Acta Pharmaceutica Sinica B

Home Latest Articles

Latest Articles

Author correction to “Cerium single-atom catalysts-armed Lactobacillus reuteri for multipronged anti-inflammatory/anti-fibrotic therapy of inflammatory bowel disease” [Acta Pharmaceutica Sinica B 15 (2025) 5400-5415]

Yinying Pu, Shaorong Huang, Shuang Gao, Yangying Duan, Wenhao Li, Qiyue Li, Han Lin, Kun Zhang, Min Zhou, Wencheng Wu

Acta Pharmaceutica Sinica B. 2026, 16(2): 1173-1174.
Transmitophagy in the heart: An overview of molecular mechanisms and implications for pathophysiology

Acta Pharmaceutica Sinica B. 2026, 16(1): 1-12.

Mitochondria are essential for meeting cardiac metabolic demands and their dysfunction is associated with heart failure and is a key mediator of cardiac ischemia-reperfusion injury. Cardiomyocytes engage integrated mechanisms to maintain mitochondrial function; however, chronic stress or disease can overwhelm this capacity. The removal of damaged mitochondria is mediated by a process known as mitophagy, which, together with mitochondrial biogenesis, plays a key role in maintaining mitochondrial quality control. Maintenance of mitochondrial quality control was initially thought to be autonomously regulated within each cellular population with little exchange between cells. However, recently the phenomenon of transmitophagy has been identified in which damaged mitochondria are transferred to neighboring cells for degradation. This review discusses the current understanding of transmitophagy in the context of heart injury, aging and disease, with particular emphasis on exophers, migrasomes, and tunneling nanotubes as pathways mediating cell-cell communication between cardiomyocytes, macrophages and fibroblasts. We further discuss the potential of targeting transmitophagy for cardioprotection and highlight key unanswered questions and challenges. Addressing these gaps may reveal novel strategies to preserve mitochondrial homeostasis and improve the outcomes of patients with cardiovascular disease.
Targeting glial cells: Unveiling the neuroprotective mechanisms of Ginseng in the brain microenvironment

Acta Pharmaceutica Sinica B. 2026, 16(1): 13-34.

The burden imposed by central nervous system disorders (CNSD) on global health is substantial, characterized by a significant impact on quality of life, increased mortality rates, and escalating economic costs. Glial cells, primarily comprising astrocytes, microglia, oligodendrocytes, and oligodendrocyte precursor cells (OPCs, also known as NG2 cells), play crucial and diverse roles in neurological health and disease. In the treatment of CNSD with traditional herbal medicines, ginseng and its active components have made a notable impression. This comprehensive review investigates the interaction between ginseng and these essential glial cells, detailing their contributions to neurological well-being and disease states. Additionally, it thoroughly assesses the effects of ginseng on glial function, highlighting its neuroprotective potential through anti-inflammatory, antioxidative, and other restorative actions via complex molecular pathways. Moreover, the review analyzes how ginseng can facilitate neuronal viability and regeneration, as well as modulate signaling cascades, thereby highlighting the therapeutic potential of ginseng in the management of CNSD.
Unraveling the FGFR-RNA splicing axis: Mechanisms, oncogenic crosstalks and innovations for therapeutic purpose

Acta Pharmaceutica Sinica B. 2026, 16(1): 35-61.

