdentification of Covalent Transcriptional Dependencies in MelanomaR01CA285415 · NCI · MASSACHUSETTS GENERAL HOSPITAL · PI Liron Bar-Peled, Brian Liau · 2024 to 2026
$2.0MDeciphering the Role of Reductive Stress in Non Small Cell Lung CancerR37CA260062 · NCI · MASSACHUSETTS GENERAL HOSPITAL · PI Liron Bar-Peled · 2022 to 2026
$1.9MA druggable dependency in low-MITF/high-AXL melanoma: preclinical efficacy and mechanism of action in a key treatment-resistant subclass.R01CA222871 · NCI · MASSACHUSETTS GENERAL HOSPITAL · PI FISHER, DAVID E · 2018 to 2022
$1.8MNCI NIH HHS K08 CA226391NCI NIH HHS K99 CA215249NCI NIH HHS P01 CA163222NCI NIH HHS R00 CA215249NCI NIH HHS R01 CA129933NCI NIH HHS R01 CA137008NCI NIH HHS R01 CA164273NCI NIH HHS R01 CA222871NCI NIH HHS R01 CA285415NCI NIH HHS R21 CA256082NCI NIH HHS R37 CA245523NCI NIH HHS R37 CA260062NIAMS NIH HHS R01 AR043369NIAMS NIH HHS R01 AR072304NIA NIH HHS R21 AG083413NIGMS NIH HHS DP2 GM137494NIGMS NIH HHS R35 GM146933NIGMS NIH HHS R35 GM153476
Abstract
Cysteine-focused chemical proteomic platforms have accelerated the clinical development of covalent inhibitors for a wide range of targets in cancer. However, how different oncogenic contexts influence cysteine targeting remains unknown. To address this question, we have developed "DrugMap," an atlas of cysteine ligandability compiled across 416 cancer cell lines. We unexpectedly find that cysteine ligandability varies across cancer cell lines, and we attribute this to differences in cellular redox states, protein conformational changes, and genetic mutations. Leveraging these findings, we identify actionable cysteines in NF-κB1 and SOX10 and develop corresponding covalent ligands that block the activity of these transcription factors. We demonstrate that the NF-κB1 probe blocks DNA binding, whereas the SOX10 ligand increases SOX10-SOX10 interactions and disrupts melanoma transcriptional signaling. Our findings reveal heterogeneity in cysteine ligandability across cancers, pinpoint cell-intrinsic features driving cysteine targeting, and illustrate the use of covalent probes to disrupt oncogenic transcription-factor activity.
Indexed as
CysteineNeoplasmsAnimalsCell Line, TumorHumansLigandsMelanomaMiceNF-kappa BOxidation-ReductionSignal TransductionSOXE Transcription FactorsCysteineLigandsNF-kappa BSOX10 protein, humanSOXE Transcription Factorschemical proteomicscovalent inhibitorscysteine ligandabilitytranscription factors
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