Zhiqiang Zheng

Abstract 4569: D3S-003, an orally bioavailable potent and selective dual-state inhibitor targeting both GDP- and GTP-bound KRAS G12D

Jing Zhang, Tienan Wang, Robert A. Mook, Haibo Xie et autres

Abstract KRAS G12D is the most prevalent KRAS mutation in human cancers and represents a highly attractive yet challenging oncogenic target. Compared with KRAS G12C, the intrinsic hydrolysis rate of KRAS G12D is significantly slower, resulting in a more persistent active (GTP-bound) …

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Abstract 1831: First-in-human clinical pharmacokinetic prediction of D3S-003, an orally bioavailable dual-state KRAS G12D inhibitor.

Shaonan Wang, Zhiqiang Zheng, Jing Zhang, Tienan Wang et autres

Abstract Background: D3S-003 is a potent and selective KRAS G12D inhibitor that engages both GDP-bound (OFF) and GTP-bound (ON) KRAS G12D and demonstrates broad preclinical antitumor activity. To support rational first-in-human (FIH) dose selection, translational pharmacokinetic (PK) modeling and allometric scaling were …

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Abstract A005: D3S-002: A Purposefully Designed ERK1/2 Inhibitor Achieving Low-Dose, Pulsatile Target Inhibition for Combination with D3S-001, a New-Generation KRAS G12C Inhibitor

Jing Zhang, Wenqian Wang, Zhiqiang Zheng, Xin Xiong et autres

Abstract Recent genome-wide screens have identified ERK as a central signaling hub in KRAS-mutant tumors and a key driver of resistance to KRAS-targeted therapies. However, prior clinical development of ERK1/2 inhibitors has been hindered by narrow therapeutic windows and on-target toxicity. Consequently, …

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Discovery of D3S-001, a highly potent and CNS-penetrant inhibitor of KRAS G12C with rapid and sustained target engagement kinetics

Junhuai Zhang, J. Lu, Zhiqiang Zheng, An‐Min Wang et autres

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Degradation of the Emerging Contaminant Naproxen in Aqueous Solutions by Dielectric Barrier Discharge

J.Q. Wang, Bowen Zheng, J.B. Zhang, Zhiqiang Zheng