Fibroblast growth factor receptor (FGFR) signaling is a pivotal regulator of tumor progression, driving cell proliferation, survival, metastasis, and therapeutic resistance across diverse cancer types. RNA alternative splicing profoundly shapes FGFR isoform diversity, endowing tumors with heterogeneity and adaptability to targeted interventions. While significant progress has been made in identifying splicing regulators that govern FGFR pre-mRNA processing, the extracellular cues influencing this process and the reciprocal impact of FGFR signaling pathway on global splicing networks remain underexplored. This review provides a comprehensive overview of the bidirectional interplay linking FGFR signaling and RNA splicing in cancer. Mechanistically, we first detail how FGFR mutations, epigenetic modifications, and crosstalks with oncogenic pathways reprogram splicing to generate tumor-specific FGFR splice variants. We then systematically classify distinct FGFR isoforms and delineate how they contribute to main cancer hallmarks, underscoring the central role of the FGFR-splicing axis in driving tumor plasticity, heterogeneity and adaptive progression. Conversely, we also examine how FGFR signaling modulates RNA splicing programs beyond FGFR itself, reshaping global splicing events that contribute to tumorigenesis, an emerging and still largely unexplored area of cancer biology. From therapeutic perspective, we highlight emerging strategies targeting the axis. Notably, FGFR splicing isoform-directed radiopharmaceuticals hold great promise for patient stratification and biomarker-directed theranostics, providing a precise approach to identify aggressive tumors and guide tailored interventions. As well, complementary approaches, including CRISPR/Cas9-based splicing modulation and long non-coding RNAs-targeted therapies, further expand the toolbox for isoform-specific intervention. Moreover, integrating splicing modulators with FGFR TKIs may overcome drug resistance. Understanding the intricate interplay between FGFR signaling and RNA splicing will not only advance biomarker-guided therapeutic development but also provide a novel framework to counteract tumor adaptability, ultimately improving outcomes in FGFR-driven malignancies.
Computational approaches to druggable site identification: Current status and future perspective

Acta Pharmaceutica Sinica B. 2026, 16(1): 62-92.

With the rapid advancements in computer technology and bioinformatics, the prediction of protein-ligand-binding sites has become a central component of modern drug discovery and development. Traditional experimental methods are often constrained by long experimental cycles and high costs; therefore, the development of accurate and efficient computational methods is of paramount significance for conserving time and cost. This review comprehensively summarizes the methodological advancements and current applications in the field of screening for druggable protein target sites, systematically comparing the fundamental principles, advantages, and disadvantages of four main categories of methods: structure- and sequence-based methods, machine learning-based methods, binding site feature analysis methods, and druggability assessment methods. Subsequently, by integrating classic case studies, this paper elaborately discusses the technical support and theoretical guidance afforded by the screening of protein druggable target sites for drug discovery and drug repositioning. Finally, this paper thoroughly explores the current challenges inherent in the field of protein-ligand binding site prediction, with a particular focus on future technological trends, systematically elucidating the developmental prospects and potential applications of these predictive methods.
Structural biology of HIV-1 reverse transcriptase allosteric inhibitors for drug design

Acta Pharmaceutica Sinica B. 2026, 16(1): 93-121.

HIV-1 reverse transcriptase (RT) is responsible for reverse transcription of viral single-stranded RNA to double-stranded DNA, which plays an important role in the replication cycle of HIV-1 and has been identified as a key target for anti-HIV-1 drug discovery. Among HIV-1 RT inhibitors, allosteric inhibitors acting on non-catalytic sites have the advantages of high efficiency and low cytotoxicity, which are the focus of the research on anti-HIV-1 inhibitors. Great progress has been achieved in the structural biology of HIV-1 RT, which significantly facilitated the development of RT allosteric inhibitors. Herein, we provided a detailed review of the co-crystal structures of small molecule allosteric inhibitors in complex with RT reported in the last decade. Moreover, the strategies to discover novel and efficient inhibitors based on co-crystal structures have also been discussed, expecting to provide a reference for the development of the next-generation anti-HIV-1 drugs.
Omics-based large language models: A new engine for drug discovery innovation

Acta Pharmaceutica Sinica B. 2026, 16(1): 122-136.

Traditional drug discovery suffers from low efficiency and high attrition rates, largely due to the complexity and heterogeneity of human diseases. Omics technologies offer a systems-level perspective for uncovering disease mechanisms and identifying therapeutic targets, but present challenges such as high dimensionality, noise, and heterogeneity. Large language models (LLMs), originally developed for natural language processing, are emerging as powerful tools to address these issues by capturing complex patterns and inferring missing information from large, noisy datasets. We present a three-part framework: (1) Analyzing how LLM architectures and learning paradigms handle challenges specific to genomics, transcriptomics, and proteomics data; (2) Detailing LLM applications in key areas: uncovering disease mechanisms, identifying drug targets, predicting drug response, and simulating cellular behavior; (3) Discussing how insights from omics-integrated LLMs can inform the development of drugs targeting specific pathways, moving beyond single targets towards strategies grounded in underlying disease biology. This framework provides both conceptual insights and practical guidance for leveraging LLMs in omics-driven drug discovery and development.
The progress and perspective of nanomedicine in modulating the tumor immune microenvironment

Nan Lin, Keqin Tan, Yuhao Wei, Songtao Xie, Jiaming Liu, Xuelei Ma

Acta Pharmaceutica Sinica B. 2026, 16(1): 137-168.

