HK2 inhibitors(Hexokinase type II inhibitors), MASP2 inhibitors(Mannan-binding lectin serine protease 2 inhibitors), PDC complex inhibitors(Pyruvate dehydrogenase complex inhibitors)

Therapeutic Areas

NeoplasmsSkin and Musculoskeletal Diseases

Active Indication-

Inactive Indication

Breast Cancer

Originator Organization

The Johns Hopkins University

Active Organization-

Inactive Organization

The Johns Hopkins University

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

RegulationOrphan Drug (United States)

Structure/Sequence

Molecular FormulaC3H3BrO3

InChIKeyPRRZDZJYSJLDBS-UHFFFAOYSA-N

CAS Registry1113-59-3

100 Clinical Results associated with Bromopyruvate

100 Translational Medicine associated with Bromopyruvate

100 Patents (Medical) associated with Bromopyruvate

903

Literatures (Medical) associated with Bromopyruvate

31 Dec 2025·Green Chemistry Letters and Reviews

Guaiazulene and aureusidin inhibit metabolic adaptability and virulence in Candida albicans by targeting the glyoxylate cycle under alternative carbon conditions

Author: Shastry, Rajesh P. ; Mallik, Saurav ; Rao, R. Shyama Prasad ; Zhao, Zhongming ; Ghate, Sudeep D. ; Giri, Jayant

Several Candida species such as C. albicans and C. auris have emerged as formidable multidrug-resistant pathogens, posing significant challenges to global healthcare.C. albicans can rapidly adapt its metabolism under nutrient-limited conditions, such as low-carbon environments, leading to virulence and drug resistance.Therefore, identifying novel compounds that can disrupt this metabolic adaptability is crucial for developing effective therapeutic strategies against this elusive pathogen.In this study, we first employed an in-silico dynamics approach to investigate the inhibitory effects of guaiazulene and aureusidin on C. albicans metabolic adaptability and virulence.By employing mol. docking and mol. dynamics simulations, we demonstrated that these compounds strongly interacted with crucial enzymes involved in the glyoxylate cycle, impairing their catalytic functions.Guaiazulene exhibited the highest binding affinity for malate synthase and isocitrate lyase, with a docking score of -8.5 and -9.3 kcal/mol, resp.The ADME properties of these mols. were also examined to evaluate the pharmacol. parameters.Furthermore, we investigated the impact of guaiazulene and aureusidin on C. albicans growth and biofilm formation.Our findings indicated that the targeting the glyoxylate cycle represents a promising strategy to counteract the metabolic adaptability of C. albicans and enhance the efficacy of antifungal agents.

01 Jul 2025·Free Radical Biology and Medicine

3-Bromopyruvate boosts the effect of chemotherapy in acute myeloid leukemia by a pro-oxidant mechanism

Article

Author: Casal, Margarida ; Preto, Ana ; Celeiro, Sónia Pires ; Baltazar, Fátima ; Granja, Sara ; Ko, Young Hee ; Barbosa-Matos, Catarina ; Queirós, Odília ; Pereira-Vieira, Joana

Acute myeloid leukemia (AML) comprises a diverse group of blood cancers with varying genetic, phenotypic, and clinical traits, making development of targeted therapy challenging. Metabolic reprogramming in AML has been described as relevant for chemotherapy effectiveness. 3-Bromopyruvate (3-BP) is an anticancer agent that undermines energy metabolism of cancer cells. However, the effect of 3-BP in hematologic malignancies, such as AML, needs further investigation. Thus, we aimed to explore 3-BP as a chemo-sensitizing agent in AML. Different approaches of combining 3-BP with classical chemotherapy (daunorubicin and cytarabin) were tested in diverse AML cell lines. Cell sensitivity to the different drug combinations was analyzed by Trypan blue staining. The effect of pre-treatment with a non-toxic concentration of 3-BP was assessed on the AML cell metabolic profile (Western blot and immunofluorescence), mitochondrial activity (cytometry flow), and antioxidant capacity (colorimetric detection kit). KG-1 and MOLM13 cells showed increased sensitivity to chemotherapy (decreased EC₅₀ values) after exposure to a non-toxic concentration (5 μM) of 3-BP. In both cell lines, 5 μM 3-BP decreased glucose consumption without changing extracellular lactate levels. 5 μM 3-BP treatment increased reactive oxygen species levels and decreased cell antioxidant capacity by depleting reduced glutathione levels in both KG-1 and MOLM13 cells. Our results demonstrate that non-toxic concentrations of 3-BP enhance the effect of classical chemotherapy in AML cells through a pro-oxidant mechanism. These data unveiled a new approach for AML treatment, using 3-BP or other pro-oxidant agents as co-adjuvants of chemotherapy, subsiding chemotherapy-induced side effects.

01 Jun 2025·Regenerative Therapy

DDIT4 participates in high glucose-induced fibroblast-like synoviocytes overactivation and cartilage injury by regulating glycolysis

Article

Author: Dong, Yonghui ; Zheng, Jia ; Liu, Yunke ; Cheng, Cheng ; Tang, Chao ; Qiang, Shuo

ObjectiveMore and more evidence show that diabetes is closely related to osteoarthritis (OA). However, the role and mechanism of DNA damage-inducible transcript 4 protein (DDIT4) in diabetic OA (DOA) have not been clarified.MethodsWe collected OA patients and non-OA subjects who underwent total knee replacement surgery, and analyzed the DDIT4 expression in synovial samples using RT-qPCR. The cell viability of fibroblast-like synoviocytes (FLSs) was measured by CCK-8 assay. Annexin V-FITC/PI double staining was used to detect the cell apoptosis. Scratch and Transwell assays were used to determine cell migration and invasion, respectively.ResultsThe levels of cellular inflammatory factors (IL-1β, IL-6 and TNF-α), oxidative stress and glycolysis related indicators were detected by using kits. Western blot was used to determine the expression of DDIT4, Aggrecan, COL3A1, MMP3, MMP13, HK2, PFKP and PKM2 in FLSs or ATDC5 cells. The results showed that the expression level of DDIT4 was significantly reduced in the synovial samples of OA patients and primary FLSs. Functional studies showed that DDIT4 overexpression inhibited the overactivation, migration, and invasion of FLSs, as well as alleviated chondrocyte injury co-cultured with FLSs. Importantly, the expression of DDIT4 was down-regulated in patients with DOA and closely related to DOA. Further research found that high glucose (HG) promoted excessive activation, migration, and invasion of FLSs, and exacerbated the followed chondrocyte injury. Overexpression of DDIT4 alleviated HG-induced abnormal function of FLSs and injury to chondrocytes. Importantly, DDIT4 inhibited lactate synthesis, glucose uptake, LDH activity, extracellular acidification rate, oxygen consumption rate, and expression levels of glycolysis related protein (HK2, PFKP, PKM2) in HG-induced FLSs. And the glycolysis inhibitors (Cyto-B and 3BrPA) alleviated the injury of ATDC5 chondrocytes co-cultured with FLSs.ConclusionsDDIT4 participates in HG-induced FLSs overactivation and inflammation response, as well as chondrocyte injury and OA progression by regulating glycolysis processes.

100 Deals associated with Bromopyruvate

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Indication	Highest Phase	Country/Location	Organization	Date
Breast Cancer	Preclinical	-	The Johns Hopkins University	-

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