The widespread application of nanomedicine in oncology is reshaping cancer treatment paradigms. Using the precise targeting mechanisms and the rapid advancements in nanoscale materials, nanomedicine is driving progress in cancer therapy, particularly within the complex landscape of the tumor immune microenvironment (TIM). This review provides a comprehensive overview of recent studies elucidating the critical role of nanomedicine in modulating the TIM, augmenting the efficacy of immunotherapies, and overcoming therapeutic resistance. Emphasis is placed on the significance of targeted drug delivery systems, innovative nanoscale vaccines, and strategies for reprogramming immunosuppressive cells. Furthermore, the review explores the clinical applicability and prospects of personalized nanomedicine, highlighting its increasingly prominent role in tailored cancer therapeutics.
Immunocyte reprogramming empowers live-cell drug delivery: Mechanistic insights, delivery strategies, and clinical perspectives

Acta Pharmaceutica Sinica B. 2026, 16(1): 169-197.

Conventional drug-delivery systems (DDSs) for oncology often face challenges such as insufficient tumor selectivity, rapid systemic clearance, limited penetration across stromal and immune barriers, and suboptimal biocompatibility. Live immune cell-based drug-delivery systems (LCDDSs) overcome these limitations by exploiting the innate tumor-homing capacity, high biocompatibility, and dynamic tumor microenvironment (TME) interactions intrinsic to leukocytes, facilitating precise targeting with minimal systemic toxicity. Furthermore, immune cells act as “mobile microprocessors”, actively converting precursor payloads into therapeutically functional cargos at the tumor site and dynamically reshaping the TME. Nonetheless, the clinical translation of LCDDSs remains impeded by limited drug-loading capacities, premature payload degradation, potential impairment of immune-cell function, and insufficient persistence in immunosuppressive environments. To overcome these hurdles, immune cell reprogramming via genetic, metabolic, or epigenetic modifications emerges as a promising strategy. Such interventions improve cellular fitness, enhance tumor infiltration, augment payload transport efficiency, confer programmable release profiles, mitigate cellular exhaustion, and increase adaptability to the hostile TME. This review systemically evaluates how immune cell reprogramming advances LCDDSs by examining mechanistic benefits, drug compatibility considerations, payload loading strategies, and design criteria essential for achieving clinical controllability, safety, and scalability. By integrating immune-cell engineering with cutting-edge drug delivery technologies, reprogrammed LCDDSs represent a versatile and powerful platform for next-generation precision oncology therapeutics.
Concerns and challenges in clinics-guided nanovaccines design and applications

Acta Pharmaceutica Sinica B. 2026, 16(1): 198-230.

Vaccines play a crucial role in the prevention and treatment of multiple diseases. Given the constraints of conventional vaccines, the development of nanovaccines, characterized by their superior design flexibility and controllability, has emerged as a compelling alternative. By utilizing nanotechnology, nanovaccines optimize the targeted delivery of antigens and adjuvants, augment antigen presentation, and facilitate precise modulation of immune cell responses, thereby exhibiting substantial potential for both preventive and therapeutic applications across a range of diseases. However, research on nanovaccines is currently stalled at the preclinical stage, with numerous challenges and shortcomings hindering their clinical translation. Herein, we discuss various design concepts and strategies for nanovaccines, along with their biomedical applications, with an emphasis on the challenges, future directions, and strategies of their clinical translation. We specifically highlight the core principles that need to be achieved in the preclinical development of nanovaccines, aiming to explore strategies to overcome existing challenges and promote their clinical application.

Previous 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 61 62 63 64 65 66 67 68 69 70 71 72 Next

Submission

Peer Review

Staff Login